Applications Products Services Documents Support. All Photos (1) Documents. SML3234. This approach Product Description. CAS No. GSK778 (iBET-BD1) is a potent and selective inhibitor of bromodomain (BRD) BD1. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. Storage Class Code. COO/ COA. All Photos (1) SML3234. If not otherwise indicated, cells were pretreated with I-BET151, iBET-BD1, iBET-BD2 or vehicle (DMSO) for 48 hours, irradiated with 0 or 6 Gy, and incubated for additional time intervals with concurrent drug. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Molecular Weight: 511. The two tandem bromodomains of the BET. GSK778 (iBET-BD1) is an analogue of I-BET151 with good potency against BET BD1 (IC 50 = 40 nM) and similar selectivity to LT052 (150-fold) over BD2 [48]. 9. They are epigenetic readers of histone acetylation with broad specificity. Among this class, RVX-208 mainly blocks BD2 function [99], whereas GSK778 is a BD1 selective inhibitor [99]. 5 mg/dL, except in individuals with Gilbert's syndrome. M28843 CAS No. HY-136570 25mg GSK778 CAS: 2451862-42-1 GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 hydrochloride hydrochloride is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Another report showed that BD2-selective BET family inhibitors exhibited good efficacies in treating prostate cancer 22. GSK778 Hydrochloride. COO/ COA. COO/ COA. Solicite agora um orçamentoGSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. SML3234. Available to order from Sigma-Aldrich. Contains a pharmaceutically active ingredient. ≥98% (HPLC)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. S1F, and table S1). It achieves this complex task by recruiting BRD4, via a pan-BET ligand (JQ1), to the GAA repeats by using a sequence-selective DNA-binding polyamide. (a) Phylogenetic tree of bromodomains, with available chemical probes noted; the BET subfamily and the divergence of its first and second bromodomains, BD1 and BD2, are highlighted (adapted from chromohub. SML3234. Email. Discovery of potent BET bromodomain 1 stereoselective inhibitors using DNA-encoded chemical library selections Ram K. Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). SML3234. In contrast to other reported domain-selective molecules, these compounds showed little binding to bromodomains outside of. Membranes were blocked with 5% milk in Tris-buffered saline (TBS) with 0. GSK778, a potent pan-D1 inhibitor, was reported by Gilan et al. (A) Schematic of the BET bromodomain proteins and chemical structures. 5. 0; BRD4 (BD2) pKd = 5. GSK778 has a more pronounced effect on the growth and viability of MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells, GSK778 reduces the clonogenic capacity of primary human AML cells. GSK778 hydrochloride hydrochloride phenocopies the effects of pan-BET inhibitors in cancer models[1]. Applications Products Services Documents Support. 1 μg/mL, which we determined was the equivalent of 1000 units/mL (U/mL) via in-house. Despite their profound preclinical efficacy, the clinical utility of pan-inhibitors is limited due to observed cytotoxicicities. Their affinities for the individual bromodomains of the BET family were initially determined by TR-FRET (Fig. Comparison of the binding modes of CDD-956 with BD1, CDD-1302 with BRDT-BD2 , and iBET-BD1 (GSK778) with BRD4-BD1 (Fig. . Email. Drugs that inhibit both bromodomains equally have shown efficacy in certain malignant and inflammatory conditions. Applications Products Services Documents Support. Download scientific diagram | Correlations of protein vibrational entropy between standard NMA and scaled coarsegrained NMAs: a) sBNM, b) sGNM, and c) sANM. Código de clase de almacenamiento. Applications Products Services Documents Support. 00. GSK778 (iBET-BD1) is a strong BD1 bromodomain inhibitor of the BET proteins, with IC50 value of 75. Their affinities for the individual bromodomains of the BET family were initially determined by TR-FRET (Fig. Email. 0; BRD4 (BD2) pKd = 5. Herein, GSK778 and GSK046 are referred to as iBET-BD1 and iBET-BD2, respectively. COO/ COA. Pan-BD1 inhibitors (which have higher inhibitory activity for BD1 than BD2 of BET proteins) are comparable to pan-BD inhibitors, such as MS436, 59 Olinone, 60 MS402, 61 3U, 62 GSK778, 19 ZL0516, 63 UMN627, 64 and GSK789. Email. Copy Link. Herein, GSK778 and GSK046 are referred to as iBET-BD1 and iBET-BD2, respectively. S9683 Synonyms: iBET-BD1. ≥98% (HPLC)Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). Hazard Description: Toxic. Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months). GSK778 Hydrochloride. , 1999). TC EN. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. BD1 selective inhibitors, such as GSK778, MS-436, Olinone, and BI-2536, as well as the BD2 selective inhibitors RVX-208, RVX-297, GSK046, and ABBV-744 have been produced. GSK778 reduces the production of anti-keyhole limpet. GSK778 Hydrochloride. Copy Link. Copy Link. 125 nM (MV-4−11 cells) ≤. The . GSK778 phenocopies the. to produce antitumor effects in vivo. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. SynTEF1, a prototype synthetic genome reader/regulator (SynGR), was designed to target GAA triplet repeats and restore the expression of frataxin (FXN) in Friedreich’s ataxia patients. I-BET151 (GSK1210151A), iBET-BD1 (GSK778) and iBET-BD2 (GSK046) were provided by GlaxoSmithKline plc (GSK, London, UK). Email. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. Instead, a unique effect of BD2-selective antagonism was revealed with GSK046 affecting the induction of gene expression more so than the expression of steady-state genes, in contrast to GSK778 . WGK 3. MCP-1 in LPS-stimulated PBMCs: 1000 <1: 32193360. Available to order from Sigma-Aldrich. We would like to show you a description here but the site won’t allow us. Copy Link. GSK778 Hydrochloride. COO/ COA. GSK778 reduces the production of anti-keyhole limpet. Catalog Number: AA01KEG7. GSK778 Hydrochloride. The calculations of the energy contributions of individual residues demonstrate that residues corresponding to (BD1, BD2) generate significant energy difference in binding of SG3-179, GSK778, and. GSK778에 대한 모든 정보는 Chemicalbook 에서 조회 할 수 있습니다. 8300 Cypress Creek Parkway, Suite 450 Houston. Pharmacological inhibition of BET BDs using the chemical probes JQ1 (Filippakopoulos et al. The addition of olinone to oligodendrocyte progenitor cells demonstrated biological effects divergent from pan-BET inhibition. Safety Information. The distinct families are. ≥98% (HPLC) All Photos (1)GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Available to order from Sigma-Aldrich. ChemScene Provide GSK778(CAS 2451862-42-1)In-stock or Backordered impurities,Bulk custom synthesis,Formular C30H33N5O3,MW 511. Developing BDII selective compounds was far more challenging, and only a handful of BDII selective inhibitors have been developed to date (Figure 1). GSK778 hydrochloride | C30H34ClN5O3 | CID 168013350 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological. 65 ABBV-744 shows potent anti-proliferative effects against. 125 nM (MV-4−11 cells) ≤. Open in a. 5 gsk778 (pan-bd2) ↓mcp-1 in lps-stimulated pbmcs: 1000 <10 gsk791 32193360 6 brd: baz2a/2b baz2-icr frap, baz2a: 1000 1 - 25719566 7 gsk2801 frap, baz2b: 1000 3 gsk8573 25799074 8 brd: brd9/7 bi-9564 frap, brd9/7: 100/1000 1 - 26914985 9 tp-472 nanobret, brd9: 323 (ec 50) 1 tp-472n 10 brd: brd9 i-brd9 nanobret, brd9: 159 1 - 25856009 11 brd. All Photos (1) Documents. ≥98% (HPLC)We would like to show you a description here but the site won’t allow us. ([email protected]) and I. 3 Details of the supplier of the safety data sheet; Company: Abmole Bioscience Inc. Drugs that inhibit both bromodomains equally have shown efficacy in certain malignant and inflammatory conditions. Get latest info on GSK778, suppliers, manufacturers, wholesalers, traders with GSK778 prices for buying. Sigma-Aldrich. Copy Link. Please continue to check back for new reviews and commentary. All Photos (1) Documents. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. 5), is a highly selective BD1 inhibitor (BRD4(1), IC 50 = 41 nM) with a 143-fold selectivity over BD2. AR EN. Flight status, tracking, and historical data for N778SK including scheduled, estimated, and actual departure and arrival times. WGK. (C) X-ray crystal structure of I-BET151 in. Endoplasmic Reticulum Stress Modulator (ERSM) Epigenetics Resch Products. Drugs that inhibit both bromodomains equally have shown efficacy in certain malignant and inflammatory conditions. mil. ≥98% (HPLC)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Email. CAS Number: 2451862-42-1. SML3234. ABBV-744 is highly selective for BD2 of BRD2, BRD3 and BRD4, 64 exhibiting several hundred-fold higher affinity for the BD2 over BD1. DNA/RNA Synthesis Inhibitor/Blocker. Federal government websites often end in . GSK778 is a Potent and Selective Inhibitor of BET BD1 . GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. In almost half of hepatocellular carcinoma (HCC) cases, the Akt pathway is activated. Applications Products Services Documents Support. SML3234. Available to order from Sigma-Aldrich. 8902. GSK778 Hydrochloride. Developing BDII selective compounds was far more challenging, and only a handful of BDII selective inhibitors have been developed to date (Figure 1). SML3234. iBET-BD1 dihydrochloride . Miransertib is an Orally Active Akt Inhibitor for Cancer and Infection Research. This approachGSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. BROMODOMAIN AND EXTRA‐TERMINAL (BET) PROTEINS. Copy Link. I-BET151, GSK778, GSK046 and GSK620 are available from R. Available to order from Sigma-Aldrich. JP EN. 61: Molecular Formula: C 30 H 33 N 5 O 3. All Photos (1) SML3234. All Photos (1) Documents. All Photos (1) Documents. The authors report the development of GSK046 (iBET-BD2), a potent BD2-selective inhibitor with >1000-fold selectivity over BD1. Your information is safe with us. ≥98% (HPLC)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Glatiramer acetate is a mixture of synthetic peptides randomly composed of glutamic acid, lysine, alanine, and tyrosine. Inhibitor/agonist potency: goal is < 50 nM (IC 50, K D) Surpasses criterion: :BET mutant TR-FRET assay: BRD2 (BD1) pIC 50 = 7. Email. Comprar GSK778 na CymitQuimica. The subsequent development and application of GSK778 (BD1 selective) and GSK046 (BD2 selective) revealed that inhibition of BD2 was ineffective in displacing BET proteins from chromatin. WGK 3. Email. Email. The oldest compound, RVX-208 based on a quinazolinone chemical core, exhibited a selectivity of 20-fold with K D values of 4100 nMComprar GSK778 hydrochloride na CymitQuimica a partir de 187,0 €I-BET151 (GSK1210151A), iBET-BD1 (GSK778) and iBET-BD2 (GSK046) were provided by GlaxoSmithKline plc (GSK, London, UK). EG EN. Catalog No. rednibar) and I. All products from TargetMol are for Research Use. COO/ COA. Potent, selective and cell-permeable inhibitors of protein function ("chemical probes") are valued reagents in both fundamental and applied biological research, and they are essential for the early stages of drug discovery by allowing preclinical target validation in both academic and industrial laboratories. 11 - Combustible Solids. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. ([email protected]) under a material transfer agreement with GSK. GSK778 Hydrochloride. Storage Class Code. G-Protein-coupled Receptor Ligands. All Photos (1) Documents. 61 bulk manufacturing, sourcing and procurement. GB EN. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. ≥98% (HPLC)HY-136570 10mg GSK778 CAS: 2451862-42-1 GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. 2 (LPS-PBMC assay) <10. A concentration of 1-2 µM of I-BET151, GSK778, GSK789, or GSK046 was used for cell culture treatments as recommended by our collaborators at GlaxoSmithKline (54–56). GSK778 (iBET-BD1) [GSK reference 1, 5] is an analogue of I-BET151 [68] with good potency against BET BD1s (IC 50 s ≈ 40–75 nM) and similar selectivity to LT052 between the BDs of BRD4 (110-fold -to 140-fold depending on assay format), but this selectivity is slightly lower for BRD2 and BRD3 (30–65-fold). Selectivity profile of I-BET151, iBET-BD1 (GSK778), and iBET-BD2 (GSK046). 33DFTG (TD139) $21. The calculations of the energy contributions of individual residues demonstrate that residues corresponding to (BD1, BD2) generate significant energy difference in binding of SG3-179, GSK778, and. P (moc. and GSK778 (iBET-BD1), a BD1-selective in-hibitor (see the figure). The BD2 selective inhibitor RVX-208 could significantly decrease atherosclerosis in hyperlipidemic apolipoprotein E-deficient mice 14 , and increase high-density lipoprotein cholesterol as well as apolipoprotein A-1 in monkeys 15 . 6 GSK789 (BD1) IC50= 125 nM (MV-4−11 cells) <10: GSK791. IQ EN. Resolution:Description GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. 06 (n = 8); (BD2) 5. Hazard identification. Applications Products Services Documents Support. Safety Information. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. The authors found that in mouse models of various cancers, BD1 inhibition is. 6147. their selectivity. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models [1]. GSK778: GSK778 (iBET-BD1) is a strong BD1 bromodomain inhibitor of the BET proteins, with IC50 value of 75 nM for BRD2 BD1, 41 nM for BRD3 BD1, 41 nM for BRD4 BD1, and 143 nM for BRDT BD1. 61 bulk manufacturing, sourcing and procurement. 1B, fig. Preis und Verfügbarkeit anzeigen. GSK778 offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model. Catalog No. GSK778 Hydrochloride. Hazard identification. Coordinates and structure factors have been deposited in the Protein Data Bank (PDB) with identification code 6SWN, 6SWO, 6SWP and 6SWQ. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778 : Catalog Number: M10828: CAS Number: 2451862-42-1: 1. Instruction. WGK. Heat Shock Protein Research Products. But, how does GSK778 work on the target? Let’s discuss it in detail. MOscan analysis of GSK778 indicated the binding of this compound only to BET bromodomains with strong binding to BET BD1 domains while weakly binding to BET BD2 domains. WGK. E-newsletter Get updates ,discounts and special offers. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. Copy Link. CAS: 2451862-42-1 (free base) Chemical Name: GSK778 2HCl; 4-(2-(Methoxymethyl)-1-((R)-1-phenylethyl)-8-(((S)-pyrrolidin-3-yl)methoxy)-1H. This advance has helped to highlight more distinct roles of BD1 and BD2 ( Figure 5 ). The bromodomain (BD) is a ~110 amino acid motif that binds to acetyl-lysine modifications on histone and non-histone proteins (Dhalluin et al. 4 D and E) shows that our BD1-selective and BD2-selective DECL-derived inhibitors each occupy the same KAc pocket as GSK778 but also access adjacent grooves that differ between the two domain types. Biological Activity：GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC 50 s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Preis und Verfügbarkeit anzeigen. GSK778 phenotyping the role of pan-BET inhibitors in cancer models. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Not for human use. Safety Information. RU EN. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models [1]. Available to order from Sigma-Aldrich. Glioblastoma multiforme (GBM) is the most common and aggressive malignant primary brain tumor in adult humans, characterized by a poor prognosis despite the existence of multimodal therapy []. • GSK778 exhibits >130-fold BD1 selectivity over BD2 due to BD1 Asp144/His433 displacement (Kharenko et al. Some, such as ABBV-744 and GSK778, are optimized for greater selectivity for one of two distinct BET protein bromodomains in an effort to improve therapeutic indices [55, 56]. Copy Link. GSK778 Hydrochloride. ChemicalBook 致力于为化学行业用户提供FREEBASE的性质、化学式、分子式、比重、密度,同时也包括FREEBASE的沸点、熔点、MSDS、用途、作用、毒性、价格、生产厂家、用途、上游原料、下游产品等信息。 Recently, Gilan et al. Its mechanism of action is not fully understood. DC42300: GSK620:manuscript, GSK778 and GSK046 are termed iBETBD1 and - iBET-BD2 respectively. Available to order from Sigma-Aldrich. Shelf Life: >3 years if stored properly. Email. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. 7 B) indicated that GSK778 maintains all of the critical interactions of I-BET151 with BRD4-BD1, including the hydrogen bonding interaction of the 3,5-dimethylisoxazole moiety with the conserved Asn140, the hydrophobic interaction of the aryl ring of the α-methylbenzyl group with the. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. The nitrogen atom in pyrrolidine can form water-mediated hydrogen bonds with Asp144 (replaced with His433 in BRD2(2)) and Asp145, which may be. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. 10 µM; GSK791. GSK778 and GSK046 are termed iBET-BD1 and iBET-BD2 respectively. Available to order from Sigma-Aldrich. Recently, inhibitors were developed that selectively target the first (BD1) and second (BD2) bromodomain of the BET proteins (iBET-BD1 [GSK778] and iBET-BD2 [GSK046]). SML3234. CAS Number: 2451862-42-1. All Photos (1) SML3234. 02:05PM IST Netaji Subhash Chandra Bose Int'l - CCU. P (moc. Primary Citation of Related Structures: 6SWN, 6SWO, 6SWP, 6SWQ. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC 50 s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. 27, 42. Available to order from Sigma-Aldrich. Safety Information. In contrast to other reported domain-selective molecules, these compounds showed little binding to bromodomains. 1. Potency in Cells and Cellular Target Engagement: GSK778 engages the target in HEK293 cells: pIC50 = 7. GSK778 phenocopied the effects of pan-BET inhibitors in cancer models. COO/ COA. gov means it’s official. All products from TargetMol are for Research Use Only. GSK778 Hydrochloride. Drug Formulation: This drug may be formulated in DMSO. All Photos (1) SML3234. ID EN. WGK 3. GSK789 was derived from a series of naphthyridone ATAD2 inhibitors. Copy Link. Chemical Structure. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Copy Link. 4 D and E) shows that our BD1-selective and BD2-selective DECL-derived inhibitors each occupy the same KAc pocket as GSK778 but also access adjacent grooves that differ between the two domain types. 1. Not for human use. For research use only. described the development of GSK778 (iBET-BD1) and GSK046 (iBET-BD2), the first highly selective small-molecule inhibitors of BET-BD1 and BET-BD2, respectively . SML3168. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Email. GSK778 Hydrochloride. GSK778. CAS# 2451862-42-1. Lagerklassenschlüssel. , 2016). Applications Products Services Documents Support. 5 ± 0. amni) under a material transfer agreement with GSK. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. In spite of the structural similarity to RVX-208, RVX-297 has demonstrated a different pharmacodynamical profile, as well as distinct cellular and biological activity which was elucidated in the. GSK778, also known as iBET-BD1, is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). The mammalian bromodomain and extra-terminal domain (BET) family of proteins consists of four conserved members (Brd2, Brd3, Brd4, and Brdt) that regulate numerous cancer-related and immunity-associated genes. GSK778 (iBET-BD1) is a potent and selective inhibitor of the BD1 bromine domain of the BET protein,IC50 The values are 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1). 53 reported the development route of iBET-BD1 from a pan-BET imidazoquinolinone-based inhibitor with a slight BD1-bias, iBET151. Available to order from Sigma-Aldrich. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. The calculations of the energy contributions of individual residues demonstrate that residues corresponding to (BD1, BD2) generate significant energy difference in binding of SG3-179, GSK778, and. Coordinates and structure factors have been deposited in the Protein Data Bank (PDB) with identification codes 6SWN, 6SWO, 6SWP, and 6SWQ. e. Miransertib is a highly selective, orally active, pan-Akt inhibitor. Fig. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC 50 s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. BG EN. Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months). Storage Class Code. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. GSK778 is a potent and selective inhibitor of BD1 bromodomain such as BRD2 BD1 (IC50s = 75 nM), BRD3 BD1 (IC50s = 41 nM), BRD4 BD1 (IC50s = 41 nM), and BRDT BD1 (IC50s = 143 nM). All Photos (1) Documents. GSK789 was derived from a series of naphthyridone ATAD2 inhibitors. GSK778: CAS Registry Number: 2451862-42-1: Molecular Weight: 511. INTRODUCTION. More than 7 days of UK778 history is available with an upgrade to a Silver (90 days), Gold (1 year), or Business (3 years) subscription. All Photos (1) Documents. 10 µM; GSK791. All Photos (1) Documents. Description: GSK778, also known as iBET-BD1, is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). Coordinates and structure factors have been deposited in the Protein Data Bank (PDB) with identification code 6SWN, 6SWO, 6SWP and 6SWQ. GSK778 inhibits proliferation, induces a cell cycle arrest and apoptosis. Recently, BET proteins inhibitors that selectively target BD1 (GSK778, MS-436, Olinone, and BI-2536) and BET proteins inhibitors that selectively target BD2 (GSK046, RVX-208, RVX-297, ABBV-744) have been developed [42-47]. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Catalog Number: AA01KEG7. from publication: Fast and Accurate. No; GlaxoSmithKline The mammalian bromodomain and extra-terminal domain (BET) family of proteins consists of four conserved members (Brd2, Brd3, Brd4, and Brdt) that regulate numerous cancer-related and immunity-associated genes. showed that BD(1)-specific GSK778 phenocopied the effects of pan-BET BRD inhibitors, while GSK046 and its orally bioavailable GSK620 derivative had minimal impact on cell viability while impairing the induction, but not the maintenance, of transcriptional programs [133]. Le GSK778 montre également de forts effets anti-cancéreux in vivo, prolongeant la survie de souris atteintes de leucémies myéloïdes aiguë [422, 423].