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Bisindolylmaleimide X hydrochloride (BIM-X hydrochloride) is a potent and selective protein kinase C (PKC) inhibitor. Bisindolylmaleimide X hydrochloride is a potent cyclin-dependentkinase 2 (CDK2) antagonist with an IC50 of 200 nM .
GW8510 is a potent cyclin-dependentkinase-2 (CDK2) inhibitor. GW8510 is also a ribonucleotide reductase M2 (RRM2) inhibitor. GW8510 exhibits neuroprotective and anticancer activities .
SNX7 is a Cyclin-DependentKinase Inhibitor (CDKI) pathway inhibitor. SNX7 can be used for research of senescence-related and other CDKI-related diseases .
XC219 (compound 43) is a cyclin-dependentkinaseCDK) inhibitor, that covalently binds to CDK active site Lys. XC219 can be used in antifungal research .
OTS964 hydrochloride is an orally active, high affinity and selective TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor with an IC50 of 28 nM . OTS964 hydrochloride is also a potent inhibitor of the cyclin-dependentkinaseCDK11, which binds to CDK11B with a Kd of 40 nM .
NSC 107512 is a potent inhibitor of cyclin-dependentkinase 9 (CDK9). NSC 107512 is a class of sangivamycin-like molecules (SLM). NSC 107512 inhibits growth and induces apoptosis of multiple myeloma tumors .
Aloisine B (compound 9) is a cyclin-dependentkinase (CDK) inhibitor. Aloisine B inhibits cell proliferation by arresting cells in both G1 and G2 via competing with ATP-binding pocket .
OTS964 is an orally active, high affinity and selective TOPK inhibitor with an IC50 of 28 nM . OTS964 is also a potent inhibitor of the cyclin-dependentkinaseCDK11, which binds to CDK11B with a Kd of 40 nM .
CDK8-IN-10 (compound 2) is a potent, selective cyclin-dependentkinase (CDK8) inhibitor with an IC50 value of 8.25 nM. CDK8-IN-10 can be used for research of cancer .
CDK7-IN-31 (compound 13) is a potent and orally active cyclin-dependentkinase 7 (CDK7) inhibitor with a Kd value of 0.18 nM. CDK7-IN-31 shows anticancer activity .
(S)-PHA533533 is a cyclin-dependentkinase 2 (CDK2) inhibitor. (S)-PHA533533 shows anti-tumor activity and can induce widespread neuronal UBE3A expression in angelman syndrome model mice .
CDK7-IN-1, an analog of YKL-5-124, is a cyclin-dependentkinase 7 (cdk7) inhibitor, with an IC50 of less than 100 nM, extracted from patent WO 2016105528 A2, Compound 215 .
CDK7-IN-27 (Compound 37) is a selective inhibitor for cyclin-dependentkinase 7 (CDK7), with Ki of 3 nM. CDK7-IN-27 arrests the cell cycle at G0/G1 phase .
H1k, a Eudistomin Y derivative, is a lysosome-targeted antiproliferation agent. H1k increases the autophagy signal and downregulate the expression of cyclin-dependentkinase (CDK1) and cyclin B1. H1k can be used in research of cancer .
PF-06873600 is a selective and orally bioavailable inhibitor of cyclin-dependentkinase(CDK), with Ki values of 0.09 nM, 0.13 nM and 0.16 nM for CDK2, CDK4 and CDK6, respectively. PF-06873600 has potential antineoplastic activity .
7-Hydroxystaurosporine (UCN-01) is a synthetic derivative of Staurosporine (HY-15141) with antitumor activity. 7-hydroxystaurosporine inhibits serine/threonine kinaseAKT and calcium-dependentprotein kinase C activity. 7-hydroxystaurosporine also activates indirectly cyclin-dependentkinases (CDKs). 7-hydroxystaurosporine arrests tumor cells in the G1/S of the cell cycle and prevents nucleotide excision repair by inhibiting the G2 checkpoint kinase chk1, resulting in apoptosis .
PROTAC CDK2 Degrader-1 (Compound 41) is a PROTAC degrader for cyclin-dependentkinase 2 (CDK2). PROTAC CDK2 Degrader-1 inhibits the phosphorylation of RB protein in CDK2 dependent cell line OVCAR3 with an IC50 of 100-500 nM .
Metralindole hydrochloride is a significant inhibitor of human cyclin-dependentkinase-2 and Human Protein Kinase CK2 Holoenzyme, exhibiting high binding affinity in the context of lung cancer treatment. Metralindole hydrochloride demonstrates promising docking scores and molecular dynamics stability, indicating its potential efficacy as a therapeutic agent against non-small cell lung cancer. Metralindole hydrochloride further shows excellent pharmacokinetic properties, including outstanding solubility and bioavailability, making it a compelling candidate for future experimental validation in lung cancer therapy.
Anticancer agent 241 (HZ1) is an orally active first-in-class cyclin-dependentkinase like 3 (CDKL3)-specific inhibitor. Anticancer agent 241 shows a strong tumor-suppressing effect, and has the potential to overcome the resistance of CDK4/6 inhibitor .
7BIO (7-Bromoindirubin-3-Oxime) is the derivate of indirubin. 7BIO (7-Bromoindirubin-3-Oxime) has inhibitory effects against cyclin-dependentkinase-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].
3-ATA (NSC 680434) is a selective inhibitor of cyclin-dependentkinase 4 (CDK4) with neuroprotective and antitumor effects. 3-ATA can alleviate kainic acid (HY-N2309)-induced apoptosis in cerebellar granule neurons, which can be used in the study of neurodegenerative diseases .
Akt1&PKA-IN-1 is a potent dual Akt/PKA inhibitor with IC50 values of 0.03 , 0.11 μM, and 9.8 μM for PKAa, Akt, and CDK2, respectively. Akt1&PKA-IN-1 is selective for cyclin-dependentkinase 2 (CDK2) .
CDK9-IN-2 is a special cyclin-dependentkinase 9 (CDK9) inhibitor, extracted from patent WO/2012131594A1, compound CDKI(8), has an IC50 of 5 nM and 7 nM in H929 multiple myeloma(MM) cell line (72 hours) and A2058 skin cell line (72 hours), respectively.
CDK8/19-IN-2 (compound 12) is an orally active and potent cyclin-dependentkinase 8/19 (CDK8 and CDK19) inhibitor, with IC50 values of 2.08 and 2.49 nM, respectively. CDK8/19-IN-2 can be used for acute myeloid leukemia (AML), breast cancer, and lymphoma research .
FLT3/CDKs ligand-1 (Compound 14) is a ligand for target protein, which promotes the degradation of cyclin-dependentkinase (CDK) and the FMS-like tyrosine kinase 3 (FLT3), inhibits FLT3/CDK related proliferations and survivals of leukemia cells. LT3/CDKs ligand-1 can be used for synthesis of PROTAC FLT3/CDKs degrader-1 (HY-161708) .
CDK7-IN-4 (compound I) is a potent CDK7 (Cyclin-dependentkinase 7) inhibitor. CDK7-IN-4 shows anticancer activity. CDK7-IN-4 inhibits the in vitro growth of cancer cell lines from a variety of histologies including colon , breast , lung , ovary and stomach , in a dose dependent manner .
CDK4/6-IN-12 is a potent cyclin-dependentkinase 4/6 (CDK4/6) inhibitor. CDK4/6-IN-12 has enzymatic inhibitory activity for CDK4 and CDK6 with IC50 of 592.3 nM and 3090 nM, respectively. CDK4/6-IN-12 can be used for the research of cancer .
Akt1&PKA-IN-2 ((R)-29) is an inhibitor of PKB/AKT with cyclin-dependentkinase 2 (CDK2) selectivity. Akt1&PKA-IN-2 inhibits AKT1, PKAa and CDK2 a with IC50 values of 0.007 µM, 0.01 µM and 0.69 µM, respectively .
1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC (PC(18:0/22:4)) is an inhibitor of cyclin-dependentkinases (CDKs).? 1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC induces apoptosis and inhibits the growth of various cancer cell lines .
P-gp/CDK2-IN-1 (Compound 4j) is an inhibitor for is inhibitor for P-glycoprotein (P-gp) and for cyclin-dependentkinase-2 (CDK2). P-gp/CDK2-IN-1 inhibits the proliferation of cancer cells SW-480 and MCF-7 wit IC50 of 38.6 μM and 26.6 μM. P-gp/CDK2-IN-1 exhibits antioxidant efficacy with EC50 of 580 μM in DPPH experiment .
CDK-IN-14 (Compound 9) is a potent and selective CDKL2 (Cyclin-dependentkinase-like 2) inhibitor with an IC50 value of 460 nM. CDKL2 is involved in various biological processes such as tumorigenesis, development, and viral infections. CDK-IN-14 serves as a powerful tool for studying the biological functions of CDKL2 and holds promise for research in fields related to cancer, infections, and other diseases .
Riviciclib (P276-00 free base) is a potent cyclin-dependentkinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively .
Riviciclib shows antitumor activity on cisplatin-resistant cells .
Vanicoside B is a phenylpropanoyl sucrose derivative, can be isolated from the herb Persicaria dissitiflora. Vanicoside B targets cyclin-dependentkinase 8 (CDK8) and exhibits anti-tumor activity. The potential mechanism is Vanicoside B blocks CDK8-mediated signaling pathways and decreases the expression of epithelial-mesenchymal transition proteins, so that it leads to cell cycle arrest and apoptosis .
MFH290 is a potent and highly selective cyclin-dependentkinase 12/13 (CDK12/13) covalent inhibitor. MFH290 forms a covalent bond with Cys-1039 of CDK12 and exhibits excellent kinome selectivity and inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II). MFH290 is used for cancer research .
Milciclib (PHA-848125) maleate is a cyclin-dependentkinase inhibitor that impairs melanoma cell growth and modulates gene expression involved in cell cycle regulation. Milciclib maleate has been shown to significantly affect the expression of various genes, including down-regulating PTTG1, contributing to its antiproliferative activity. Milciclib maleate enhances sensitivity to treatment in p53 mutated melanoma cells when combined with PTTG1 silencing.
Riviciclib hydrochloride (P276-00) is a potent cyclin-dependentkinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively .
Riviciclib hydrochloride (P276-00) shows antitumor activity on cisplatin-resistant cells .
Indirubin-3′-oxime (IDR3O), a synthetic derivative of indirubin, is a potent inhibitor of cyclin-dependentkinases(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 .
CDK7-IN-6 is a potent and selective cyclin-dependentkinase (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 .
BMS-265246 is a potent and selective cyclin-dependentkinaseCDK1 and CDK2 inhibitor, with IC50 values of 6 and 9 nM, respectively. BMS-265246 inhibits CHI3L1 (chitinase 3-like-1) stimulation of ACE2 (angiotensin converting enzyme 2) and SPP (viral spike protein priming proteases). BMS-265246 can be used for ovarian cancer and COVID-19 research .
Ulecaciclib is an orally activitive inhibitor of cyclin-dependentkinase (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 .
Anticancer agent 199 (Compound G-4) induces apoptosis in triple negative breast cancer (TNBC) cells via the mitochondrial pathway through inhibiting EGFR, AKT and MAPK pathways. Anticancer agent 199 also induces Ferroptosis by down-regulating LCN2. Anticancer agent 199 inhibits TNBC cell viability and migration, and induces S phase cell cycle arrest. Anticancer agent 199 is a derivate of cyclin-dependentkinase inhibitor Rocovitine .
CDK2 degrader 1 (Compound 3) is an orally active cyclin-dependentkinase 2 (CDK2) degrader based on PROTAC technology. CDK2 degrader 1 binds to cereblon to induce ubiquitination and subsequent proteasomal degradation of the CDK2. CDK2 degrader 1 is used in the research of a wide range of cancers (Red: spiro[3.3]heptan-2- ylmethyl carbonochloridate; Blue: N,N-diisopropylethylamine; Black: linker) .
Zotiraciclib hydrochloride is a novel small molecule multi-target enzyme inhibitor with activity in inhibiting tumor growth. Zotiraciclib hydrochloride exerts its anti-tumor effect by reducing the level of Myc through inhibiting cyclin-dependentkinase 9 (CDK9). Zotiraciclib hydrochloride may be useful for inhibiting cancers that cross the blood-brain barrier. The high protein level of MCL-1 of Zotiraciclib hydrochloride is associated with survival, suggesting that it may serve as a prognostic factor and inhibitory target in further studies .
AS2863619 enables conversion of antigen-specific effector/memory T cells into Foxp3 + regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 is a potent, orally active cyclin-dependentkinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 inhibition of CDK8/19, which consequently activates the Foxp3 gene .
DCB-3503 is a small molecule inhibitor of cell cycle progression, which has the activity of inducing G?/G? phase arrest and apoptosis in human hepatoma cells. DCB-3503 can inhibit the proliferation of human hepatoma cells, induce cell cycle arrest and apoptosis, and its mechanism is related to downregulating cyclin-dependentkinase (CDK) 2, CDK4 and CDK6, while activating PARP, caspase-3, caspase-9 and Bax, and downregulating Bcl-2.
SKLB70326 is a small molecule inhibitor of cell cycle progression, which has the activity of inducing G?/G? phase arrest and apoptosis in human hepatoma cells. SKLB70326 can inhibit the proliferation of human hepatoma cells, induce cell cycle arrest and apoptosis, and its mechanism is related to downregulating cyclin-dependentkinase (CDK) 2, CDK4 and CDK6, while activating PARP, caspase-3, caspase-9 and Bax, and downregulating Bcl-2.
Indirubin-5-sulfonate is a cyclin-dependentkinase (CDK) inhibitor, with IC50 values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, and CDK5/p35, respectively . Indirubin-5-sulfonate also shows inhibitory activity against GSK-3β .
AS2863619 free base enables conversion of antigen-specific effector/memory T cells into Foxp3 + regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 free base is a potent, orally active cyclin-dependentkinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 free base inhibition of CDK8/19, which consequently activates the Foxp3 gene .
CDK8-IN-6 (compound 9) is a potent cyclin-dependentkinase 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 .
CDK/HDAC-IN-4 is a high selective dual cyclin-dependentkinase (CDK)/histone deacetylase (HDAC) inhibitor with IC50 values of 88.4 and 168.9 nM, respectively. CDK/HDAC-IN-4 exhibits antiproliferative capacities against hematological and solid tumor cells. CDK/HDAC-IN-4 also induces MV-4-11 cell Apoptosis and S cell cycle arrests. CDK/HDAC-IN-4 possesses a significant antitumor potency in the MV-4-11 xenograft model .
Olomoucine is an ATP competitive inhibitor of CDKs. Olomoucine is a purine (HY-34431) derivative and inhibits CDC2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E (both IC50=7 μM), CDK/p35 kinase (IC50=3 μM) and ERK1/p44 MAP kinase (IC50=25 μM) . Olomoucine regulates cell cycle and shows anti-melanin tumor activity .
CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependentkinase (CDK) inhibitor (IC50 values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T, respectively). CGP60474 is a selective and ATP-competitive PKC inhibitor .
CDK8-IN-7 (compound 12) is a potent and selective cyclin-dependentkinase 8 (CDK8) inhibitor with an Kd of 3.5 nM. CDK8-IN-7 shows cytotoxicity for MOLM-13, OCI-AML3, MV4-11, NRK and H9c2 cells with IC50s of 5.9, 4.8, 5.4, 16.2, 12.5-25 µM, respectively. CDK8-IN-7 has the potential for the research of AML-cancer .
PROTAC FLT3/CDKs degrader-1 (Compound C3) is a degrader for cyclin-dependentkinases (DC50 is 18.73 nM for CDK2) and the FMS-like tyrosine kinase 3 (FLT3). PROTAC FLT3/CDKs degrader-1 induces differentation of HL-60 (72.77% differentation at 6.25 nM), inhibits proliferation of AML cells, with IC50s of 2.9-37 nM. PROTAC FLT3/CDKs degrader-1 is potential for ameliorating acute myeloid leukemia. (Pink: ligand for target protein FLT3/CDKs ligand-1 (HY-161709); Black: linker (HY-W012935); Black: ligand for E3 ligase Thalidomide 5-fluoride (HY-W087383))
CDK7/9-IN-1 is a cyclin-dependentkinases 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 .
3-Methylthienyl-carbonyl-JNJ-7706621 is a potent and selective inhibitor of cyclin-dependentkinase (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 .
Aloisine A (RP107) is a a potent cyclin-dependentkinase (CDK) inhibitor with IC50s of 0.15 μM, 0.12 μM, 0.4 μM, 0.16 μM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK5/p35, respectively. Aloisine A ininhibits GSK-3α (IC50=0.5 μM) and GSK-3β (IC50=1.5 μM). Aloisine A stimulates wild-type CFTR and mutated CFTR, with submicromolar affinity by a cAMP-independent mechanism. Aloisine A has the potential for CFTR-related diseases, including cystic fibrosis research .
Cdc2 kinase substrate is a biological active peptide. (The native peptide HATPPKKKRK is a substrate for cyclin-dependent protein kinase 1 (CDC2; CDK1).)
Vanicoside B is a phenylpropanoyl sucrose derivative, can be isolated from the herb Persicaria dissitiflora. Vanicoside B targets cyclin-dependentkinase 8 (CDK8) and exhibits anti-tumor activity. The potential mechanism is Vanicoside B blocks CDK8-mediated signaling pathways and decreases the expression of epithelial-mesenchymal transition proteins, so that it leads to cell cycle arrest and apoptosis .
CKS2 protein intricately binds to TEK/TIE2 to regulate ANGPT1 signaling. Its binding induces receptor tyrosine phosphorylation, affecting downstream cellular responses. CKS2 Protein, Human is the recombinant human-derived CKS2 protein, expressed by E. coli , with tag free. The total length of CKS2 Protein, Human is 79 a.a., .
CKS1 Protein is vital, binding to the catalytic subunit of cyclin-dependent kinases and serving as an essential factor for their biological function. Forming a homohexamer, CKS1's potential to bind six kinase subunits underscores intricate regulatory mechanisms. This highlights CKS1's importance in modulating cyclin-dependent kinase activity, emphasizing its crucial role in facilitating the proper functioning of these key cellular regulators. CKS1 Protein, Human is the recombinant human-derived CKS1 protein, expressed by E. coli , with tag free. The total length of CKS1 Protein, Human is 79 a.a., .
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