cyclin dependent kinase

Nimbolide suppresses CDK4 CDK6 kinase activity. Nimbolide inhibits the NF-κB, Wnt, PI3K-Akt, MAPK, and JAK-STAT signaling pathways. Nimbolide causes apoptosis through the inactivation of NF-κB. Nimbolide is a triterpene derived from the leaves and flowers

Dinaciclib (SCH 727965) is a selective CDK inhibitor targeting CDK1, CDK2, CDK5, and CDK9 (IC50 = 3/1/1/4 nM). It exhibits potential antitumor activity by inhibiting the incorporation of thoracic glycan (dThd) DNA.

RO-3306 is a selectivity ATP-competitive CDK1 inhibitor (Ki: 20 nM). The selectivity of RO-3306 for CDK1 is >15-fold higher than a diverse panel of human kinases.

Flavopiridol (Alvocidib) (Alvocidib) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM. It is 7.5-fold more selective for CDK1, 2, 4, 6 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Phase 1/2.

5-Iodo-indirubin-3'-monoxime is a potent inhibitor of GSK-3β, CDK5 P25, and CDK1 cyclin B, competing with ATP for binding to the catalytic site of the kinase (IC50s: 9, 20, and 25 nM).

CDK9-IN-2 is a specific CDK9 inhibitor with an IC50 of 5 nM in the A2058 skin cell line (72 hours) and 7 nM in the H929 multiple myeloma cell line (72 hours).

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.

3MB-PP1 is a bulky purine analog and a Polo-like kinase 1 (Plk1) inhibitor. In cells expressing analog-sensitive Plk1 alleles, 3MB-PP1 blocks mitotic progression and cell division arise by targeting Plk1. 3MB-PP1 specifically inhibits analog-sensitive Ssn3 (Cdk8). 3MB-PP1 inhibits Leu93 Mutant Zipper-interacting protein kinase with IC50 of 2 μM. 3MB-PP1 can be used for the research of cell division and hypha formation of Candida albicans.

XL-413 is an orally bioavailable cell division cycle 7 homolog (CDC7) kinase inhibitor with potential antineoplastic activity. XL-413 binds to and inhibits the activity of CDC7, which may result in the inhibition of DNA replication and mitosis, the induct

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).

Amantadine hydrochloride (CI-719) is an antiviral that is used in the prophylactic or symptomatic treatment of influenza A and Parkinson disease.

Ribociclib succinate (LEE011 succinate) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and exhibits over 1,000-fold reduced potency against the cyclin B/CDK1 complex.

Palbociclib (PD 0332991) is a CDK inhibitor that inhibits CDK4 and CDK6 (IC50=11/16 nM) and is orally active. Palbociclib has anti-tumorigenic activity and has investigational potential for use in ER-positive and HER2-negative breast cancer.

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).

Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor (IC50:10/39 nM).

Palbociclib monohydrochloride (PD 0332991 hydrochloride) is a selective inhibitor of CDK4/6 (IC50s: 11/16 nM). It exhibits no inhibition against a panel of 36 additional protein kinases.

Amantadine (1-Aminoadamantane) is an antiviral, is a weak antagonist of the NMDA-type glutamate receptor, increases dopamine release, and blocks dopamine reuptake.

6-(Dimethylamino)purine (N,N-Dimethyladenine) is a serine threonine protein kinase and CDK inhibitor

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.

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.

THZ531 is a covalent inhibitor of both CDK12(IC50=158 nM) and CDK13(IC50=69 nM).