1. Cell Cycle/DNA Damage PROTAC
  2. CDK Molecular Glues
  3. HQ461

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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HQ461 Chemical Structure

HQ461 Chemical Structure

CAS No. : 1226443-41-9

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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Description

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[1].

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.

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 10 μM
Incubation Time: 0-8h
Result: Induces 50% reduction of CDK12 protein level at 8 h, and >8 fold reduction of the CCNK protein level at 4 h.
Molecular Weight

345.44

Formula

C15H15N5OS2

CAS No.
Appearance

Solid

Color

Gray to light brown

SMILES

O=C(NC1=NC=C(C)S1)CC2=CSC(NC3=NC(C)=CC=C3)=N2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8949 mL 14.4743 mL 28.9486 mL
5 mM 0.5790 mL 2.8949 mL 5.7897 mL
View the 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.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Purity & Documentation
References

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
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HQ461 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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HY-144981
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