(-)-BAY-1251152 is an enanthiomer of BAY-1251152 with rotation (-). BAY-1251152 is a potent and highly selective PTEF/CDK9 inhibitor.

A clinical analog of THZ1 and a selective, covalent CDK12 inhibitor that is not susceptible to ABC transporter-mediated drug efflux.

A clinical analog of THZ1 and a selective, covalent CDK12 inhibitor that is not susceptible to ABC transporter-mediated drug efflux.

A non-planar analogue of fascaplysin that selectively inhibits CDK4/cyclin D1 with IC50 of 5.5 uM.

A novel, potent and selective inhibitor of CDK4/6 with biochemical IC50 of 1 nM and 2 nM for CDK4/cyclin D1 and CDK6/cyclin D3, respectively.

A novel, potent and selective inhibitor of CDK4/6 with biochemical IC50 of 1 nM and 2 nM for CDK4/cyclin D1 and CDK6/cyclin D3, respectively.

A potent, ATP-competetive CDKs inhibitor with IC50 of 7, 7, 7, 3 uM for Cdc2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk/p35 kinase.

AG-24322 is a second generation CDK inhibitor. AG-024322 is a potent inhibitor of CDK1, CDK2, and CDK4 that produces cell-cycle arrest and antitumor activity in preclinical models. The no-adverse-effect dose of AG-024322 was 2 mg/kg and associated with ov

Alsterpaullone is a potent ATP-competitive and cell cycle cyclin-dependent kinase inhibitor, that is reported to be the most active Paullone.

AMG 925 is a potent and selective dual inhibtor of CDK4/FLT3 with IC50s of 1.5 nM and 2.4 nM for CDK4 and FLT3, respectively; with IC50 of 19 nM in MOLM-13 cell.

amsilarotene (TAC-101) is a retinobenzoic acid with potential antineoplastic activity. TAC-101 inhibits retinoblastoma-gene product (RB) phosphorylation and increases the presence of 2 cyclin-dependent kinase (CDK) inhibitors, resulting in cell cycle arrest. This agent also causes a cytotoxic decline in cyclin A and thymidylate synthase expression. Check For active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).For the detailed information of TAC-101, the solubility of TAC-101 in water, the solubility of TAC-101 in DMSO, the solubility of TAC-101 in PBS buffer, the animal experiment (test) of TAC-101, the cell expriment (test) of TAC-101, the in vivo, in vitro and clinical trial test of TAC-101, the EC50, IC50,and Affinity of TAC-101, Please contact DC Chemicals..

AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM; less potent to CDK3 and little active to CDK7.

AT7519 is a novel multi-CDK inhibitor for CDK1/cyclin B, CDK2/Cyclin A, CDK3/Cyclin E, CDK4/Cyclin D1, CDK5/p35 and CDK6/Cyclin D3 with IC50 of 210 nM, 47 nM, 360 nM, 100 nM, 13 nM and 170 nM, respectively.

AT7519 trifluoroacetate is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM; less potent to CDK3 and little active to CDK7.

AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor, inhibits human GSK3α and GSK3β with Ki of 6.9 nM and 31 nM, respectively, shows >14-fold selectivity against CDK2, CDK5, CDK1 and Erk2.

AZD4573 is a CDK9 inhibitor with an IC50 of <3 nM extracted from patent US 20160376287 A1, example 14.

AZD5438 is a potent inhibitor of CDK1/2/9 with IC50 of 16 nM/6 nM/20 nM. It is less potent to CDK5/6.

AZD-5597 is potent CDK inhibitor with in vitro anti-proliferative effects against a range of cancer cell lines.

BAY 1143572 is a highly selective, potent and orally available inhibitor of PTEFb/CDK9; inhibits the proliferation of AML cell lines with a median IC50 of 385 nM.

BAY-958 (BAY958, LDC526) is a potent, selective PTEFb/CDK9 inhibitor with IC50 of 5 nM against CDK9/CyclinT1.

BMS-265246 is a potent and selective CDK1/2 inhibitor for CDK1/cyclin B and CDK2/cyclin E with IC50 of 6 nM and 9 nM, respectively.

BS-181 is a highly selective CDK7 inhibitor with IC50 of 21 nM. ; >40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.

BS-181 is a highly selective CDK7 inhibitor with IC50 of 21 nM. ; >40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.

BS-194 is a selective and potent CDK inhibitor, which inhibits CDK2, CDK1, CDK5, CDK7, and CDK9 with IC50 values of 3, 30, 30, 250, and 90 nM respectively.

Ca2+ channel agonist 1 is a N-type Ca2+ channel activity agonist, with EC50 of 14.23 uM, also inhibits cdk2 kinase activity with EC50 of 3.34 uM.

Canertinib (CI-1033) is a pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, no activity to PDGFR, FGFR, InsR, PKC, or CDK1/2/4. Phase 3. CI-1033 shows excellent potency for irreversible inhibition of erbB2 autophosphorylation in MDA-MB

CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with IC50 value of 5 nM.

CCT251921 is a potent, selective, and orally bioavailable small-molecule modulators of the mediator complex-associated kinases CDK8 and CDK19. (IC50 data: CDK8:=2.3 nM; CDK19 = 2.6 nM).

CDK12 inhibitor 2 is a potent, selective, non-covalent CDK12 inhibitor with IC50 of 52 nM, displays >192-fold selectivity over CDK2/7/8/9.

CDK12 inhibitor E9 S-isomer (E9, CDK12-IN-E9) is a clinical analog of THZ1 and a selective, covalent CDK12 inhibitor that is not susceptible to ABC transporter-mediated drug efflux.

Cdk4/6 Inhibitor IV is a cell-permeable triaminopyrimidine compound acting as a reversible and ATP-competitive inhibitor of Cdk4/6 (IC50 = 1.5 µM and 5.6 µM for Cdk4/D1 and Cdk6/D1, respectively)

CDK9-IN-1 is a novel, selective CDK9 inhibitor for the treatment of HIV infection.

CDK-IN-2 is a potent and sepecific CDK inhibitor.

Compound 919278 is a specific inhibitor of lymphotoxin β receptor (LTβR, IC50=0.169 uM), and TNF receptor superfamily member 12A (FN14)-dependent nuclear translocation of p52 (IC50=0.167 uM) via inhibiting CDK12/CCNK, does not inhibit the TNF-α-mediated nuclear translocation of p65 (RelA).

CVT-313(NG-26) is a potent, selective, reversible, and ATP-competitive inhibitor of CDK2 (IC50 = 0.5 uM for Cdk2/A and Cdk2/E; 4.2 uM for Cdk1/B; 215 uM for Cdk4/D1).

CYC065 is an orally bioavailable inhibitor of cyclin dependent kinases 2, 5 and 9 (CDK2/5/9) with potential antineoplastic and chemoprotective activities.

Dinaciclib (SCH727965) is a novel and potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM, respectively.

Fascaplysin is a potent, selective ATP-competitive CDK4 inhibitor (IC50 = 350 nM).

Flavopiridol competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM, and CDK7 with IC50 of 300 nM.

Flavopiridol hydrochloride 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 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA.

G1T28(Trilaciclib) is a potential first-in-class, short-acting IV CDK4/6 inhibitor being developed to preserve hematopoietic stem cells and enhance immune system function during chemotherapy.

ICEC0942 is a selective CDK7 inhibitor, with IC50s of 41 nM and 578 nM for CDK7/CycH/MAT1 and CDK2/cycE1, respectively.

JNJ-7706621 is pan-CDK inhibitor with the highest potency on CDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity for CDK1/2 than CDK3/4/6; also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.

Kenpaullone is an ATP-competitive inhibitor of several cyclin-dependent kinases (CDKs) as well as glycogen synthase kinase 3β (GSK3β).

LDC000067(LDC-067) is a highly specific CDK9 inhibitor with IC50 of 32.7 nM for CDK9/cyclin T1; displays 55/125/210/ >227/ >227-fold selectivity for CDK9 versus CDK2/1/4/6/7.

LDC4297 is a novel CDK7 inhibitor.

LEE011 Hcl is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity.

LEE011 is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity.

LEE011 succinate is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity.

LY2835219 is an orally available cyclin-dependent kinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity.

LY2835219 is an orally available cyclin-dependent kinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity.

LY3177833 is a novel CDC7 inhibitor,CDC7/DBF4 IC50 = 3.3 nM, pMCM2 (S53) IC50 = 290 nM and IVTI TEC70 = 1.6 mcM.

Mad2 Inhibitor-1 (M2I-1) is a small molecule protein-protein interaction inhibitor targeting the mitotic spindle assembly checkpoint.

MSC2530818, a CDK8 inhibitor with the IC50 of 2.6 nM, displays excellent kinase selectivity, biochemical and cellular potency, microsomal stability, and is orally bioavailable.

NSC23005 sodium is a novel and effective p18 inhibitor (ED50=5.21 nM) in promoting Hematopoietic stem cells (HSCs) expansion in both murine and human models.

NU 6027 inhibits both CDK1 and CDK2 with IC50 values of 2.9 and 2.2 µM, respectively.

NU2058 is a guanine-based CDK inhibitor with IC50 of 17 μM and 26 μM for CDK2 and CDK1.

NU6300 is a non-covalent ATP-competitive CDK2 inhibitor (IC50 = 0.16 mM).

NVP-LCQ195 (AT9311; LCQ195) is a small molecule heterocyclic inhibitor of CDK1, CDK2, CDK3 and CDK5 with IC50 of 1-42 nM.

ON123300 is a novel multiple kinase inhibitor.

Palbociclib (PD-0332991) is an orally available pyridopyrimidine-derived cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity.

Palbociclib is an oral, small molecule cyclin-dependent kinase 4/6 (CDK4/6) inhibitor, now in Phase 3 clinical development for advanced breast cancer.

Palbociclib isethionate(PD-0332991 isethionate) is a highly specific inhibitor of Cdk4 (IC50=11 nM) and Cdk6 (IC50=16 nM), having no activity against a panel of 36 additional protein kinases.

PHA-767491 (CAY10572) Hcl is a potent, ATP-competitive dual Cdc7/Cdk9 inhibitor with IC50 values of 10/34 nM.

PHA-767491 (CAY10572) is a potent, ATP-competitive dual Cdc7/Cdk9 inhibitor with IC50 values of 10/34 nM.

PHA-793887 is a novel and potent inhibitor of CDK2, CDK5 and CDK7 with IC50 of 8 nM, 5 nM and 10 nM, respectively.

PHA-848125(Milciclib) is a potent, ATP-competitive CDK inhibitor for CDK2 with IC50 of 45 nM; >3-fold more selective for CDK2 than CDK1, 2, 4, 5, and 7.

Purvalanol A is a potent, cell-permeable cyclin-dependent protein kinase (cdk) inhibitor.

Purvalanol B(NG-95) is a cyclin-dependent kinase inhibitor with IC50 values of 6, 6, 9, > 10,000, and 6 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35 respectively.

R547 is a potent and selective CDK inhibitor with Ki and IC50 of 1-3 nM and 80 nM respectively.

RGB-286638 is a novel CDK inhibitor with IC50s of 1 nM/2 nM/3 nM/4 nM/5 nM for cyclin T1-CDK9/cyclin B1-CDK1/cyclin E-CDK2/cyclin D1-CDK4/cyclin E-CDK3/p35-CDK5 respectively; less potent against cyclin H-CDK7 and cyclin D3-CDK6.

Ro-3306 is a potent and selective inhibitor of CDK1 with Ki value of 35 nM for CDK1/cyclin B1, 10-fold selectivity relative to CDK2/cyclin E and >50-fold relative to CDK4/cyclin D.

Roniciclib is an orally bioavailable pan-cyclin dependent kinase (CDK) inhibitor, with IC50s of 5-25 nM for CDK1, CDK2, CDK3, CDK4, CDK7 and CDK9.

Roscovitine (Seliciclib, CYC202, R-roscovitine) is a potent and selective CDK inhibitor for Cdc2/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p53 with IC50 of 0.65 μM, 0.7 μM, 0.7 μM and 0.16 μM, respectively.

SCH900776 (S-isomer) is the S-isomer form of SCH900776, which is a potent, selective and orally bioavailable inhibitor of checkpoint kinase Chk1 (IC50 = 3 nM), highly selective against Chk2 (IC50 = 1500 nM) and cyclin-dependent kinase CDK2 (IC50

Senexin A is a potent and selective inhibitor of CDK8 and its nearest relative, CDK19 with Kd values of 0.83 μM and 0.31 μM for CDK8 and CDK19 ATP site binding, respectively.

SNS-032(BMS-387032) is a potent inhibitor of cyclin-dependent kinases (cdks) 9, 2 and 7 (IC50 values are 4, 38 and 62 nM respectively).

SU-9516 is a selective CDK2 inhibtor with IC50 of 22 nM; less potent for CDK1/CDK4(IC50=40/200 nM), no inhibition on PKC, EGFR, p38MAPK etc.

THZ1 is a novel selective and potent covalent CDK7 inhibitor with IC50(binding affinity) of 3.2 nM; inhibits Jurkat cell's proliferation with IC50 of 50 nM.

THZ1 is a novel selective and potent covalent CDK7 inhibitor with IC50(binding affinity) of 3.2 nM; inhibits Jurkat cell's proliferation with IC50 of 50 nM.

THZ531 is a covalent CDK12 and CDK13 covalent inhibitor.

Voruciclib is a protein kinase inhibitor specific for the cyclin-dependent kinase 4 (CDK4) with potential antineoplastic activity.

WHI-P180(Janex 3) is a potent inhibitor of IgE-mediated mast cell responses to allergens in vitro and in vivo. Also inhibits cyclin-dependent kinase 2 (CDK2; IC50 = 1µM) by blocking the ATP site

THZ2 is a potent and selective CDK7 inhibitor with IC50 of 13.9 nM.

SB1317(TG-02) is a novel small molecule potent CDK2/JAK2/FLT3 inhibitor with IC50s of 13/73/56 nM respectively.

SR-4835 is a highly selective dual inhibitor of CDK12 and CDK13.

TCMDC-135051 is a highly selective and potent protein kinase PfCLK3 inhibitor with low off-target toxicity. TCMDC-135051 prevents trophozoite-to-schizont transition, disrupts transcription and reduces transmission to the mosquito vector. TCMDC-135051 has antiparasiticidal activity (EC50=320 nM).

Cdk1/2 Inhibitor III is a selective Cdk1/2 inhibitor, with an IC50 of 2.1 μM for CDK1/cyclin B.

(2S,3R)-Voruciclib is the (2S,3R)-enantiomer of Voruciclib. (2S,3R)-Voruciclib is an orally active CDK inhibitor.

CDK ligand for PROTAC is a CDK inhibitor with antitumor activity. CDK ligand for PROTAC and a CRBN ligand have been used to design PROTAC CDK4/6 degrader.

CDK ligand for PROTAC hydrochloride is a CDK inhibitor with antitumor activity. CDK ligand for PROTAC hydrochloride and a CRBN ligand have been used to design PROTAC CDK4/6 degrader.

CDK9-IN-9 (example 2) is a potent and selective CDK9 inhibitor with an IC50 of 1.8 nM. CDK9-IN-9 inhibits CDK2 with an IC50 of 155 nM. CDK9-IN-9 has anti-cancer activity.

Cdc7-IN-3 (compound I-A) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-B. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.

Cdc7-IN-4 (compound I-C) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-C. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.

Cdc7-IN-5 (compound I-B) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-B. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.

Cdc7-IN-6 (compound I-D) is a potent Cdc7 kinase inhibitor (IC50=4 nM), extracted from patent WO2019165473A1, compound I- D, has anti-tumor activity.

Cdc7-IN-7 (compound I-E) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-E. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.

(R)-CR8 trihydrochloride (CR8 trihydrochloride), a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 trihydrochloride inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 trihydrochloride induces apoptosis and has neuroprotective effect.

CDK7-IN-1, an analog of YKL-5-124, is a cyclin-dependent kinase 7 (cdk7) inhibitor, with an IC50 of less than 100 nM, extracted from patent WO 2016105528 A2, Compound 215.

CLK-IN-T3N, the negative control of CLK-IN-T3, is a chemical probe for CDC-like kinase (CLK).

Ribociclib D6 (LEE011 D6) 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.

CDK7/9 tide is peptide substrate for CDK7 or CDK9.

KB-0742 dihydrochloride is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 dihydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 dihydrochloride has potent anti-tumor activity.

GSK-3/CDK5/CDK2-IN-1, an imidazole derivative, is an inhibitor of cdk5, cdk2, and GSK-3 extracted from patent WO2002010141A1, example 9a. GSK-3/CDK5/CDK2-IN-1 can be used for the research of cancer, and neurodegenerative diseases.

M2N12 is a potent and highly selective cell division cycle 25C protein phosphatase (Cdc25C) inhibitor with an IC50 value of 0.09  μM. M2N12 also has promising activity against Cdc25A and Cdc25B with IC50 values of  0.53  μM and 1.39 μM, respectively. M2N12 has anti-tumor activity and can be used for cancer research.

CDK6/9-IN-1 (compound 66) is an orally active active and dual CDK 6 and CDK 9 inhibitor, with IC50 values of 40.5 nM and 39.5 nM for CDK6 anmd CDK9, respectively.

CDK7-IN-3 is a selective CDK7 inhibitor with a KD of 0.059 nM. CDK7-IN-3 shows poor inhibition on CDK2 (Ki=390 nM), CDK9 (Ki=290 nM), CDK12 (Ki=78 nM). CDK7-IN-3 induce apoptosis in tumor cells and has antitumor activity.

CDK-IN-6, a class of pyrazolo[1,5-a]pyrimidine compound, is a CDK inhibitor with anticancer activities.

BSJ-4-116 is a specific degrader of cyclin-dependent kinase 12 (CDK12). BSJ-4-116 exhibits potent antiproliferative effects.

CDK4 inhibitor compound 12 is a novel inhibitor of CDK4 with the activity 97 μM.

LY3405105 is an orally active CDK7 inhibitor with an IC50 of 92.8 nM. LY3405105 shows potential antineoplastic activity.

Indirubin-3′-oxime (IDR3O), a synthetic derivative of indirubin, is a potent inhibitor of cyclin-dependent kinases (CDKs) and glycogen synthase kinase 3β (GSK3β). Indirubin-3′-oxime directly inhibits the activity of all three isoforms of JNK (JNK1, JNK2, and JNK3), with IC50s of 0.8 μM, 1.4 μM, and 1.0 μM, respectively. Indirubin-3′-oxime can enhance height growth via activation of Wnt/β-catenin signaling in chondrocytes.

Samuraciclib (CT7001) trihydrochloride is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib trihydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib trihydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib trihydrochloride has anti-tumor effects.

CDK12-IN-2 is a potent, selective and nanomolar CDK12 inhibitor (IC50=52 nM) with good physicochemical properties. CDK12-IN-2 is also a strong CDK13 inhibitor due to CDK13 is the closest homologue of CDK12. CDK12-IN-2 shows excellent kinase selectivity for CDK12 over CDK2, 9, 8, and 7. CDK12-IN-2 inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II. CDK12-IN-2 can be used an excellent chemical probe for functional studies of CDK12.

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.

CDK7-IN-2 hydrochloride hydrate (Example 6) is a potent and selective CDK7 inhibitor. CDK7-IN-2 has potent anti-cancer activity.

CDK4/6-IN-5 is a potent CDK4 and CDK6 inhibitor with Kis of 0.2 and 4.4 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively. (from patent WO2019207463A1 example A93).

PF-07104091 hydrate is a potent and selective CDK2/cyclin E1 and GSK3β inhibitor, with Kis of 1.16 and 537.81 nM, respectively. PF-07104091 hydrate has anti-tumor activity for cyclin E1-amplified cancers. (patent WO2020157652A2).

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).

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).

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).

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.

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.

CDK8-IN-1 is a potent and selective CDK8 inhibitor with an IC50 of 3 nM.

[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).

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.

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.

Avotaciclib (BEY1107) is an orally active cyclin dependent kinase 1 (CDK1) inhibitor. Avotaciclib can be used for the research of cancer.

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.

Ocarocoxib, a potent COX-​2 (cyclooxygenase-​2) inhibitor, is a non-steroidal anti-inflammatory for veterinary use.

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.

Cimpuciclib is a cyclin-dependent kinase(CDK) inhibitor and antineoplastic.

CDK5-IN-1, a potent CDK5 inhibitor, is against CDK5 activity less than 10 nM. CDK5-IN-1 is used for kidney diseases research.

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.

Cirtuvivint (SM08502) is a potent and orally active CDC-like kinase (CLK) inhibitor. Cirtuvivint can be used for solid tumors research.

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.

CDK9-IN-12 displays the optimal CDK9 inhibitory activity with an IC50 value of 5.41 nM.

JH-XVI-178 is a highly potent and selective inhibitor of CDK8/19 that displays low clearance and moderate oral pharmacokinetic properties.

CDK2-IN-7 is a CDK2 inhibitor for treating cancer (IC50 < 50 nM).

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.

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.

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).

DS96432529 is a potent and orally active bone anabolic agent through CDK8 inhibition.

CDK7-IN-7 is a potent and selective CDK7 kinase inhibitor with an IC50 of <50 nM (Patent CN112661745A, compound T-01).

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.

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.

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.

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.

Eciruciclib is an antineoplastic and potent cyclin dependent kinase (CDK) inhibitor.

Tanuxiciclib is a cyclin dependent kinase (CDK) inhibitor.

CDK7-IN-10 is a CDK7 inhibitor with an IC50 of less than 100 nM, extracted from patent WO2021016388A1, compound I-1. CDK7-IN-10 is useful in inhibiting the activity of a kinase. CDK7-IN-10 has the potential of inhibiting cell growth and inducing cell apoptosis.

7BIO (7-Bromoindirubin-3-Oxime) is the derivate of indirubin. 7BIO (7-Bromoindirubin-3-Oxime) has inhibitory effects against cyclin-dependent kinase-5 (CDK5) and glycogen synthase kinase-3β (GSK3β). 7BIO (7-Bromoindirubin-3-Oxime) inhibits Aβ oligomer-induced neuroinflammation, synaptic impairments, tau hyper-phosphorylation, activation of astrocytes and microglia, and attenuates Aβ oligomer-induced cognitive impairments in mice[1].

NSC 107512 is a potent inhibitor of cyclin-dependent kinase 9 (CDK9). NSC 107512 is a class of sangivamycin-like molecules (SLM). NSC 107512 inhibits growth and induces apoptosis of multiple myeloma tumors.

CK7, a Cdk2/9 inhibitor, can be used for the synthesis of Nek1 inhibitor BSc5231 and BSc5367.

CDK6/PIM1-IN-1 is a potent and balanced dual CDK6/PIM1 inhibitor with IC50 values of 39 and 88 nM, respectively. CDK6/PIM1-IN-1 inhibits CDK4 (IC50=3.6 nM). CDK6/PIM1-IN-1 significantly inhibits acute myeloid leukemia (AML) cell proliferation, arrest cell cycle at the G1 phase, and promote cell apoptosis. CDK6/PIM1-IN-1 exhibits potent anti-AML activity.

CDK9-IN-13 (compound 38) is potent and selective CDK9 inhibitor, with an IC50 of <3 nM. CDK9-IN-13 exhibits short half-lives in rodents.

CDK5-IN-2 (compound 15) is a highly selective CDK5 inhibitor with IC50s of 0.2 and 23 for CDK5/p25 and CDK2/CycA, respectively.

dCeMM4 (Compound 5) is a glue degrader. dCeMM4 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex.

(E/Z)-Zotiraciclib ((E/Z)-TG02) hydrochloride is a potent CDK2, JAK2, and FLT3 inhibitor.

CDK4/6-IN-11 is a potent PROTAC CDK4/6 degrader.

(R)-CTX-712 is a potent inhibitor of cdc2-like kinase (CLK). (R)-CTX-712 inhibits CLK kinase activity, and thus inhibits cancer survival and cancer cell growth. (R)-CTX-712 has the potential for the research of cancer disease (extracted from patent JPWO2017188374A1, compound 286).

CDK7-IN-2 is a potent inhibitor of CDK7. CDK7 is implicated in both temporal control of the cell cycle and transcriptional activity. CDK7 is implicated in the transcriptional initiation process by phosphorylation of Rbpl subunit of RNA Polymerase II (RNAPII). CDK7 has the potential for the research of cancer disease, in particular aggressive and hard- to-treat cancers (extracted from patent WO2019099298A1, compound 1).

CDK5-IN-3 (compound 11) is a potent and selective CDK5 inhibitor, with IC50s of 0.6 nM and 18 nM for CDK5/p25 and CDK2/CycA, respectively. CDK5-IN-3 can be used for the research of autosomal dominant polycystic kidney disease (ADPKD).

SZ-015268 is a CDK7 inhibitor with an IC50 of 23.56 nM. SZ-015268 has extremely significant anti-tumor advantages. SZ-015268 inhibits HCC70, OVCAR-3, HCT116 and HCC1806 cells proliferation with IC50s of 33, 80.56, 12.53, and 61.55 nM, respectively.

CDK7-IN-12 is a potent inhibitor of CDK7. CDK7-IN-12 plays a key role in transcriptional regulation and cell cycle regulation. CDK7-IN-12 effectively inhibit malignant tumor proliferation in vitro and in vivo. CDK7-IN-12 has the potential for the research of cancer disease (extracted from patent WO2021249417A1, compound 43).

CDK1-IN-7 is a potent CDK1 inhibitor (CDK1/CycB IC50=161.2 nM) with potential antiproliferative activity and selectivity for cancer tissues. CDK1-IN-7 induces apoptosis in p53 dependent manner through the intrinsic apoptotic pathway. CDK1-IN-7 is a potential targeted antitumor agent.

FLT3/CDK4-IN-1 is a potent, high selective and orally active FLT3/CDK4 dual inhibitor (IC50=11 and 7 nM for FLT3 and CDK4, respectively). FLT3/CDK4-IN-1 has antiproliferative activities against certain cancer cells. FLT3/CDK4-IN-1 has good antitumor effect in vivo.

dCeMM2 (Compound 2) is a glue degrader. dCeMM2 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex.

dCeMM3 (Compound 3) is a glue degrader. dCeMM3 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex.

NSC693868 is a selective inhibitor of CDK1 and CDK5 with IC50s of 600 nM and 400 nM, respectively. NSC693868 less potently inhibits GSK3β with an IC50 of 1 µM) and does not block CDC25 activity. NSC693868 is used to help define the roles of CDK1 and CDK5 in various signaling pathways.

5,6-Dichlorobenzimidazole riboside is a nucleoside analog that inhibits several carboxyl-terminal domain (CTD) kinases including casein kinase II and CDKs. 5,6-Dichlorobenzimidazole riboside trigger p53-dependent apoptosis of human colon adenocarcinoma cells without inducing genotoxic stress to healthy cells.

(E/Z)-Zotiraciclib citrate is a potent CDK2, JAK2, and FLT3 inhibitor.

Anticancer agent 30 (compound 6f-Z), a 3-arylidene-2-oxindole derivative, is a selective CDK2 inhibitor with potent anticancer activity.

Anticancer agent 29 (Compd E/Z-6f) is an anticancer agent, with IC50 values of 0.054 μM, 0.127 μM, 0.129 μM, 0.396 μM for CDK2, CDK1, CDK4 and CDK6, respectively.

DD-03-156 is a potent and selective degrader of CDK17 and LIMK2. The selectivity and potency of DD-03-156 is exquisite and makes an advanced starting point for the development of a chemical probe for the degradation of CDK17.

THZ-1 hydrochloride is a potent, selective, covalent CDK7 inhibitor with IC50 of 3.2 nM.

(R)-CR8 is a potent CDK1/2/5/7/9 inhibitor, inhibits CDK1/cyclin B (IC50, 90 nM), CDK2/cyclin A (72 nM), CDK2/cyclin E (41 nM), CDK5/p25 ( 110 nM), CDK7/cyclin H (1.1 uM), CDK9/cyclin T (0.18 uM) and CK1δ/ε (0.4 uM); (R)-CR8 induces apoptosis and has neuroprotective effect, CR8 alsp acts as a molecular glue degrader that depletes cyclin K.

A-1592668 (A 1592668) is a novel potent, CDK9-selective inhibitor with IC50 of 1.2 nM, >1000 fold selectivity over CDK1/2/7/8; A-1592668 also displays selectivity of ~12- and 240-fold over CDK4 and CDK6 respectively. A-1467729 inhibited phosphorylation of RNA pol-II (p-RNA pol-II; Ser2) with a potency of 26.7 nM at the cellular level, inhibited MCL-1 dependent hematologic tumor cell lines H929 (IC50=39 nM) and MV4-11 (IC50=42.4 nM) following 24 h of incubation.

ASP9822 is a novel potent selective CDK7 inhibitor with IC50 of 4.3 nM, with anti-cancer activity.

AZ5576 (AZ-5576) is a potent, selective CDK9 inhibitor with an IC 50 <5 nM, decreases phosphorlyation of Ser2-RNAPII in cells with an IC 50 of 96 nM.AZ5576 downregulated Mcl-1 and MYC protein abundance across multiple tested DLBCL cell lines and in primary DLBCL cells.MYC sensitizes DLBCL cells to AZ5576, genetic downregulation of MYC in U-2932 and OCI-LY19 cells resulted in diminished susceptibility to AZ5576.AZ5576 dose-dependently downregulated MYC transcription of a luciferase reporter containing multiple canonical MYC-MAX-binding sites, an effect more pronounced compared with multi-CDK inhibitor dinaciclib.AZ5576 restricts growth of xenografted DLBCL tumors in vivo.

bio-THZ1 is a biotinylated version of THZ1 and binds irreversibly to CDK7.

CDDD11-8 is a potent CDK9 inhibitor co-targeting FLT3-ITD with Ki values of 8 and 13 nM, respectively.CDDD11-8 displays excellent kinome selectivity in a panel of 369 human kinases.CDDD11-8 displays antiproliferative activity against leukemia cell lines, and particularly potent effects against MV4-11 and MOLM-13 cells, which are known to harbor the FLT3-ITD mutation and mixed lineage leukemia (MLL) fusion proteins.CDDD11-8 causes a robust tumor growth inhibition by oral administration in animal xenografts, induces tumor regression at dose of 125 mg/kg.

CDDD2-94 is a highly potent and selective CDK4 inhibitor with Ki of 2 nM, >140-fold selective for CDK4 over CDK6 (Ki=279 nM).CDDD2-94 is ineffective against other members of the CDK family, displays high selectivity against a panel of 369 human kinases at 1uM, with exceptionally selective-CLK, DYRKs and MYLK4 were the only kinases targeted potently.CDDD2-94 is the most selective CDK4 inhibitor identified to date.CDDD2-94 demonstrated antiproliferative activityagainst MV4-11 and MDA-MB-453 cell lines with GI50 of 0.107 and 0.325 uM respectively.CDDD2-94 inhibits S780-phosphorylated Rb (pRb(S780)) and decreases transcription of Rb1 and E2F-target genes in MDA-MB-453 cells.CDDD2-94 is well tolerated and efficacious in preclinical OC xenograft model, CDDD2-94 provides better safety profile than palbociclib towards the bone marrow.

MFH290 (MFH-290) is a potent, highly selective, covalent inhibitor of CDK12/13 with IC50 of 25/49 nM.MFH290 forms a covalent bond with Cys-1039 of CDK12, and CDK12-dependent as mutation of Cys-1039 rendered the kinase refractory to MFH290.MFH290 exhibits excellent kinome selectivity, inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II), and reduces the expression of key DNA damage repair genes.MFH290 restored Pol II CTD phosphorylation and DNA damage repair gene expression AND augments the antiproliferative effect of the PARP inhibitor olaparib.

PF-06842874 is a potent, selective CDK4/6 inhibitor.

Senexin C is a novel potent, selective and orally bioavailable CDK8/19 inhibitor with Kd of 1.4 and 2.9 nM for CDK8/CycC and CDK19/CycC, respectively.Senexin C inhibits CDK8/CycC with IC50 of 3.6 nM, shows high selectivity against other HDAC isoforms.Senexin C is more metabolically stable and provides a more sustained inhibition of CDK8/19-dependent cellular gene expression when compared with the prototype inhibitor Senexin B.Senexin C inhibits MV4-11 leukemia growth in a systemic in vivo model with good tolerability.

SY-5102 (SY5102) is a highly potent, selective, noncovalent, orally available CDK7 inhibitor with SPR Kd of 0.03 nM (binding to CDK7/Cyclin H).SY-5102 (SY5102) displays highly selectivity against CDK2, CDK9, and CDK12 (all IC50>75 nM).SY-5102 potently inhibits HCC70 cell proliferation with EC50 of 9 nM.SY-5102 showed dose-dependent tumor growth inhibition including tumor regression at 4 mg/kg po (dosed twice daily) in an HCC70 cell line derived xenograft mouse model.

(S)-CR8 is the S-isomer of CR8. (S)-CR8 is a potent and selective CDK inhibitor with IC50s of 0.060, 0.080, 0.11, 0.12, and 0.15 μM for CDK2/cyclin E, CDK2/cyclin A, CDK9/cyclin T, CDK5/p25, and CDK1/cyclin B, respectively. (S)-CR8 reduces SH-SY5Y cells survival (IC50 0.40 μM).

ZDLD20, a β-carboline, is orally active and selective CDK4/CycD3 inhibitor with an IC50 value of 6.51  μM. ZDLD20 exhibits potent anti-HCT116 activity including inhibition of colony formation, inhibition of invasion and migration, inducing of apoptosis, and arresting of G1 phase in cell cycle. ZDLD20 exhibits potent anticancer activity.

ZDLD13, a β-carboline, is an orally active and selective CDK4/CycD3 inhibitor with an IC50 value of 0.38 μM. ZDLD13 exhibits potent anti-HCT116 activity including inhibition of colony formation, inhibition of invasion and migration, inducing of apoptosis, and arresting of G1 phase in cell cycle. ZDLD13 shows significant tumor growth inhibition in HCT116 tumor xenograft model.

Dalpiciclib (SHR-6390) hydrochloride is an orally active and highly selective inhibitor of CDK4 and 6 with IC50 values of 12.4 nM and 9.9 nM, respectively. Dalpiciclib hydrochloride shows antitumor activity against breast cancer and esophageal squamous cell carcinoma.

Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride hydrate has anti-tumor effects.

FN-1501 is a potent inhibitor of Fms-like receptor tyrosine kinase 3 (FLT3) and cyclin-dependent kinase (CDK), with IC50s of 2.47, 0.85, 1.96, and 0.28 nM for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 and FLT3, respectively.

Palbociclib (PD 0332991) orotate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib orotate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib orotate can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.

PROTAC CDK12/13 Degrader-1 (7f) is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 has anti-proliferative activity and can be used in breast cancer research.

Ulecaciclib is an orally activitive inhibitor of cyclin-dependent kinase (CDK), with Ki values of 0.62 μM (CDK2/Cyclin A), 0.2 nM (CDK4/Cyclin D1), 3 nM (CDK6/Cyclin D3), and 0.63 μM (CDK7/Cyclin H), respectively. Ulecaciclib can cross blood brain barrier and has good pharmacokinetic characteristics.

DSS30 is a P25/CDK5 inhibitor that reduces β-amyloid (Aβ) secretion by inhibiting amyloid precursor protein lyase 1 (BACEl) phosphorylation. DSS30 can be used in the study of neurodegenerative diseases such as Alzheimer's disease.

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.