cdk12 — TargetMol Chemicals

Cat No.	Product Name	Synonyms	Targets
T39752	CDK12-IN-2	CDK12 inhibitor 2,CDK12-IN-2	CDK
	CDK12-IN-2 (CDK12 inhibitor 2) is an effective and selective inhibitor of CDK12 with an IC50 of 52 nM, >100 μM, >10 μM and 16 μM for CDK12, CDK2, CDK7, and CDK9. CDK12-IN-2 can be used in studies about the function of CD...		CDK
T40290	CDK12-IN-5	CDK12-IN-5
	CDK12-IN-5 is a pyrazolotriazine compound that effectively inhibits CDK12, with an IC50 value of 23.9 nM at a high ATP concentration of 2 mM. However, CDK12-IN-5 does not exhibit inhibitory effects on CDK2/Cyclin E (IC50...
T40288	CDK12-IN-4	CDK12-IN-4
	CDK12-IN-4, a pyrazolotriazine compound, exhibits potent inhibition of CDK12 by achieving an IC50 value of 0.641 μM, utilizing high ATP levels (2 mM). Notably, CDK12-IN-4 does not impact CDK2/Cyclin E (IC50 > 20 μM) or C...
T40289	CDK12-IN-6	CDK12-IN-6
	CDK12-IN-6, a pyrazolotriazine compound, is a powerful inhibitor of CDK12. Its inhibitory activity is significant with an IC50 value of 1.19 μM when tested at high ATP concentration (2 mM). Notably, CDK12-IN-6 does not e...
T14915	CDK12-IN-E9		CDK
	CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and non-covalent CDK9 inhibitor while avoiding ABC transporter-mediated efflux. It has a weak binding ability to CDK7/CyclinH complex (IC50> 1 μM).		CDK
T14990	CDK12-IN-3		CDK
	CDK12-IN-3 is a selective CDK12 inhibitor (IC50: 491 nM in an enzymatic assay).		CDK
T64284	PROTAC CDK12/13 Degrader-1
	PROTAC CDK12/13 Degrader-1 (7f) is a potent and selective dual degrader of the cell cycle protein-dependent kinases CDK12 (DC50: 2.2 nM) and CDK13 (DC50: 2.1 nM). Breast cancer.
T9117	BSJ-4-116		CDK , Ligand for E3 Ligase
	BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. It downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation).		CDK , Ligand for E3 Ligase
T9849	HQ461		CDK , Molecular Glues
	HQ461 is a molecular glue that promotes CDK12-DDB1 interaction to trigger cyclin K degradation, resulting in decreased CDK12 substrate phosphorylation, downregulation of DNA damage response genes, and cell death.		CDK , Molecular Glues
T9758	DCeMM3	2-(1H-benzimidazol-2-ylsulfanyl)-N-(5-chloropyridin-2-yl)acetamide	Others
	dCeMM3 (2-(1H-benzimidazol-2-ylsulfanyl)-N-(5-chloropyridin-2-yl)acetamide) is a glue degrader. dCeMM3 prompts an interaction of CDK12-cyclin K with a CRL4B ligase complex, result in inducing ubiquitination and degradati...		Others
T8325	SR-4835		Apoptosis , CDK
	SR-4835 is a highly selective dual inhibitor of CDK12 and CDK13(CDK12: IC50=99 nM, Kd=98 nM; CDK13: Kd=4.9 nM), which disables triple-negative breast cancer (TNBC) cells		Apoptosis , CDK
T4293	THZ531		CDK
	THZ531 is a covalent inhibitor of both CDK12(IC50=158 nM) and CDK13(IC50=69 nM).		CDK
T61477	DCeMM2		Molecular Glues
	dCeMM2 is a glue degrader. dCeMM2 prompts an interaction of CDK12-cyclin K with a CRL4B ligase complex, leading to the ubiquitination and degradation of cyclin K.		Molecular Glues
T22461	YKL-5-124		CDK
	YKL-5-124, a potent, selective and covalent CDK7 inhibitor with an IC50 of 9.7 nM, 1300 nM and 3020 nM for CDK7/Mat1/CycH, CDK2 and CDK9 respectively, displays biochemical and cellular selectivity for CDK7 over CDK12/13...		CDK
T3664	THZ1	CDK7 inhibitor,THZ1 2HCl	CDK
	THZ1 (CDK7 inhibitor) is a novel selective and potent covalent CDK7 inhibitor.		CDK
T74359	PP-C8
	PP-C8, a potent and selective PROTAC CDK12-Cyclin K degrader, efficiently induces degradation of CDK12 and Cyclin K, with DC50 values of 416 nM and 412 nM, respectively. This compound exhibits significant synergistic ant...
T63841	BSJ-01-175
	BSJ-01-175 is a selective and potent covalent inhibitor of CDK12/13. BSJ-01-175 is significantly selective for cancer cells, exhibits potent inhibition of phosphorylated RNA polymerase II, and significantly downregulates...
T69931	MFH290
	MFH290 is a novel cysteine (Cys)-directed covalent inhibitor of CDK12/13. MFH290 forms a covalent bond with Cys-1039 of CDK12, exhibits excellent kinome selectivity, inhibits the phosphorylation of serine-2 in the C-term...
T61057	DCeMM4
	dCeMM4 (Compound 5) is a glue degrader that induces cyclin K ubiquitination and degradation through prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex [1].
T72512	THZ1 Hydrochloride
	THZ1 Hydrochloride is a potent, selective covalent inhibitor of CDK7, exhibiting an IC50 value of 3.2 nM. It also targets closely related kinases CDK12 and CDK13, leading to the downregulation of MYC expression.