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Merck
CN

SML2994

Sigma-Aldrich

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

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About This Item

Empirical Formula (Hill Notation):
C15H15N5OS2HBr
Molecular Weight:
426.35
UNSPSC Code:
12352200
NACRES:
NA.77
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Quality Level

Assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: 2 mg/mL, clear (warmed)

storage temp.

2-8°C

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).

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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