HQ461
Based on 2 publication(s) in Google Scholar
HQ461 is a molecular glue that promotes CDK12-DDB1 interaction to trigger cyclin K degradation. HQ461-mediated degradation of cyclin K impairs CDK12 function, resulting in decreased CDK12 substrate phosphorylation, downregulation of DNA damage response genes, and cell death.
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- Pureza: 98.10%
- No. CAS: 1226443-41-9
- Fòrmula: C15H15N5OS2
- Peso molecular:345.44
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) HQ461
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Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
1.3 μM
Compound: HQ461
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Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by Cell-titer glo luminescent assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by Cell-titer glo luminescent assay
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[PMID: 37984298] |
| HCT-116 | IC50 |
1.3 μM
Compound: HQ461
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Cytotoxicity against human HCT-116 cells assessed a s reduction in cell growth incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human HCT-116 cells assessed a s reduction in cell growth incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay
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[PMID: 37984298] |
In Vitro
HQ461 inhibits A549 viabilbity with an IC50 of 1.3 µM[1].
HQ461 (10 μM, 8 h) reduces CDK12 protein level in A549 cells[1].
HQ461 (0-10 μM) mediates recruitment of CDK12/CCNK to DDB1 in A549 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cells
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Concentration:10 μM
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Incubation Time:0-8h
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Result:Induces 50% reduction of CDK12 protein level at 8 h, and >8 fold reduction of the CCNK protein level at 4 h.
Chemical Information
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No. CAS 1226443-41-9
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Appearance Solid
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Peso molecular 345.44
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Fòrmula C15H15N5OS2
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Color Gray to light brown
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SMILES
O=C(NC1=NC=C(C)S1)CC2=CSC(NC3=NC(C)=CC=C3)=N2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Sci Adv
Cyclin K condensates bridge CDK12 to phosphorylate and drive oncogenic YAP activation in hepatocellular carcinoma. [Abstract]2026 Jul 3;12(27):eaec6492. PMID: 42397909 -
bioRxiv
2025 Nov 3:2025.11.02.685764. PMID: 41279360
Solvente y solubilidad
In Vitro:
DMSO : 62.5 mg/mL (180.93 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Ethanol : < 1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8949 mL | 14.4743 mL | 28.9486 mL | 72.3715 mL |
| 5 mM | 0.5790 mL | 2.8949 mL | 5.7897 mL | 14.4743 mL | |
| 10 mM | 0.2895 mL | 1.4474 mL | 2.8949 mL | 7.2371 mL | |
| 15 mM | 0.1930 mL | 0.9650 mL | 1.9299 mL | 4.8248 mL | |
| 20 mM | 0.1447 mL | 0.7237 mL | 1.4474 mL | 3.6186 mL | |
| 25 mM | 0.1158 mL | 0.5790 mL | 1.1579 mL | 2.8949 mL | |
| 30 mM | 0.0965 mL | 0.4825 mL | 0.9650 mL | 2.4124 mL | |
| 40 mM | 0.0724 mL | 0.3619 mL | 0.7237 mL | 1.8093 mL | |
| 50 mM | 0.0579 mL | 0.2895 mL | 0.5790 mL | 1.4474 mL | |
| 60 mM | 0.0482 mL | 0.2412 mL | 0.4825 mL | 1.2062 mL | |
| 80 mM | 0.0362 mL | 0.1809 mL | 0.3619 mL | 0.9046 mL | |
| 100 mM | 0.0289 mL | 0.1447 mL | 0.2895 mL | 0.7237 mL |
HQ461 Related Classifications
HY-144981 Related Classifications
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