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GSK046

Catalog No. T8932 CAS 2474876-09-8

Synonyms: iBET-BD2

GSK046 (iBET-BD2) is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins(IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively). It has immunomodulatory activity.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

GSK046, CAS 2474876-09-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 115.00
5 mg	In stock	$ 247.00
10 mg	In stock	$ 397.00
25 mg	In stock	$ 663.00
50 mg	In stock	$ 945.00
100 mg	In stock	$ 1,280.00
1 mL * 10 mM (in DMSO)	In stock	$ 272.00

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Purity: 99.94%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GSK046 (iBET-BD2) is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins(IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively). It has immunomodulatory activity.
Targets&IC50	BRD4 BD2:49 nM (IC50), BRD3 BD2:98 nM (IC50), BRDT BD2:214 nM (IC50), BRD2 BD2:264 nM (IC50)
In vivo	GSK046 (40 mg/kg/QD;?s.c. for 14 days) has immunomodulatory activity.?GSK046 exhibits Cmax (C57BL6 1589, C57B16 2993 ng/mL) and terminal elimination half-lives (C57BL6 1.8, C57B16 1.9 h) following oral administration (C57BL6 10, C57B16 40 mg/kg).?GSK046 exhibits Cmax (mouse 1589, rat 202 ng/mL) and terminal elimination half-lives (mouse 1.8, rat 1.4 h) following oral administration (mouse 10, rat 10 mg/kg)[1].

Synonyms	iBET-BD2
Molecular Weight	414.47
Formula	C23H27FN2O4
CAS No.	2474876-09-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 83.33 mg/mL (201.05 mM), Sonification is recommended.

References and Literature

1. Omer G, et, al. Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation. Science. 2020 Apr 24; 368(6489): 387-394. 2. The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor[J]. Journal of Medicinal Chemistry, 2020, 63(17):9093-9126.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compounds Library Max Reprogramming Compound Library Epigenetics Compound Library PPI Inhibitor Library Orally Active Compound Library Immunology/Inflammation Compound Library Bioactive Compound Library NO PAINS Compound Library Histone Modification Compound Library

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Related compounds with same targets

BAY-850 Eleven-Nineteen-Leukemia Protein IN-2 ZEN-3219 MS7972 BRD7-IN-3 Hexamethylene bisacetamide C-82 BRD4-IN-4

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

GSK046 2474876-09-8 Chromatin/Epigenetic Epigenetic Reader Domain GSK-046 BRDT BRD2 inhibit immuno-inflammation iBET-BD2 BRD4 GSK 046 Inhibitor BD2 BRD3 inhibitor

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