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GSK046

GSK046 (iBET-BD2), a chemical probe, is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins, with IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively. GSK046 has immunomodulatory activity[1].

Product Specifications

CAS Number

[2474876-09-8]

Product Name Alternative

IBET-BD2

UNSPSC

12352005

Target

Epigenetic Reader Domain

Type

Reference compound

Related Pathways

Epigenetics

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/gsk046.html

Purity

99.65

Solubility

DMSO : 83.33 mg/mL (ultrasonic)

Smiles

O=C(N[C@H]1CC[C@H](O)CC1)C2=CC(O[C@H](C3=CC=CC=C3)C)=C(NC(C)=O)C(F)=C2

Molecular Formula

C23H27FN2O4

Molecular Weight

414.47

References & Citations

[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.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

BRD2; BRD3; BRD4; BRDT

Available Sizes

Curated Selection

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