CDK

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.

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

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.

Flavopiridol hydrochloride (MDL 107826A) is a synthetic N-methylpiperidinyl chlorophenyl flavone compound. As an inhibitor of cyclin-dependent kinase, alvocidib induces cell cycle arrest by preventing phosphorylation of cyclin-dependent kinases (CDKs) and by down-regulating cyclin D1 and D3 expression, resulting in G1 cell cycle arrest and apoptosis. This agent is also a competitive inhibitor of adenosine triphosphate activity.

AS2863619 is an oral inhibitor of cyclin-dependent kinase 8 (CDK8) and CDK19. Inhibition of CDK8 19 can enhance the activation of STAT5, thereby activating the Foxp3 gene. It can convert antigen-specific effector memory T cells into Foxp3+ regulatory T cells to study various immune diseases.

Simurosertib (TAK-931) is a selective and ATP-competitive cell division cycle 7 kinase inhibitor (IC50: <0.3 nM).

KB-0742 dihydrochloride is a potent, selective, and orally administered inhibitor of CDK9.

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

PF-562271 is an effective ATP-competitive, reversible inhibitor of FAK(IC50=1.5 nM) and Pyk2 kinase(IC50=13 nM).

SY-5609 (CDK7-IN-3) is a selective non-covalent CDK7 inhibitor (Kd value is 0.07 nM), with weak inhibitory activity against CDK2, CDK9 and CDK12 with IC50 values ​​of 5.5, 1.9 and 1.7 μM, respectively, and has anti-tumor activity and inhibits cell apoptosis.

SR-4835 is a highly selective dual inhibitor of CDK12 and CDK13(CDK12: IC50=99 nM, Kd=98 nM; CDK13: Kd=4.9 nM), which disables triple-negative breast cancer (TNBC) cells

Cdk1 2 Inhibitor III is a selective inhibitor of Cdk1 2 with an IC50 value of 2.1 μM against CDK1 cyclin B.

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.

Sodium Oxamate (Oxamic acid sodium salt) is an LDH inhibitor that specifically inhibits LDHA. Sodium Oxamate has antitumor activity and induces cell cycle arrest and apoptosis.

PHA-767491 (CAY10572) is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM, respectively.

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

PF07104091 inhibits CDK2, which may lead to cell cycle arrest, induce apoptosis and inhibit tumor cell proliferation.[1]

JSH-150 is a highly selective CDK9 inhibitor with an IC50 of 1 nM.

Indisulam (E 7070) is a carbonic anhydrase inhibitor and antitumor CDK inhibitor that targets the G1 phase of the cell cycle by depleting cyclin E, inducing p53 and p21, and inhibiting CDK2, thereby causing a blockade in the G1 S transition.

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.

HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor (IC50: 10.5 nM) that also inhibits PIM1 2 3, RIPK2, DYRK3, smMLCK, and CLK2. It can be used to study breast cancer.

PF-06873600, a selective and orally bioavailable cyclin-dependent kinase (CDK) inhibitor (CDK2, CDK4, and CDK6 with Ki values of 0.09 nM, 0.13 nM, and 0.16 nM, respectively), has potential antineoplastic activity.

(E Z)-Zotiraciclib ((E Z)-TG02) effectively inhibits CDK2, JAK2, and FLT3 with IC50s of 13 nM, 73 nM, and 56 nM, respectively.

XY028-140 is a selective CDK4/CDK6 degrade and inhibits both CDK4/6 expression and activity in cancer cells. XY028-140 is a PROTAC connected by ligands for Cereblon and CDK.

CDK4 6-IN-2 is a potent inhibitor of CDK4 and CDK6 [IC50s: 2.7 and 16 nM].

BX795 is an effective and selective PDK1 inhibitor (IC50: 6 nM), and its selectivity is 140- and 1600-fold for PDK1 over PKA and PKC in cell-free assays, respectively. Meanwhile, the selectivity for PDK1 is 100-fold than GSK3β.

CDK4/6/1 Inhibitor (Crozbaciclib) is a type of CDK4/6 inhibitor (IC50s: 3 and 1 nM). CDK4/6 inhibitor is a class of compounds used for the treatment of some types of hormone receptor positive, HER2-negative breast cancer, which can block the process of breast cancer cell division and reproduction.

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

P18IN011 (P18IN011 - CAS 77408-67-4 - Calbiochem) is a novel inhibitor of p18(INK4C).

BSJ-03-123 is a potent, CDK6-selective small-molecule degrader.

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.

OTS964 hydrochloride (OTS964) is a potent and selective TOPK inhibitor with potential anticancer activity.

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.

ML141 (CID-2950007) is an effective, specific and reversible non-competitive inhibitor of Rho family GTPase cdc42 (IC50: 200 nM).

CDK12-IN-2 (CDK12 inhibitor 2) is an effective and selective inhibitor of CDK12 with an IC50 of 52 nM, >100 μM, >10 μM and 16 μM for CDK12, CDK2, CDK7, and CDK9. CDK12-IN-2 can be used in studies about the function of CDK12.

CDK4/6-IN-6 is a potent CDK4/CDK6 inhibitor with Ki of 0.6 nM and 13.9 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively.

(S)-Enitociclib (VIP152) is a selective CDK9 inhibitor that induces complete regression of MYC+ lymphomas by inhibiting RNA polymerase II-mediated transcription of anti-apoptotic and pro-survival proteins.

Abemaciclib metabolite M20 (CDK4/6-IN-4) is an active metabolite of Abemaciclib. Abemaciclib metabolite M20 is a selective CDK4/6 inhibitor and can be used for researches on the treatment of cancer.

CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor [IC50: 2.3 nM].

PF 477736 (PF-736,PF-00477736) is a specifc, effective and ATP-competitive Chk1 inhibitor (Ki: 0.49 nM ) and also inhibits FGFR3, Aurora-A, VEGFR2, Flt3, Fms (CSF1R), Ret and Yes.

T025 is a pan CLK inhibitor with Kds of 4.8, 0.096, 6.5, 0.61, and 0.074 nM for CLK1-4, respectively. T025 displays anti-proliferative activities with IC50s of 30-300 nM in hematological and solid cancer cell lines. T025 can be used in studies about MYC-driven diseases.

BLU-222 is an orally available but selective cell cycle protein-dependent kinase (CDK2) inhibitor with antitumor activity for the study of ovarian and uterine cancer.

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.

MBM-55 is an effective inhibitor of NIMA related kinase 2 (NEK2) with an IC50 of 1 nM. MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis.

AZD-5597 ((S)-(4-((5-Fluoro-4-(1-isopropyl-2-methyl-1H-imidazol-5-yl)pyrimidin-2-yl)amino)phenyl)(3-(methylamino)pyrrolidin-1-yl)methanone) is a potent imidazole pyrimidine amide CDK inhibitor.

SU9516 is a potent CDK2 inhibitor with an IC50 of 22 nM and also inhibits CDK1 and CDK4, with IC50s of 40 nM and 200 nM, respectively.

YKL-5-124, a potent, selective and covalent CDK7 inhibitor with an IC50 of 9.7 nM, 1300 nM and 3020 nM for CDK7/Mat1/CycH, CDK2 and CDK9 respectively, displays biochemical and cellular selectivity for CDK7 over CDK12/13.