- Cat. No.
- A17029
BAY-1251152
BAY-1251152, also known as (+)-BAY-1251152, is a CDK9 inhibitor.
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CDK inhibitors block cyclin-dependent kinases (CDKs), the serine/threonine kinases that drive the cell cycle. Each CDK becomes active only when bound to a cyclin partner, and successive cyclin-CDK complexes order DNA replication and mitosis. CDK4 and CDK6 pair with D-type cyclins to control progression through G1, while CDK1 governs entry into mitosis. Palbociclib and abemaciclib are selective CDK4/6 inhibitors used to study G1 arrest and retinoblastoma protein phosphorylation. Dinaciclib and seliciclib act on several family members, including CDK2, CDK5 and CDK9, which also links them to transcription research. Ro 3306 inhibits CDK1 and is used to hold cells reversibly at the G2/M boundary for synchronization experiments.
BAY-1251152, also known as (+)-BAY-1251152, is a CDK9 inhibitor.
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.
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.
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.
TG 003 is a CDC2 link kinase inhibitor that inhibits Clk1 and Clk4 with IC50 values of 20 and 15 nM, respectively.
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.
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.
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.
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.
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.
SY-1365 is a highly selective covalent inhibitor of CDK7. SY-1365 possesses therapeutic potential in both hematological and solid tumors.
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.
CDK4/6-IN-2 is a potent CDK4 and CDK6 inhibitor with IC50s of 2.7 and 16 nM for CDK4 and CDK6, respectively.
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).
BI-1347 is a selective inhibitor of CDK8/cyclin C with an IC50 of 1.1 nM.
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.
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.
THAL-SNS-032 is a selective CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).
IIIM-290 is a potent and oral CDK inhibitor with IC50s of 90 and 94 nM for CDK2/A and CDK9/T1.
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.
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.
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.
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.
JH-XI-10-02 is a potent and selective degrader of CDK8, with an IC50 of 159 nM, based on PROTAC.
CDK4/6/1 Inhibitor is a CDK4/6 inhibitor with IC50s of 3 and 1 nM, respectively.