SML3447

GO289

Name: GO289
Brand: SIGMA

≥98% (HPLC)

别名:

(E)-5-Bromo-2-methoxy-4-((3-(methylthio)-5-phenyl-4H-1,2,4-triazol-4-ylimino)methyl)phenol, 5-Bromo-2-methoxy-4-[[[3-(methylthio)-5-phenyl-4H-1,2,4-triazol-4-yl]imino]methyl]phenol, GO 289, GO-289

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关于此项目

经验公式（希尔记法）:

C₁₇H₁₅BrN₄O₂S

化学文摘社编号:

694522-87-7

分子量:

419.30

UNSPSC Code:

12352200

NACRES:

NA.77

MDL number:

MFCD03718152

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assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Quality Level

100

Biochem/physiol Actions

GO289 is a highly potent and selective casein kinase CK2 (CKII) inhibitor (IC50 = 7 nM/CK2, 13 μM/PIM2, >50 μM/CLK2; <50% inhibition of CK1α/δ/γ and 56 other kinases at 5 μM) that targets CK2-specific residues (CK2α V66, M163, and H160) with more overall interactions at the CK2 ATP-binding pocket than TBB, DMAT & CX-4945. GO289 selectively inhibits cellular CK1 substrates phosphorylation (0.8-8 μM; HEK293T, U2OS), including clock proteins PER2, CRY1, CLOCK & BMAL1, and displays circadian period-lengthening (Bmal1-dLuc USOS EC50 = 3.3 μM) as well as growth inhibitory potency in CK2-dependent human renal cell carcinoma (RCC) cultures.

Potent and highly selective CK2 (CKII) inhibitor with circadian period-lengthening and cancer growth inhibitory efficacy in human renal cell carcinoma cultures.