- Cat. No.
- A17029
BAY-1251152
BAY-1251152, also known as (+)-BAY-1251152, is a CDK9 inhibitor.
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- Cat. No.
- A17036
THZ531
THZ531 is a covalent CDK12 and CDK13 covalent inhibitor. THZ531 irreversibly targets a cysteine located outside the kinase domain. THZ531 causes a loss of gene expression with concurrent loss of elongating and hyperphosphorylated RNA polymerase II.
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- Cat. No.
- A17084
Trilaciclib
Synonyms: G1T28
Trilaciclib is a potential first-in-class short-acting CDK4/6 inhibitor in development to preserve hematopoietic stem cells and enhance immune system function during chemotherapy.
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- Cat. No.
- A17086
SEL120-34A
SEL120-34A is a potent and selective CDK8 inhibitor active in AML cells with high levels of serine phosphorylation of STAT1 and STAT5 transactivation domains.
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- Cat. No.
- A17124
TG 003
TG 003 is a CDC2 link kinase inhibitor that inhibits Clk1 and Clk4 with IC50 values of 20 and 15 nM, respectively.
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- Cat. No.
- A18058
Ribociclib succinate
Synonyms: LEE011 succinate
Ribociclib succinate is an orally active inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), functioning through ATP-competitive mechanisms. It demonstrates potent activity with IC50 values of 10 nM and 39 nM against CDK4 and CDK6, respectively, while exhibiting over 1,000-fold selectivity against the cyclin B/CDK1 complex. This selectivity makes it a valuable tool in cancer research, particularly in studies targeting cell cycle regulation and therapeutic strategies for hormone receptor-positive breast cancer.
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- Cat. No.
- A18059
Ribociclib succinate hydrate
Synonyms: LEE011 succinate hydrate
Ribociclib succinate hydrate is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), functioning through competitive inhibition of ATP binding. With IC50 values of 10 nM and 39 nM against CDK4 and CDK6, respectively, it demonstrates significant selectivity over the cyclin B/CDK1 complex. This compound is utilized in cancer research, particularly in studies focusing on cell cycle regulation, tumor proliferation, and the therapeutic potential in various malignancies. Its ability to cross the blood-brain barrier allows for exploration in central nervous system-related cancers.
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- Cat. No.
- A18320
Lerociclib (G1T38)
Synonyms: G1T-38
Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC50s of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.
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- Cat. No.
- A18321
AZD4573
AZD4573 is a potent and selective inhibitor of CDK9, with fast-off binding kinetics and high selectivity versus other kinases, including other CDK family kinases.
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- Cat. No.
- A18416
Abemaciclib Metabolites M2
Abemaciclib Metabolites M2 is a metabolite of abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50s in the range of 1-3 nM. Anti-cancer activity.
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- Cat. No.
- A18482
SY-1365
SY-1365 is a highly selective covalent inhibitor of CDK7. SY-1365 possesses therapeutic potential in both hematological and solid tumors.
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- Cat. No.
- A18559
bio-THZ1
bio-THZ1 is a biotinylated version of THZ1 and binds irreversibly to CDK7. THZ1 is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM.
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- Cat. No.
- A18657
CDK4/6-IN-2
CDK4/6-IN-2 is a potent CDK4 and CDK6 inhibitor with IC50s of 2.7 and 16 nM for CDK4 and CDK6, respectively.
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- Cat. No.
- A18667
CDK2-IN-4
CDK2-IN-4 is a potent and selective CDK2 inhibitor with an IC50 of 44 nM for CDK2/cyclin A, shows 2,000-fold selectivity over CDK1/cyclin B (IC50=86 uM).
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- Cat. No.
- A18769
BI-1347
BI-1347 is a selective inhibitor of CDK8/cyclin C with an IC50 of 1.1 nM.
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- Cat. No.
- A18892
MC180295
MC180295 is a highly selective CDK9 inhibitor (IC50 = 5 nM). MC180295 also inhibits GSK-3α and GSK-3β. MC180295 ((rel)-MC180295) has potent anti-tumor effect.
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- Cat. No.
- A18911
FMF-04-159-2
FMF-04-159-2 is a covalent CDK14 inhibitor. FMF-04-159-2 inhibits CDK14 and CDK2 with IC50s of 39.6 nM and 256 nM in NanoBRET assay, respectively.
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- Cat. No.
- A19222
IIIM-290
IIIM-290 is a potent and oral CDK inhibitor with IC50s of 90 and 94 nM for CDK2/A and CDK9/T1.
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- Cat. No.
- A19458
Toyocamycin
Synonyms: Vengicide
Toyocamycin (Vengicide) is an adenosine analog produced by Actinomycete, acts as an XBP1 inhibitor, inhibits IRE1α-induced ATP-dependent XBP1 mRNA cleavage, with an IC50 of 80 nM.
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- Cat. No.
- A19461
Indirubin-5-sulfonate
Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK) inhibitor, with IC50 values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, and CDK5/p35, respectively.
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- Cat. No.
- A19470
Indirubin-3'-monoxime-5-sulphonic acid
Indirubin-3'-monoxime-5-sulphonic acid is a potent and selective inhibitor of CDK1, CDK5, and GSK-3β with IC50s of 5 nM, 7 nM, and 80 nM, respectively.
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- Cat. No.
- A19479
5-Iodo-indirubin-3'-monoxime
5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase, with IC50s of 9, 20 and 25 nM, respectively.
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- Cat. No.
- A19641
CDK4/6/1 Inhibitor
CDK4/6/1 Inhibitor is a CDK4/6 inhibitor with IC50s of 3 and 1 nM, respectively.
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- Cat. No.
- A19768
CDK12-IN-3
CDK12-IN-3 is a potent and selective CDK12 inhibitor with an IC50 of 491 nM in enzymatic assay.
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- Cat. No.
- A19820
CDK8-IN-4
CDK8-IN-4 is an inhibitor of CDK8 extracted from patent WO2014090692A1, compound example 16, with an IC50 of 0.2 nM.
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