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GSK778

GSK778 (iBET-BD1), a chemical probe, 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 phenocopies the effects of pan-BET inhibitors in cancer models[1].

Product Specifications

CAS Number

[2451862-42-1]

Product Name Alternative

IBET-BD1

UNSPSC

12352005

Target

Apoptosis; Epigenetic Reader Domain

Type

Reference compound

Related Pathways

Apoptosis; Epigenetics

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/gsk778.html

Purity

98.93

Solubility

DMSO : 41.67 mg/mL (ultrasonic)

Smiles

CC1=NOC(C)=C1C2=C(OC[C@@H]3CNCC3)C=C4C5=C(N=C(COC)N5[C@H](C)C6=CC=CC=C6)C=NC4=C2

Molecular Formula

C30H33N5O3

Molecular Weight

511.61

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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