SML2994

HQ461 Hydrobromide

≥98% (HPLC)

• Synonym(s): 2-(2-((6-Methylpyridin-2-yl)amino)thiazol-4-yl)-N-(5-methylthiazol-2-yl)acetamide hydrobromide, 2-[(6-Methyl-2-pyridinyl)amino]-N-(5-methyl-2-thiazolyl)-4-thiazoleacetamide hydrobromide
• Empirical Formula (Hill Notation): C₁₅H₁₅N₅OS₂HBr
• Molecular Weight: 426.35
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

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

Description

Biochem/physiol Actions

CDK12 kinase domain-targeting molecular glue that impairs CDK12/13 downstream signaling by inducing cyclin K (CycK) ubiquitination and degradation.

HQ461 is a CDK12 kinase domain-targeting molecular glue that promotes CDK12 interaction with DDB, resulting in DDB1-CUL4-RBX1 E3 ubiquitin ligase complex-mediated CDK12-interacting protein cyclin K (CycK) polyubiquitination and degradation (1-10 μM; A549). HQ461 treatment impairs A549 cellular CDK12 and CDK13 downstream signaling events, including RNA pol II C-terminal domain (CTD) Ser2 phosphorylation (1-10 μM) and DNA damage response genes expression (10 μM, 16 hrs).

Safety Information

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