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Cyclin-dependent Kinase (CDK)

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Cat. No. Product Name Field of Application Chemical Structure
DC46439 CDK12-IN-4 CDK12-IN-4, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 0.641 μM at high ATP (2 mM). CDK12-IN-4 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1).
DC46440 CDK12-IN-5 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).
DC46441 CDK12-IN-6 CDK12-IN-6, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 1.19 μM at high ATP (2 mM). CDK12-IN-6 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1).
DC46459 3-Methylthienyl-carbonyl-JNJ-7706621 3-Methylthienyl-carbonyl-JNJ-7706621 is a potent and selective inhibitor of cyclin-dependent kinase (CDK), with IC50s of 6.4 nM and 2 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. 3-Methylthienyl-carbonyl-JNJ-7706621 also shows potent inhibition of GSK-3 (IC50=0.041 μM) and modest potency against CDK4, VEGF-R2, and FGF-R2 (IC50=0.11, 0.13, 0.22 μM, respectively). 3-Methylthienyl-carbonyl-JNJ-7706621 can be used for the research of cancer.
DC46470 CPS2 CPS2 is a first-in-class, highly potent, selective and irreversible PROTAC CDK2 degrader (IC50= 24 nM). CPS2 can be used for the research of acute myeloid leukemia.
DC46497 CDK8-IN-1 CDK8-IN-1 is a potent and selective CDK8 inhibitor with an IC50 of 3 nM.
DC46607 [pSer2, pSer5, pSer7]-CTD TFA [pSer2, pSer5, pSer7]-CTD (TFA), a substrate for CDK7 (cyclin dependent protein kinase), is a phosphorylated polypeptide at ser2, ser5 and ser7 sites of RNA polymerase II carboxy-terminal domain (CTD).
DC46943 Dalpiciclib Featured 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.
DC46944 Ipivivint Ipivivint (SM08502), a first-in-class, orally active and potent CDC-like kinase (CLK) inhibitor, inhibits CLK1 (IC50=1.4 μM), CLK2 (IC50=0.002 μM) and CLK3 (IC50=0.022 μM). Ipivivint reduces Wnt pathway signaling gene expression through inhibiting CLK activity and serine and arginine rich splicing factor (SRSF) phosphorylation and disrupting spliceosome activity. Ipivivint can be used for the research of cancer.
DC46945 Avotaciclib Avotaciclib (BEY1107) is an orally active cyclin dependent kinase 1 (CDK1) inhibitor. Avotaciclib can be used for the research of cancer.
DC46946 PF-07220060 Featured PF-07220060 is a potent CDK4/CDK6 inhibitor with a Ki of 0.6 nM and 13.9 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively.
DC47043 Ocarocoxib Ocarocoxib, a potent COX-​2 (cyclooxygenase-​2) inhibitor, is a non-steroidal anti-inflammatory for veterinary use.
DC47048 Rebamipide mofetil Featured Rebamipide mofetil is an orally active prodrug of Rebamipide (OPC12759). Rebamipide is a mucoprotective agent. Rebamipide induces COX-2 expression, increases PGE2 levels, and enhances gastric mucosal defense in a COX-2-dependent manner.
DC47109 Cimpuciclib Cimpuciclib is a cyclin-dependent kinase(CDK) inhibitor and antineoplastic.
DC47130 CDK5-IN-1 CDK5-IN-1, a potent CDK5 inhibitor, is against CDK5 activity less than 10 nM. CDK5-IN-1 is used for kidney diseases research.
DC47205 Eltenac Eltenac, a non-steroidal anti-inflammatory drug (NSAID), is a COX inhibitor. Eltenac shows IC50 of 0.03 μM for both COX-1 and COX-2 in isolated human whole blood.
DC47236 Cirtuvivint Cirtuvivint (SM08502) is a potent and orally active CDC-like kinase (CLK) inhibitor. Cirtuvivint can be used for solid tumors research.
DC47269 Samuraciclib Featured Samuraciclib (CT7001) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib has anti-tumor effects.
DC47704 CDK9-IN-12 CDK9-IN-12 displays the optimal CDK9 inhibitory activity with an IC50 value of 5.41 nM.
DC47705 JH-XVI-178 JH-XVI-178 is a highly potent and selective inhibitor of CDK8/19 that displays low clearance and moderate oral pharmacokinetic properties.
DC47706 CDK2-IN-7 CDK2-IN-7 is a CDK2 inhibitor for treating cancer (IC50 < 50 nM).
DC47707 CDK/HDAC-IN-1 CDK/HDAC-IN-1 shows remarkable CDK2/4/6 and HDAC6 inhibitory activity of IC50 = 60.9 ± 2.9, 276 ± 22.3, 27.2 ± 4.2, and 128.6 ± 0.4 nM, respectively.
DC47914 Ribociclib-d6 hydrochloride Ribociclib D6 (LEE011 D6) hydrochloride is a deuterium labeled Ribociclib. Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
DC47966 KH-CB20 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).
DC48001 DS96432529 DS96432529 is a potent and orally active bone anabolic agent through CDK8 inhibition.
DC48027 CDK7-IN-7 CDK7-IN-7 is a potent and selective CDK7 kinase inhibitor with an IC50 of <50 nM (Patent CN112661745A, compound T-01).
DC48028 CDK7-IN-6 CDK7-IN-6 is a potent and selective cyclin-dependent kinase (CDK7) inhibitor (IC50≤100 nM), extracted from patent WO2019197549 A1, compound 210. CDK7-IN-6 is > 200-fold selective for CDK7 over CDK1, CDK2, and CDK5. CDK7-IN-6 can be used for the research of cancer.
DC48029 CDK7/9-IN-1 CDK7/9-IN-1 is a cyclin-dependent kinases 7/9 (CDK7/9) inhibitor. CDK7/9-IN-1 selectively inhibits CDK7 over CDK9. CDK7/9-IN-1 inhibits CDK7 with IC50s of 0.0656 μM and 0.00574 μM without pre-incubation and after 3 hours pre-incubation, respectively. CDK7/9-IN-1 inhibits CDK9 with an IC50 of 2.14 μM after 3 hours pre-incubation. CDK7/9-IN-1 can be used for the research of cancer.
DC48034 BSJ-01-175 BSJ-01-175 is a potent and selective CDK12/13 covalent inhibitor. BSJ-01-175 demonstrates exquisite selectivity, potent inhibition of RNA polymerase II phosphorylation, and downregulation of CDK12-targeted genes in cancer cells.
DC48048 Avotaciclib trihydrochloride Avotaciclib (BEY1107) trihydrochloride is a potent and orally active inhibitor of cyclin dependent kinase 1 (CDK1). Avotaciclib trihydrochloride can be used for the research of locally advanced or metastatic pancreatic cancer.
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