cdk5/p35

Olomoucine is an ATP-competitive inhibitor of Cdk2/cyclin A, Cdc2/CyclinB, CDK2/CyclinE, CDK5/p35, and ERK1/p44 MAP kinase with IC50s of 7, 7, 7, 3, and 25 µM, respectively. It regulates the cell cycle and exhibits anti-melanin tumor activities.

(R)-Atuveciclib is an isomer of Atuveciclib. Atuveciclib (BAY 1143572) is a potent and highly selective PTEFb/CDK9 inhibitor with an IC50 value of 13 nm for CDK9/CycT1 and a selectivity ratio of 100 for CDK2, with highly bioavailable and orally available advantages.

Atuveciclib (BAY 1143572) is a potent and highly selective PTEFb/CDK9 inhibitor with an IC50 value of 13 nm for CDK9/CycT1 and a selectivity ratio of 100 for CDK2, with highly bioavailable and orally available advantages.

Lerociclib (G1T38) is a selective and highly potent CDK4/6 inhibitor with anticancer and antitumor activity, inhibits CDK4/CyclinD1 and CDK6/CyclinD3, and inhibits tumor growth in an animal model of endocrine-resistant breast cancer. Due to the poor solubility, for animal studies, the salt form T11345L is recommended.

Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potent and selective CDK4/CDK6 inhibitor, with IC50 values of 2 nM for CDK6/CyclinD3 and 1 nM for CDK4/CyclinD1.

Indirubin-5-sulfonate shows inhibitory activity against GSK-3β. 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,

BRD7389 is an inhibitor of RSK family kinase with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively.

AT7519 Hydrochloride (AT7519 HCl) is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9.

GSK 3 Inhibitor IX (6-BIO) is a selective reversible, ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex. It inhibits (GSK-3α/β)/CDK1/CDK5 activity with IC50 values of 5 nM/320 nM/83 nM, respectively.

Seliciclib (Roscovitine) is a potent inhibitor of Cdk2/cyclin E (IC50=0.1 µM). Seliciclib also inhibits Cdk7/cyclin H, Cdk5/p35 and Cdc2/cyclin B (IC50=0.49/0.16/0.65 µM). Seliciclib has antitumor activity.

Aminopurvalanol A is a competitive, selective and cell-permeable inhibitor of cyclin-dependent kinase (CDK) that potently inhibits Cyclin A/cdk2, Cyclin B/cdk1, Cyclin E/cdk2, and P35/cdk5 with IC50 of 33 nM, 33 nM, 28 nM and 20 nM, respectively.

KenPaullone (9-Bromopaullone), a potent CDK1, CDK2 and CDK5 inhibitor, as new enhancer for iTreg cell differentiation. Kenpaullone promotes iTreg cell differentiation through increased and prolonged transcription of foxp3 gene by enhancing TGFβ-Smad3 signaling pathway.

Milciclib (PHA-848125) (PHA-848125) is a potent, ATP-competitive CDK inhibitor for CDK2 with IC50 of 45 nM. It is >3-fold more selective for CDK2 than CDK1, 2, 4, 5, and 7. Phase 2.

AT7519 is a CDK1/2/4/6/9 inhibitor (IC50: 10-210 nM). It is less effective to CDK3 and little active to CDK7.

GP-82996 (CINK4) is a pharmacological inhibitor specifically targeting CDK4/6, exhibiting IC50 values of 1.5 μM for CDK4/cyclin D1, 5.6 μM for CDK6/cyclin D1, and 25 μM for Cdk5/p35. It effectively induces apoptosis in U2OS cancer cells, positioning it as a potential investigational tool in cancer research [1] [2].

R547 (Ro 4584820) is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM. It is less potent to CDK7 and GSK3α/β, while inactive to other kinases. Phase 1.

NVP-LCQ195 (LCQ-195) (AT9311) is a potent inhibitor of CDK1, CDK2, CDK3 and CDK5 (IC50: 1-42 nM).

Abemaciclib (LY2835219) is a dual inhibitor of CDK4/6 (IC50=2/10 nM) with selectivity and specificity. Abemaciclib has antitumor activity and is used to treat advanced or metastatic breast cancer.

Abemaciclib methanesulfonate (LY2835219) is a specific and effective inhibitor of CDK4(IC50=2 nM) and CDK6(IC50=10 nM).

Samuraciclib hydrochloride (ICEC0942 hydrochloride) is a potent, selective, ATP competitive and oral active CDK7 inhibitor with IC50 of 41 nM. The selectivity of Samuraciclib hydrochloride is 45-, 15-, 230- and 30-fold higher than CDK1, CDK2 (IC50 is 578 nM), CDK5 and CDK9 respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride has anti-tumor effects.

BS-181 is a highly selective CDK7 inhibitor (IC50: 21 nM); >40-fold selective for CDK7 than CDK1/2/4/5/6/9.

AZD2858 is a selective GSK-3 inhibitor, inhibiting tau phosphorylation at the S396 site and activating Wnt signaling pathway.

Purvalanol A (NG-60) is an effective and cell-permeable CDK inhibitor with IC50 of 70/4/35/850 nM for cdk2-cyclin A/B/E, and cdk4-cyclin D1, respectively.

BLINK15 is a blood-brain barrier-permeable Cdk5 inhibitor. It reduces CDK5 activity in CDK5/p35 (IC50= 29.34 nM) and CDK5/p25 (IC50= 12.08 nM) complexes. Additionally, BLINK15 exhibits antidiabetic and neuroprotective effects. It lowers blood glucose levels in type 2 diabetes (T2D) mice, enhances cognitive abilities, and diminishes neurodegenerative lesions.