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CDK

CDK

CDKs (Cyclin-dependent kinases) are serine-threonine kinases first discovered for their role in regulating the cell cycle.Additionally, they control mRNA processing, transcription, and nerve cell differentiation. With molecular weights between 34 and 40 kDa, CDKs are relatively small proteins that only contain the kinase domain. In fact, when their CDK gene has been replaced with the homologous human gene, yeast cells can proliferate normally. A CDK by definition binds the control protein cyclin. Only the cyclin-CDK complex is an active kinase; CDK lacks much kinase activity on its own.

Around 20 Cyclin-dependent kinases (CDK1-20) have been identified as of yet. While CDK 7, 8, 9 and 11 are linked to transcription, CDK1, 4, and 5 are involved in the cell cycle.

The majority of CDK regulation occurs post-translationally, and CDK levels are essentially constant throughout the cell cycle. The majority of knowledge about CDK structure and function is based on CDKs from vertebrates (CDC2 and CDK2), S. pombe (CDC28), and S. cerevisiae (Cdc2). Cyclin binding, CAK phosphorylation, regulatory inhibitory phosphorylation, and CDK inhibitory subunit (CKI) binding are the four main mechanisms of CDK regulation.

CDK related products

Structure Cat No. Product Name CAS No. Product Description
(+)-BAY-1251152 V4163 (+)-BAY-1251152 1610358-56-9 BAY-1251152 is a potent and highly selective PTEF/CDK9 inhibitor.
(2S,3R)-Voruciclib hydrochloride V77392 (2S,3R)-Voruciclib hydrochloride rel-(2S,3R)-Voruciclib HCl is an enantiomer of Voruciclib HCl.
(E/Z)-BIO-acetoxime (GSK-3 Inhibitor X) V52146 (E/Z)-BIO-acetoxime (GSK-3 Inhibitor X) 740841-15-0 (E/Z)-BIO-acetoxime (GSK-3 Inhibitor X) is a potent and specific GSK-3α/β inhibitor (antagonist) with IC50 of 10 nM.
(E/Z)-TG003 V55086 (E/Z)-TG003 300801-52-9 (E/Z)-TG003 is the racemate of (Z)-TG003 and (E)-TG003.
(E/Z)-THZ1 dihydrochloride V84546 (E/Z)-THZ1 dihydrochloride 2095433-94-4
(E/Z)-Zotiraciclib ((E/Z)-TG02; (E/Z)-SB1317) V52837 (E/Z)-Zotiraciclib ((E/Z)-TG02; (E/Z)-SB1317) 937270-47-8 (E/Z)-Zotiraciclib ((E/Z)-TG02) is a potent inhibitor of CDK2, JAK2 and FLT3 with IC50s of 13, 73 and 56 nM respectively.
(E/Z)-Zotiraciclib HCl-TG02 HCl V50450 (E/Z)-Zotiraciclib HCl-TG02 HCl 1321626-25-8 (E/Z)-Zotiraciclib HCl (TG02 HCl) is a novel and potent CDK2, JAK2, and FLT3 inhibitor with the potential for the treatment of cancer.
(R)-CR8 triHCl V40461 (R)-CR8 triHCl 1786438-30-9 (S)-CR8 trihydrochloride, ananalog of Roscovitine, is a novel, potent 2nd-generation cyclin-dependent kinase (CDK) inhibitor, also acting as a molecular glue degrader that depletes cyclin K.
(R)-DRF053 dihydrochloride V69796 (R)-DRF053 dihydrochloride 1241675-76-2 (R)-DRF053 di-HCl is a potent inhibitor of casein kinase 1 (CK1), CDK1/cyclin B, and CDK5/p25 with IC50s of 14 nM, 220 nM, and 80 nM, respectively.
(R)-PROTAC CDK9 ligand-1 V75982 (R)-PROTAC CDK9 ligand-1 2411021-95-7 (R)-PROTAC CDK9 ligand-1 (compound 19.4) is a CDK9-targeted degrader that may be utilized to prepare PROTACs with anti-tumor activity.
(rel)-MC180295 V3635 (rel)-MC180295 2237942-08-2 (rel)-MC180295 is a novel, potent and selective CDK9-Cyclin T1 inhibitor with an IC50 of 5 nM and with broad anti-cancer activity in vitro.
(S)-GFB-12811 V55070 (S)-GFB-12811 2757672-69-6 (S)-GFB-12811 (compound 596) is a potent and specific CDK5 inhibitor (antagonist) with IC50 of less than 10 nM.
(±)-BAY-1251152 V4202 (±)-BAY-1251152 1610358-53-6 BAY-1251152 is a racemic mixture of BAY-1251152 which is a novel, potent and highly selectivePTEF/CDK9 inhibitor.
1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC (PC(18:0/22:4)) V84078 1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC (PC(18:0/22:4)) 137254-39-8
3-Methylthienyl-carbonyl-JNJ-7706621 V52503 3-Methylthienyl-carbonyl-JNJ-7706621 443798-09-2 3-Methylthienyl-carbonyl-JNJ-7706621 is a potent and specific cyclin-dependent kinase (CDK) inhibitor (antagonist) with IC50s of 6.4 nM and 2 nM for CDK1/cyclin B and CDK2/cyclin A, respectively.
6-Dimethylaminopurine V5243 6-Dimethylaminopurine 938-55-6 6-Dimethylaminopurine is a novel and potent serine threonine protein kinase inhibitor which inhibits the germinal vesicle breakdown and the meiotic maturation of oocytes.
7BIO (7-Bromoindirubin-3-Oxime) V52479 7BIO (7-Bromoidirubin-3-Oxime) 916440-85-2 7BIO (7-Bromoidirubin-3-Oxime) is an analogue of indirubin.
[pSer2, pSer5, pSer7]-CTD TFA V77486 [pSer2, pSer5, pSer7]-CTD TFA [pSer2, pSer5, pSer7]-CTD (TFA) is a substrate of CDK7 and is a polypeptide phosphorylated at the ser2, ser5, and ser7 sites of the carboxyl-terminal domain (CTD) of RNA polymerase II.
[pThr3]-CDK5 Substrate TFA V77487 [pThr3]-CDK5 Substrate TFA [pThr3]-CDK5 Substrate TFA is a CDK5 substrate for Thr3 phosphorylation.
Abemaciclib (LY2835219) mesylate V1547 Abemaciclib (LY2835219) mesylate 1231930-82-7 Abemaciclib mesylate (formerly known as LY-2835219; LY2835219; trade name:Verzenio) is a potent and selective, orally bioavailable dual inhibitor of CDK4 (cyclin-dependent kinase) and CDK6 with potential antineoplastic activity.
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