MFH290

MFH290 : Covalent inhibitor of CDK12, CDK13

Structure

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Probe MFH290 is in the process of SERP review.

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Information

CDK12
CDK13

Covalent

up to 100 nM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: Q9NYV4

Target Class: Kinase

Target SubClass: CMGC

Potency: IC50

Potency Value: 25 nM

Potency Assay: Biochemical assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Cyclin-dependent kinase 12, KIAA0904, CRKRS, CRK7, ...

DOI Reference: 10.1021/acs.jmedchem.9b01929

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): MFH290 was tested on an extensive enzymatic CDKs panel which included CDKs 1–9, 12–14, and 16. The measured IC50 values across all other CDKs were higher than 100 nM, indicating that MFH290 did not potently inhibit any of these CDKs Outside target family: DiscoverX’s KinomeScan binding assays against a panel of 468 kinases at a concentration of 1 μM: MFH290 exhibits exquisite selectivity with CDK13 as the only potently inhibited target.

Probe Selectivity in Vitro:

CDK1: 1470 nM (Z’-Lyte); CDK2: 120 nM (Z’-Lyte); CDK3: 366 nM (LanthaScreen™ Eu); CDK4: >10000 nM (Adapta); CDK5: 1130 nM (Z’-Lyte); CDK6: >10000 nM (Adapta); CDK7: 6020 nM (Adapta); CDK8: 4490 nM (LanthaScreen™ Eu); CDK9: 114 nM (Adapta); CDK12: 25 nM (Radioisotope); CDK13: 49 nM (Radioisotope); CDK14: 3130 nM (LanthaScreen™ Eu); CDK16: 3830 nM (LanthaScreen™ Eu)

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(last updated: 22 Feb 2023 )