TG693 is an orally active inhibitor of CLK1. TG693 regulates the mutated exon 31 of the dystrophin gene in vivo. TG693 is used in Duchenne muscular dystrophy (DMD) research[1].
HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a Kd value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer[1].
PF 477736 is a potent, selective ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, 100-fold selectivity versus Chk2 (Ki, 47 nM).
BAY-1143572 Racemate is the racemate mixture of BAY-1143572. BAY-1143572 is a potent and highly selective, oral P-TEFb/CDK9 inhibitor which supresses CDK9/CycT1 with an IC50 of 13 nM.
THZ531 is a covalent inhibitor of both CDK12 and CDK13 with IC50s of 158 nM and 69 nM, respectively.
Eciruciclib is an antineoplastic and potent cyclin dependent kinase (CDK) inhibitor[1].
5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase, with IC50s of 9, 20 and 25 nM, respectively[1].
CDK9-IN-18 is a potent CDK9 inhibitor. CDK9-IN-18 blocks the phosphorylation function of kinase CDK9. CDK9-IN-18 exhibits both good anticancer activity and low cellular activity. CDK9-IN-18 induces apoptosis.
CDK8-IN-6 (compound 9) is a potent cyclin-dependent kinase 8 (CDK8) inhibitor with an Kd of 13 nM. CDK8-IN-6 shows cytotoxicity for MOLM-13, OCI-AML3, MV4-11, NRK and H9c2 cells with IC50s of 11.2, 7.5, 8.6, 20.5, 12.5-25 µM, respectively. CDK8-IN-6 has the potential for the research of AML-cancer[1].
Alsterpaullone (9-Nitropaullone;NSC 705701) is a potent cyclin-dependent kinases (CDK) inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to glycogen synthase kinase-3 alpha/beta (GSK-3alpha/GSK-3beta) with an IC50 of 4 nM, with antitumor activity and potential for the treatment of neurodegenerative and proliferative disorders[1].
HDAC1/CDK7-IN-1 (compound 8e) is a dual CDK7 and HDAC1 inhibitor with IC50s of 893 nM and 248 nM, respectively. HDAC1/CDK7-IN-1 inhibits the growth cells of MDA-MB-231, MCF-7, A549, and HCT-116 cancer cells. HDAC1/CDK7-IN-1 induces cell cycle arrest and apoptosis in HCT-116 cells, as well as hindered the migration of HCT-116 cells[1].
LY3143921 ((S)-Example 2) is an orally active CDC7 kinase inhibitor. LY3143921 shows broad in vitro anticancer activity[1].
CDK12-IN-5, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 23.9 nM at high ATP (2 mM). CDK12-IN-5 has no effect on CDK2/Cyclin E (IC50=173 μM) and CDK9/Cyclin T1 (IC50=127 μM) at high ATP (2 mM) (WO2021116178A1)[1].
Carbonic anhydrase inhibitor 14 (Compound 8b) is a carbonic anhydrase (CA) inhibitor with Ki values of 1203, 99.7, 9.4 and 27.7 nM against hCA I, hCA II, hCA IX and hCA XII, respectively. Carbonic anhydrase inhibitor 14 can also inhibit CDK2 with an IC50 of 20.3 μM. Carbonic anhydrase inhibitor 14 shows antitumor activity[1].
KH-CB20, an E/Z mixture, is a potent and selective inhibitor of CLK1, with an IC50 of 16.5 nM. KH-CB20 also can inhibits DYRK1A (IC50=57.8 nM) and CLK3 (IC50=488 nM)[1].
Palbociclib hydrochloride is a highly selective CDK4/6 inhibitor with IC50s of 11 nM and 16 nM, respectively.
Cirtuvivint (SM08502) is a potent and orally active CDC-like kinase (CLK) inhibitor. Cirtuvivint can be used for solid tumors research[1].
LY3143921 (LY-3143921) is an orally available, potent, selective inhibitor of Cdc7 kinase inhibitor, inhibits CDC7/DBF4 I and pMCM2 (S53) with IC50 values of 3.3 nM and 290 nM, respectively. Solid Tumors Phase 1 Clinical
CDK9-IN-12 displays the optimal CDK9 inhibitory activity with an IC50 value of 5.41 nM.
Ryuvidine is a potent inhibitor of SET domain-containing protein 8(SETD8) with an IC50 of 0.5 µM and suppresses monomethylation of H4K20 in vitro[1]. Ryuvidine also inhibits CDK4 with an IC50 of 6.0 μM and is cytotoxic against a range of human cancer cells[2].
Palbociclib isethionate is a highly selective inhibitor of?CDK4/6?with?IC50s?of 11 nM/16 nM, respectively.?
Ro-3306 is a potent and selective inhibitor of CDK1, with Kis of 20 nM, 35 nM and 340 nM for CDK1, CDK1/cyclin B1 and CDK2/cyclin E, respectively.
Ribociclib (LEE011) is a highly specific CDK4/6 inhibitor with IC50s of 10 nM and 39 nM, respectively.
AZD-5438 is a potent inhibitor of CDK1/2/9 with IC50 of 16 nM/6 nM/20 nM in cell-free assays. It also inhibits GSK3β, but is less potent to CDK5/6.
Dalpiciclib (SHR-6390) is a highly selective, orally bioavailable CDK4/6 inhibitor with comparable potencies against CDK4 (IC50=12.4 nM) and CDK6 (IC50=9.9 nM). Dalpiciclib exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated tumor-suppressor retinoblastoma protein (Rb) and inducing G1 cell cycle arrest[1][2].
CP681301 is a potent CDK5 inhibitor. CP681301 shows antiproliferative activity. CP681301 decreases the expression of CD133, OLIG2, SOX2, KI67, pCDK5 protein level in GSCs (Glioma stem cells). CP681301 reduces self-renewal in mouse glioma xenografts. CP681301 shows anti-tumor activity in Drosophila[1].
Cdc7-IN-15 (Example 108) is a cdc7 kinase inhibitor. Cdc7-IN-15 can be used for cancer research[1].
PHA-690509 is an anti-ZikV compound that inhibits ZikV replication. PHA-690509 is also a CDK inhibitor, and inhibits caspase-3 activity[1][2].
EGFR/HER2/CDK9-IN-3 (Compound 10) is a potent inhibitor of EGFR/HER2/CDK9 with IC50s of 191.08, 132.65, and 113.98 nM, respectively. EGFR/HER2/CDK9-IN-3 exhibits remarkable antitumor activity[1].
Cdc7-IN-19 (compound 1-1) is a potent CDC7 inhibitor with an IC50 of 1.49 nM[1].