SML3447

GO289

≥98% (HPLC)

• Synonym(s): (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
• Empirical Formula (Hill Notation): C₁₇H₁₅BrN₄O₂S
• CAS Number: 694522-87-7
• Molecular Weight: 419.30
• MDL number: MFCD03718152
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C

Description

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.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable