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SML3131

Sigma-Aldrich

GSK620

≥98% (HPLC)

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Synonym(s):
1-Benzyl-N5-cyclopropyl-N3-methyl-2-oxo-1,2-dihydropyridine-3,5-dicarboxamide, GSK 620, GSK-620, N5-Cyclopropyl-1,2-dihydro-N3-methyl-2-oxo-1-(phenylmethyl)-3,5-pyridinedicarboxamide
Empirical Formula (Hill Notation):
C18H19N3O3
CAS Number:
Molecular Weight:
325.36
MDL number:

Quality Level

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

O=C1N(C=C(C=C1C(NC)=O)C(NC2CC2)=O)CC3=CC=CC=C3

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GSK620 ≥98% (HPLC)

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SML3131

GSK620

GSK′962 ≥98% (HPLC)

Sigma-Aldrich

SML2377

GSK′962

GSK′963 ≥98% (HPLC)

Sigma-Aldrich

SML2376

GSK′963

GSK′481 ≥98% (HPLC)

Sigma-Aldrich

SML2745

GSK′481

form

powder

form

powder

form

powder

form

powder

color

white to beige

color

white to beige

color

white to beige

color

white to beige

solubility

DMSO: 2 mg/mL, clear

solubility

DMSO: 2 mg/mL, clear

solubility

DMSO: 2 mg/mL, clear

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

−20°C

Quality Level

100

Quality Level

-

Quality Level

-

Quality Level

100

Biochem/physiol Actions

GSK620 Is an orally active, potent and selective pan-second bromodomain (BD2) inhibitor (BD2/BD1 pIC50 = 6.5/4.6/BRD2, 7.1/4.6/BRD3, 7.1/4.8/BRD4, 6.7/4.6/BRDT) with improved oral availability than GSK046 (iBET-BD2) and in vivo efficacy in inflammatory disease models, including collagen-induced arthritis (3-10 mg/kg/d p.o. in rats), imiquimod (IMQ)-induced psoriasis (20 mg/kg/d p.o. in mice), and a nonalcoholic steatohepatitis (NAFLD) model (20 mg/kg/d p.o. in STAM mice).

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


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