CDK Inhibitor

CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC₅₀ of 6 μM and a K_i of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases.

CDK2 degrader 4 (compound 104) is a potent CDK2 degrader. CDK2 degrader 4 has the potential for the research of cancer.

GSK-3 inhibitor 3 is a selective, orally active and brain-penetrant inhibitor of GSK-3, with IC₅₀s of 0.35 nM and 0.25 nM for GSK-3α and GSK-3β, respectively. GSK-3 inhibitor 3 lowers levels of tau protein phosphorylation at S396 in a triple-transgenic mouse Alzheimer’s disease model, with IC₅₀ of 10 nM. GSK-3 inhibitor 3 can be used for neurological disease research.

YKL-1-116 is a selective and covalent inhibitor of Cdk7. YKL-1-116 does not target Cdk9, Cdk12, or Cdk13. YKL-1-116 is more potent than THZ1 (HY-80013) toward both Cdk7^WT and Cdk7^as, although Cdk7^as is relatively resistant to this compound as well.

Cdk1/2 Inhibitor III (compound 3n) is a highly potent and selective Cdk1/cyclin B and Cdk2/cyclin A inhibitor of with IC₅₀s of 0.6 nM and 0.5 nM, respectively. Cdk1/2 Inhibitor III shows selectivity over VEGF-R2 (IC₅₀ of 32 nM), GSK-3β (IC₅₀ of 140 nM), and a other kinases. Cdk1/2 Inhibitor III inhibits in cell proliferation with IC₅₀s of 20 nM, 35 nM and 92 nM for HCT-116, HeLa, and A375 cells, respectively.

Vanicoside B is a phenylpropanoyl sucrose derivative, can be isolated from the herb Persicaria dissitiflora. Vanicoside B targets cyclin-dependent kinase 8 (CDK8) and exhibits anti-tumor activity. The potential mechanism is Vanicoside B blocks CDK8-mediated signaling pathways and decreases the expression of epithelial-mesenchymal transition proteins, so that it leads to cell cycle arrest and apoptosis.

CDK8-IN-11 is a potent and selective CDK8 inhibitor with an IC₅₀ value of 46 nM. CDK8-IN-11 inhibits WNT/β-catenin signaling pathway. CDK8-IN-11 can be used in the research of colon cancer.

BS-194 is an orally active, selective and potent CDK inhibitor. BS-194 inhibits CDK2, CDK1, CDK5, CDK7, CDK9 (IC₅₀s: 3, 30, 30, 250, and 90 nM respectively). BS-194 potently inhibits cancer cells proliferation. BS-194 can be used in the research of cancers like breast cancer, colon cancer.

CDK8-IN-4 is an inhibitor of CDK8 extracted from patent WO2014090692A1, compound example 16, with an IC₅₀ of 0.2 nM.

CDK7/12-IN-1 is a selective CDK7/12 inhibitor with IC₅₀s of 3 and 277 nM for CDK7 and CDK 12, respectively. CDK7 and CDK12 inhibition is an effective strategy to inhibit tumour growth.

Cdk5i peptide is a CDK5 inhibitory peptide with high binding affinity for Cdk5/p25 (K_d of 0.17 μM), which can block the interaction between CDK5 and p25 and reduce the kinase activity of CDK5/p25. Cdk5i peptide can be used in the stud y of neurodegenerative diseases.

CDK-IN-6, a class of pyrazolo[1,5-a]pyrimidine compound, is a CDK inhibitor with anticancer activities.

CDK9-IN-2 is a special cyclin-dependent kinase 9 (CDK9) inhibitor, extracted from patent WO/2012131594A1, compound CDKI(8), has an IC₅₀ of 5 nM and 7 nM in H929 multiple myeloma(MM) cell line (72 hours) and A2058 skin cell line (72 hours), respectively.

Atuveciclib Racemate (BAY-1143572 Racemate) is the racemate mixture of Atuveciclib. Atuveciclib is a potent and highly selective, oral P-TEFb/CDK9 inhibitor which supresses CDK9/CycT1 with an IC₅₀ of 13 nM.

(S)-PHA533533 is a CDK2 and CDK5 inhibitor with blood-brain barrier permeability, with IC₅₀ values of 37 nM and 55 nM, respectively. (S)-PHA533533 effectively restores UBE3A expression by downregulating UBE3A-ATS and relieving the epigenetic silencing of paternal UBE3A in mature neurons. (S)-PHA533533 can be used for the research of Angelman syndrome.

CDK9-IN-8 is a highly effective and selective CDK9 inhibitor with an IC₅₀ of 12 nM.

CDK4/6-IN-2 is a potent CDK4 and CDK6 inhibitor extracted from patent US20180000819A1, Compound 1, has IC₅₀s of 2.7 and 16 nM for CDK4 and CDK6, respectively.

Avotaciclib (BEY1107) trihydrochloride is an orally active cyclin-dependent kinase 1 (CDK1) inhibitor. Avotaciclib trihydrochloride can inhibit the proliferation and induce apoptosis of tumor cells. Avotaciclib trihydrochloride can be used in the research of cancer such as pancreatic cancer and lung cancer.

BLK degrader 1 is a selective B lymphoid tyrosine kinase (BLK) degrader with a BLK DC₅₀ of 49 nM in cells. BLK degrader 1 induces ubiquitin-proteasome-dependent BLK degradation through binding. BLK degrader 1 exhibits anticancer activity in multiple B lymphocyte cell lines and downregulates CDK2 protein levels. BLK degrader 1 can be used in research related to B cell lymphoma.

Crozbaciclib (CDK4/6/1 Inhibitor) is a CDK4/6 inhibitor with IC₅₀s of 3 and 1 nM, respectively.