cdk1

CDK1-IN-7 is a potent inhibitor of CDK1 with an IC50 value of 161.2 nM for CDK1/CycB. CDK1-IN-7 induces apoptosis in a p53-dependent manner via the apoptosis-intrinsic pathway. CDK1-IN-7 selectively acts on tumour tissue and has potential anti-proliferative effects. CDK1-IN-7 is a potential CDK1-IN-7 is a potential targeted anti-tumour agent.

CDK1 2 4-IN-1 (compound 3a) is a potent CDK inhibitor with IC50 values of 1.47, 0.78, and 0.87 μM for CDK1, CDK2, and CDK4, respectively. It can be used in cancer research to arrest the cell cycle at the G2 M phase and induce apoptosis, elevating Bax, caspase-3, and P53 levels while decreasing Bcl-2 levels [1].

CDK1 Cyc B-IN-1 (Compound 5) is a potent inhibitor of the CDK1 Cyc B complex with an IC50 value of 97 nM. This compound induces apoptosis and G2 M cell cycle arrest, halting cancer cell proliferation, and exhibits a wide-ranging cytotoxic effect on various cancer cell lines [1].

KDM1 CDK1-IN-1 (compound 4) is a potent inhibitor of KDM1 (IC50: 0.096 μM) and CDK1 (IC50: 0.078 μM), blocking the cell cycle of HOP-92 cells in the G2 M phase and inducing apoptosis. It is highly cytotoxic to CCRF-CEM cells (IC50: 16.34 μM), HOP-92 cells (IC50: 3.45 μM), and Hep-G2 cells (IC50: 7.79 μM).

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

CDK1-IN-5 (10h) is a selective CDK1 inhibitor with an IC50 of 42.19 nM for CDK1, 188.71 nM for CDK2, and 354.15 nM for CDK5. It influences the cell cycle, inhibits cancer cell growth, and is applicable in cancer research.

CDK1-IN-4 (10d) is a selective CDK1 inhibitor that acts on CDK1 (IC50: 44.52 nM), CDK2 (IC50: 624.93 nM), and CDK5 (IC50: 135.22 nM). It affects the cell cycle, inhibiting the growth of cancer cells, and can be used in cancer research.

CDK1-IN-2 (cdk1 inhibitor 2) is a CDK1 inhibitor with IC50 of 5.8 μM. A broad-spectrum kinase profiling of CDK1-IN-2 revealed nonselective inhibition of several kinases.

CDK1-IN-3 (8g) is a selective CDK1 inhibitor with IC50 values of 36.8 nM for CDK1, 305.17 nM for CDK2, and 369.37 nM for CDK5. CDK1-IN-3 can affect the cell cycle, inhibit cancer cell growth, and is suitable for use in cancer research.

CDK12-IN-3 is a selective and potent CDK12 inhibitor with anti-tumor activity, which can be used to study malignant tumors.

CDK/HDAC-IN-1 exhibits potent inhibitory activity towards CDK2/4/6 and HDAC6, with IC50 values of 60.9 ± 2.9 nM, 276 ± 22.3 nM, 27.2 ± 4.2 nM, and 128.6 ± 0.4 nM, respectively.

NSC-37445 has anti-tumor activity, such as inhibits growth of bladder tumor cells in a nude mice model , prevents the recurrence and progression of non-muscle-invasive urothelial cell carcinoma. NSC-37445 can significantly reduce the expression of CDK1-inhibitory kinases, Myt1 and Wee1, and cause cyclin B1 protein accumulation leading to CDK1 activation in T24 cells. 3. Flavokawain A (Flavokavain A) may exert anti-inflammatory responses by suppressing LPS-induced expression of pro-inflammatory mediators via blockage of NF-κB-AP-1-JNK/p38 MAPK signaling pathways in the murine macrophages.

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.

H1k is an eudistomin Y fluorescent derivative and lysosome-targeted antiproliferative agent that dose-dependently increases autophagy signalling and down-regulates the expression of cyclin-dependent kinase (CDK1) and cyclin B1.

GW297361 is a potent inhibitor of the cell cycle protein-dependent kinase Cdk1 and also inhibits the Pho85 signaling pathway.The IC50s of GW297361 on yeast Cdk1 and Pho85 were 20 nM and 400 nM, respectively.

hSMG-1 inhibitor 11j is a pyrimidine derivative. hSMG-1 inhibitor 11j is a potent and selective inhibitor of hSMG-1, IC50 = 0.11 nM. hSMG-1 inhibitor 11j exhibits >455-fold selectivity for hSMG-1 over mTOR (IC50=50 nM), PI3Kα γ (IC50=92 60 nM) and CDK1 CDK2 (IC50=32 7.1 μM). hSMG-1 inhibitor 11j can be used for the research of cancer.

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

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).

hSMG-1 inhibitor 11e is an effective and selective inhibitor of hSMG-1 (IC50 <0.05 nM) and can be used in studies about cancer treatment.

CDK4 inhibitor is a novel and specific CDK4/Cyclin D1 inhibitor with an IC50 of 10 nM; 1500 and 500 fold than CDK1/Cyclin B (IC50>15 uM) and CDK2/Cyclin A (IC50=5.265 uM) respectively.

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.

NU6102 is a selective and potent ATP-competitive CDK2 inhibitor with antitumor activity against CDK1 cyclinB, CDK2 cyclinA3, CDK1 CDK2, CDK4, DYRK1A , PDK1, and ROCKII, and it can be used to study rectal cancer.

Avotaciclib (BEY1107) is a potent, orally active cyclin-dependent kinase 1 (CDK1) inhibitor, suitable for research in locally advanced or metastatic pancreatic cancer.

CDK12-IN-6, a pyrazolotriazine compound, is a powerful inhibitor of CDK12. Its inhibitory activity is significant with an IC50 value of 1.19 μM when tested at high ATP concentration (2 mM). Notably, CDK12-IN-6 does not exhibit any inhibitory effect on CDK2 Cyclin E (IC50 >20 μM) and CDK9 Cyclin T1 (IC50 >20 μM) when tested under the same high ATP conditions (2 mM) (WO2021116178A1).

CDK12-IN-5 is a potent CDK12 inhibitor with potential anticancer and antitumor activity, and can be used orally in the study of breast and ovarian cancer.

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.

CDK12-IN-E9 is a potent and selective covalent inhibitor of CDK12 and a non-covalent inhibitor of CDK9, while avoiding ABC transporter-mediated efflux. It exhibits weak binding to the CDK7 CyclinH complex (IC50> 1 μM).

PROTAC CDK12 13 Degrader-1 (7f) is a potent and selective dual degrader of the cell cycle protein-dependent kinases CDK12 (DC50: 2.2 nM) and CDK13 (DC50: 2.1 nM), used in the context of breast cancer.

CDK12-IN-4, a pyrazolotriazine compound, exhibits potent inhibition of CDK12 by achieving an IC50 value of 0.641 μM, utilizing high ATP levels (2 mM). Notably, CDK12-IN-4 does not impact CDK2 Cyclin E (IC50 > 20 μM) or CDK9 Cyclin T1 (IC50 > 20 μM) under the influence of high ATP (2 mM) levels (WO2021116178A1).

GW 5074 (Raf1 Kinase Inhibitor I)(IC50=9 nM) is an effective and specific c-Raf inhibitor. It has no effect on the activities of JNK1 2 3, MEK1, MKK6 7, CDK1 2, c-Src, p38 MAP, VEGFR2 or c-Fms.

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.

NVP-2 is an effective and selective ATP-competitive cyclin-dependent kinase 9 (CDK9) probe. NVP-2 induces cell apoptosis. NVP-2 inhibits CDK9 CycT activity (IC50: 0.514 nM). NVP-2 shows inhibitory effcts on CDK1 CycB, CDK2 CycA and CDK16 CycY kinases (IC5

PHA-793887 has been used in trials studying the treatment of Advanced/Metastatic Solid Tumors.

SNS-032 (BMS-387032) is a selective inhibitor of CDK2 (IC50: 48 nM), exhibiting 10- and 20-fold selectivity over CDK1 and CDK4, respectively. It is also sensitive to CDK7 (IC50: 62 nM) and CDK9 (IC50: 4 nM), with no effect on CDK6.

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.

BMS-265246 is a potent and selective CDK1 2 inhibitor. Its chemical name is (4-[R-(2,3-Dihydro-benzo[1,4]dioxin-6-yl)-1H-indol-1-yl]-1H-pyrazolo[3,4-d] pyrimidine-6-amine), and it functions by targeting CDK1 and CDK2 to potentially disrupt cell cycle progression.

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.

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

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

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.

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.

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.

Desmethylglycitein (6,7,4'-Trihydroxyisoflavone) , is a novel inhibitor of PKCα in suppressing solar UV-induced matrix metalloproteinase 1, which has antioxidant, and anti-cancer activities.

NU6027 is a potent ATR/CDK inhibitor, inhibits CDK1/2, ATR and DNA-PK with Ki of 2.5 μM/1.3 μM, 0.4 μM and 2.2 μM, enter cells more readily than the 6-aminopurine-based inhibitors.

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

NU6140 is a selective inhibitor of CDK2-cyclin A (IC50, 0.41 μM). It shows 10- to 36-fold selectivity over other CDKs. NU6140 also effectively inhibits Aurora A and Aurora B (IC50s: 67 and 35 nM, respectively). It also enhances the apoptotic effect and has anti-cancer activity.

Alsterpaullone is a Cyclin-Dependent Kinase Inhibitor, Mediated Toxicity in HeLa Cells Through Apoptosis-Inducing Effec

Voruciclib is an orally active and selective CDK inhibitor (Ki: 0.626 nM-9.1 nM) that represses the expression of MCL-1 in multiple models of diffuse large B-cell lymphoma and effectively blocks CDK9, the transcriptional regulator of MCL-1.