CDK Cyclin-dependent kinase

Inhibitors

Cat.No.	Name	Information
M1806	PD 0332991 HCL	PD-0332991 HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc.
M1974	Roscovitine (Seliciclib)	Roscovitine is a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5.
M1764	PF-477736	PF-477736 is a selective checkpoint kinase 1 (Chk1) inhibitor with Ki values of 0.49 nM and 47 nM for CHK1 and CHK2 respectively.
M2112	LY2835219 mesylate	LY2835219 mesylate is an orally available inhibitor of CDK4 and CDK6 with IC50 of 2 nM and 10 nM, respectively.
M1807	SCH727965 (dinaciclib)	SCH727965 (Dinaciclib) is a potent and selective CDK inhibitor with IC50 values of 1, 1, 3 and 4 nM for CDK2, CDK5, CDK1 and CDK9, respectively.
M11419	Trilaciclib hydrochloride	Trilaciclib hydrochloride (G1T28 Hydrochloride) is an inhibitor of CDK4/6 with IC50 values of 1 nM and 4 nM for CDK4 and CDK6, respectively.
M11249	(+)-Enitociclib	(+) -enitociclib ((+) -bay-1251152) is an enantiomer of Bay-1251152 with optical rotation of (+). (+) -enitociclib is a potent selective CDK9 inhibitor with an IC50 of 3 nM. (+) -enitociclib has antitumor activity.
M11248	LY2857785	LY2857785 is a type I reversible ATP-competitive inhibitor of CDK9, CDK8 and CDK7 with IC50 of 11 nM, 16 nM and 246 nM, respectively.
M11247	CAN508	CAN508 was an effective AND ATP-competitive inhibitor of CDK9/cyclin T1 with IC50 of 0.35 μM. CAN508 is 38 times more selective for CDK9/cyclin T1 than other CDK/cyclin. CAN508 has antitumor activity.
M11018	Cirtuvivint	Cirtuvivint (SM08502) is a potent orally active CDC-like kinase (CLK) inhibitor that can be used in the study of solid tumors.
M11010	Aminopurvalanol A	Aminopurvalanol A is a selective, cell-permeable, reversible and ATP-competitive cyclin-dependent kinase (CDK) inhibitor, inhibiting cdk1/cyclin B, cdk2/cyclin A, cdk2/cyclin E, and cdk5/p35. Aminopurvalanol A causes the inhibition of sperm fertilizing ability via the inhibition of physiological capacitation-dependent actin polymerization.
M10966	SY-5609	SY-5609 (CDK7-IN-3) is an orally potent, highly selective, non-covalent CDK7 inhibitor,KD 为 0.065 nM。 SY-5609 对 CDK2 (Ki=2600 nM)，CDK9 (Ki=960 nM)，CDK12 (Ki=870 nM) has a weaker inhibitory effect. SY-5609 induces apoptosis of tumor cells and has antitumor activity.
M10930	Dalpiciclib	Dalpiciclib (SHR-6390) is a highly selective, oral bioavailable inhibitor of CDK4/6 that is used against CDK4 (IC50=12.4 nM) and CDK6 (IC50=9.9 nM) is equivalent. SHR6390 exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated Rb protein and inducing G1 cell cycle blocking.
M10913	THZ1-R	THZ1-R is a non-cysteine-reactive analogue of THZ1 with reduced activity against CDK7 inhibition. THZ1-R in combination with CDK7 Kd 142 nM.
M10886	Samuraciclib hydrochloride	Samuraciclib (ICEC0942, CT7001) is a novel oral CDK7 inhibitor with an IC50 of 40 nM. It has IC50 values for other CDK proteins such as CDK1, CDK2, CDK5 and CDK9 as 45, 15, 230 and 30 times higher than that of CDK7 IC50, respectively. ICEC0942 (CT7001) promotes cell cycle blocking and apoptosis.
M10879	RGB-286638	RGB-286638 is a potent CDK inhibitor that inhibits cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 activity,IC50 1, 2, 3, 4, 5 and 5 nM, respectively, and can inhibit GSK-3β, TAK1, Jak2 and MEK1.IC50 The values are 3, 5, 50, and 54 nM, respectively.
M10843	KB-0742 dihydrochloride	KB-0742 dihydrochloride is a potent, selective and orally active CDK9 inhibitor against CDK9/cyclin T1 IC50 is 6 nM. KB-0742 dihydrochloride is selective for CDK9/cyclin T1, which is more than 50 times more selective than other CDK kinases. KB-0742 dihydrochloride has potent anti-tumor activity.
M10734	YKL-5-124	YKL-5-124 is a potent, selective, irreversible COVALENT inhibitor of CDK7 and CDK7/Mat1/CycH IC50 53.5 nM and 9.7 nM, respectively. YKL-5-124 is more than 100 times more selective to CDK7 than CDK9 and CDK2 and is inactive to CDK12 and CDK13. YKL-5-124 induces intense cell cycle arrest and inhibits E2F-driven gene expression with little effect on RNA polymerase II phosphorylation status.
M10707	FIT-039	FIT-039 is a selective, ATP-competitive, orally active CDK9 inhibitor against CKD9/cyclin T1 IC50 Is 5.8 μM. FIT-039 does not inhibit other CDKs and other kinases. FIT-039 inhibits HSV-1 (IC50 is 0.69 μM), HSV-2, human adenovirus, and human CMV replication. FIT-039 is a promising antiviral agent that can be used to suppress resistant HSV and other DNA viruses.
M10706	AZD4573	AZD4573 is a potent and highly selective CDK9 inhibitor (IC50 values less than 4 nM) can be used to study hematologic malignancies.
M10705	NVP-2	NVP-2 is an effective and selective ATP competitive cyclin-dependent kinase 9 (CDK9) probe that inhibits CDK9/CycT activity.IC50 The value is 0.514 nM. NVP-2 has inhibitory effects on CDK1/CycB, CDK2/CycA and CDK16/CycY kinases, which IC50 The values are 0.584 μM, 0.706 μM, and 0.605 μM, respectively. NVP-2 induces apoptosis.
M10347	Abemaciclib (LY2835219)	Abemaciclib (LY2835219) is a potent and selective inhibitor for CDK4 and CDK6 with IC50 values of 2 nM and 10 nM, respectively.
M10327	Zotiraciclib	Zotiraciclib (TG02, SB1317) is an orally bioavailable, brain penetrant multi-kinase inhibitor of CDK2, JAK2, and FLT3 with IC50 values of 13, 73, and 56 nM, respectively.
M10258	SR-4835	SR-4835 is a highly selective, dual inhibitor of CDK12 with IC50 values of 99 nM, Kd of 98 nM and CDK13 with Kd of 4.9 nM, respectively.
M10033	Trilaciclib	Trilaciclib (G1T28) is a potent first-in-class reversible CDK4/6 inhibitor with IC50 of 1 nM and 4 nM for CDK4/cyclin D1 and CDK6/cyclin D3, respectively.

Signaling Pathways

Product Type

CDK Cyclin-dependent kinase

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