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MedKoo CAT#: 408174

CAS#: 1226443-41-9 (free base)

Description: HQ461 is a Molecular-glue degrader. HQ461 acts by promoting an interaction between CDK12 and DDB1-CUL4-RBX1 E3 ubiquitin ligase, leading to polyubiquitination and degradation of CDK12-interacting protein Cyclin K (CCNK). Degradation of CCNK mediated by HQ461 compromised CDK12 function, leading to reduced phosphorylation of a CDK12 substrate, downregulation of DNA damage response genes, and cell death. Structure-activity relationship analysis of HQ461 revealed the importance of a 5-methylthiazol-2-amine pharmacophore and resulted in an HQ461 derivate with improved potency.

Chemical Structure

CAS# 1226443-41-9 (free base)

Theoretical Analysis

MedKoo Cat#: 408174
Name: HQ461
CAS#: 1226443-41-9 (free base)
Chemical Formula: C15H15N5OS2
Exact Mass: 345.07
Molecular Weight: 345.439
Elemental Analysis: C, 52.16; H, 4.38; N, 20.27; O, 4.63; S, 18.56

Price and Availability

Size Price Availability Quantity
50mg USD 750 2 Weeks
100mg USD 1250 2 Weeks
200mg USD 1950 2 Weeks
500mg USD 3650 2 Weeks
1g USD 4650 2 Weeks
2g USD 6950 2 Weeks
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Related CAS #: 2755241-76-8 (HBr)   1226443-41-9 (free base)    

Synonym: HQ461; HQ-461; HQ 461;

IUPAC/Chemical Name: 2-(2-((6-methylpyridin-2-yl)amino)thiazol-4-yl)-N-(5-methylthiazol-2-yl)acetamide


InChi Code: InChI=1S/C15H15N5OS2/c1-9-4-3-5-12(17-9)19-15-18-11(8-22-15)6-13(21)20-14-16-7-10(2)23-14/h3-5,7-8H,6H2,1-2H3,(H,16,20,21)(H,17,18,19)


Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 345.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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Lv L, Chen P, Cao L, Li Y, Zeng Z, Cui Y, Wu Q, Li J, Wang JH, Dong MQ, Qi X, Han T. Discovery of a molecular glue promoting CDK12-DDB1 interaction to trigger cyclin K degradation. Elife. 2020 Aug 17;9:e59994. doi: 10.7554/eLife.59994. PMID: 32804079; PMCID: PMC7462607.