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Purvalanol B (NG 95) is a potent, selective, reversible and ATP-competitive inhibitor CDK, with IC50s of 6 nM, 6 nM, 9 nM, 6 nM for cdc2-cyclinB, CDK2-cyclin A, CDK2-cyclin E and CDK5-p35, respectively. Purvalanol B shows selectivity for CDK over a range of other protein kinases (IC50>1000 nM). Purvalanol B inhibits the growth a chloroquine-resistant strain of P. falciparum .
Alsterpaullone (9-Nitropaullone) is a potent CDK inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclinB, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to GSK-3alpha/GSK-3beta with IC50s of both 4 nM. Alsterpaullone has antitumor activity, and possesses potential for the study in neurodegenerative and proliferative disorders . Alsterpaullone induces apoptosis in leukemia cell line .
Purvalanol A is a potent CDK inhibitor, which inhibits cdc2-cyclinB, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1, and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, resepctively.
R547 is a potent, selective and orally active ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclinB, CDK2/cyclin E and CDK4/cyclin D1, respectively .
Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK) inhibitor, with IC50 values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1/cyclinB, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, and CDK5/p35, respectively . Indirubin-5-sulfonate also shows inhibitory activity against GSK-3β .
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 .
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 .
CDK2-IN-4 (compound 73) is a potent and selective CDK2 inhibitor with an IC50 of 44 nM for CDK2/cyclin A, shows 2,000-fold selectivity over CDK1/cyclinB (IC50=86 uM) .
Milciclib (PHA-848125) is a potent, ATP-competitive and dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC50s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclinB/CDK1 and TRKA, respectively.
(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/cyclinB, respectively. (S)-CR8 reduces SH-SY5Y cells survival (IC50 0.40 μM) .
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclinB1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclinB1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
Kenpaullone is a potent inhibitor of CDK1/cyclinB and GSK-3β, with IC50s of 0.4 μM and 23 nM, and also inhibits CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 with IC50s of 0.68 μM, 7.5 μM, 0.85 μM, respectively. Kenpaullone, a small molecule inhibitor of KLF4, reduces self-renewal of breast cancer stem cells and cell motility in vitro.
(R)-CR8 (CR8), a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 inhibits CDK1/cyclinB (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 induces apoptosis and has neuroprotective effect . (R)-CR8 acts as a molecular glue degrader that depletes cyclin K .
(R)-CR8 (CR8) trihydrochloride, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 trihydrochloride inhibits CDK1/cyclinB (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 . (R)-CR8 trihydrochloride acts as a molecular glue degrader that depletes cyclin K .
Olomoucine is an ATP competitive inhibitor of CDKs. Olomoucine is a purine (HY-34431) derivative and inhibits CDC2/cyclinB, 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 .
K00546 is a potent CDK1 and CDK2 inhibitor with IC50s of 0.6 nM and 0.5 nM for CDK1/cyclinB and CDK2/cyclin A, respectively. K00546 is also a potent CDC2-like kinase 1 (CLK1) and CLK3 inhibitor with IC50s of 8.9 nM and 29.2 nM, respectively .
MeBIO is a potent AhR (aryl hydrocarbon receptor) agonist, with IC50 of 44 μM (GSK-3) and 55 μM (CDK1/cyclinB), respectively. MeBIO is inactive on GSK-3β .
(E/Z)-BIO-acetoxime (GSK-3 Inhibitor X) is a potent and selective GSK-3α/β inhibitor, with an IC50 of 10 nM. (E/Z)-BIO-acetoxime shows more than 200-flod selectivity over CDK5/p25, CDK2/cyclin A and CDK1/cyclinB (IC50=2.4, 4.3, 63 μM) .
Cucurbitacin E is a natural compound which from Cucurbitaceae plants. Cucurbitacin E significantly suppresses the activity of the cyclinB1/CDC2 complex.
Aloisine A (RP107) is a a potent cyclin-dependent kinase (CDK) inhibitor with IC50s of 0.15 μM, 0.12 μM, 0.4 μM, 0.16 μM for CDK1/cyclinB, 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 .
H1k, a Eudistomin Y derivative, is a lysosome-targeted antiproliferation agent. H1k increases the autophagy signal and downregulate the expression of cyclin-dependent kinase (CDK1) and cyclinB1. H1k can be used in research of cancer .
TDZD-8 is an inhibitor of GSK-3β, with an IC50 of 2 μM; TDZD-8 shows less potent activities against Cdk-1/cyclinB, CK-II, PKA, and PKC, with all IC50s of >100 μM.
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/cyclinB 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 .
5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclinB inhibitor, competing with ATP for binding to the catalytic site of the kinase, with IC50s of 9, 20 and 25 nM, respectively .
(R)-DRF053 dihydrochloride is a potent casein kinases 1 (CK1), CDK1/cyclinB and CDK5/p25 inhibitor with IC50s of 14 nM, 220 nM and 80 nM, respectively. (R)-DRF053 dihydrochloride prevents the CK1-dependent production of amyloid-beta in a cell model .
NU6140 is a selective CDK2-cyclin A inhibitor (IC50, 0.41 μM), exhibits 10- to 36-fold selectivity over other CDKs . NU6140 also potently inhibits Aurora A and Aurora B, with IC50s of 67 and 35 nM, respectively . Enhances the apoptotic effect, with anti-cancer activity .
Indirubin-3'-monoxime is a potent GSK-3β inhibitor, and weakly inhibits 5-Lipoxygenase, with IC50s of 22 nM and 7.8-10 µM, respectively; Indirubin-3'-monoxime also shows inhibitory activities against CDK5/p25 and CDK1/cyclinB, with IC50s of 100 and 180 nM.
Ribociclib hydrochloride (LEE011 hydrochloride) 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 cyclinB/CDK1 complex.
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-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM .
Garcinone C, a xanthone derivative, is a natural compound extracted from Garcinia oblongifolia that is used as an anti-inflammatory, astringency and granulation-promoting medicine, and has potential cytotoxic effects on certain cancers. Garcinone C stimulates the expression levels of ATR and 4E-BP1, while efficiently inhibiting the expression levels of cyclinB1, cyclin D1, cyclin E2, cdc2, Stat3 and CDK7. Garcinone C significantly inhibits cell viability of the human Nasopharyngeal carcinoma (NPC) cell lines CNE1, CNE2, HK1 and HONE1 in a time‑ and dose‑dependent manner .
Mps1-IN-3 hydrochloride is a potent and selective Mps1 inhibitor with an IC50 value of 50 nM. Mps1-IN-3 hydrochloride can inhibit the proliferation of glioblastoma cells, and effectively sensitizes glioblastomas to Vincristine in orthotopic glioblastoma xenograft model .
Ribociclib (LEE01) 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 cyclinB/CDK1 complex .
Ribociclib succinate (LEE011 succinate) 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 cyclinB/CDK1 complex.
Ribociclib succinate hydrate (LEE011 succinate hydrate) 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 cyclinB/CDK1 complex.
Hygrolidin is a 16-membered macrolide antibiotic produced by Streptomyces hygroscopicus D-1166. Hygrolidin has anti-fungus activity against Valsa ceratosperma. Hygrolidin induces p21 expression and abrogates cell cycle progression at G1 and S phases. Hygrolidin has antitumor activity .
Vanicoside B is a phenylpropanoyl sucrose derivative, can be isolated from the herb Persicaria dissitiflora. Vanicoside B targets cyclin-dependent kinase 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 .
Aurora Kinases-IN-2 (compound 12Aj) is a potent Aurora kinases inhibitor with IC50 values of 90 and 152 nM for Aurora A and Aurora B. Aurora Kinases-IN-2 arrests cell cycle at G2/M phase by regulating cyclinB1 and cdc2. Aurora Kinases-IN-2 can be used for cancer research .
Ribociclib-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 cyclinB/CDK1 complex[1].
Ribociclib-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 cyclinB/CDK1 complex[1].
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-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM .
Ribociclib-d8 is the deuterium labeled Ribociclib[1]. Ribociclib (LEE01) 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 cyclinB/CDK1 complex[2].
Flubendazole is an anthelmintic drug based on altering microtubule structure, inhibition of tubulin polymerization and disruption of microtubule function. Flubendazole induces apoptosis in human colorectal cancer (CRC) by blocking the STAT3 signaling axis and activation of autophagy. Flubendazole induces P53 expression and reduced CyclinB1 and p-cdc2 expression. Flubendazole is an antitumor agent. Flubendazole can be used for worm and intestinal parasites .
CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent kinase (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 .
LG308 is a novel synthetic compound with antimicrotubule activity. LG308 induces mitotic phase arrest and inhibits G2/M progression significantly which is associated with the upregulation of cyclinB1 and mitotic marker MPM-2 and the dephosphorylation of cdc2. LG308 also induces apoptosis and cell death. LG308 significantly suppresses tumor growth. LG308 with antimitotic activity has the potential for the research of prostate cancer .
Tubulin polymerization-IN-11 is a potent tubulin polymerization inhibitor with an IC50 value of 3.4 µM. Tubulin polymerization-IN-11 shows antiproliferative activity. Tubulin polymerization-IN-11 induces Apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-11 decreases the expression of cyclinB1, p-cdc2, and Bcl-2 protein levels and increases the expression of cleaved PARP .
Rubone, a chalcone analog, is a modulator of miR-34a. Rubone upregulates miR-34a expression in a p53 dependent manner, downregulates the downstream target Bcl-2 and Cyclin D1 expression, and suppresses hepatocellular carcinoma (HCC) growth in vivo. Rubone enhances the anticancer effect of Paclitaxel (PTX; HY-B0015) in PTX-resistant prostate cancer cell lines by reversing the expression of miR-34a downstream targets .
Autophagy inducer 2 (Compound 11i) is a potent autophagy inducer. Autophagy inducer 2 exhibits apparent antiproliferative activity against the MCF-7 cell line with an IC50 value of 1.31 μM and remarkably inhibits the colony formation of the MCF-7 cells. Autophagy inducer 2 arrests the MCF-7 cells in the G2/M phase by regulating the cell-cycle-related proteins Cdk-1 and CyclinB1. Autophagy inducer 2 has the potential for the research of breast cancer .
p53 Activator 2 (compound 10ah) intercalats into DNA and results in significant DNA double-strand break.p53 Activator 2 increases the expression of p53, p-p53, CDK4, p21 to cause cell cycle arrest at G2/M phase.p53 Activator 2 induce apoptosis and significantly down-regulates the anti-apoptosis proteins Bcl-2, Bcl-xL and the levels of cyclinB1.p53 Activator 2 has anti-proliferation activity against MGC-803 cells, with an IC50 of 1.73 µM. p53 Activator 2 displays potent anticancer efficiency against MGC-803 xenograft tumors models .
Cucurbitacin E is a natural compound which from Cucurbitaceae plants. Cucurbitacin E significantly suppresses the activity of the cyclinB1/CDC2 complex.
Garcinone C, a xanthone derivative, is a natural compound extracted from Garcinia oblongifolia that is used as an anti-inflammatory, astringency and granulation-promoting medicine, and has potential cytotoxic effects on certain cancers. Garcinone C stimulates the expression levels of ATR and 4E-BP1, while efficiently inhibiting the expression levels of cyclinB1, cyclin D1, cyclin E2, cdc2, Stat3 and CDK7. Garcinone C significantly inhibits cell viability of the human Nasopharyngeal carcinoma (NPC) cell lines CNE1, CNE2, HK1 and HONE1 in a time‑ and dose‑dependent manner .
Hygrolidin is a 16-membered macrolide antibiotic produced by Streptomyces hygroscopicus D-1166. Hygrolidin has anti-fungus activity against Valsa ceratosperma. Hygrolidin induces p21 expression and abrogates cell cycle progression at G1 and S phases. Hygrolidin has antitumor activity .
Vanicoside B is a phenylpropanoyl sucrose derivative, can be isolated from the herb Persicaria dissitiflora. Vanicoside B targets cyclin-dependent kinase 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 .
Rubone, a chalcone analog, is a modulator of miR-34a. Rubone upregulates miR-34a expression in a p53 dependent manner, downregulates the downstream target Bcl-2 and Cyclin D1 expression, and suppresses hepatocellular carcinoma (HCC) growth in vivo. Rubone enhances the anticancer effect of Paclitaxel (PTX; HY-B0015) in PTX-resistant prostate cancer cell lines by reversing the expression of miR-34a downstream targets .
The CDKN1B protein is a key cell cycle regulator that inhibits CDK2 when bound to cyclin A, thereby inhibiting G1 phase progression. It exhibits significant inhibitory effects on cyclin E- and cyclin A-CDK2 complexes. CDKN1B Protein, Human (His) is the recombinant human-derived CDKN1B protein, expressed by E. coli , with N-6*His labeled tag. The total length of CDKN1B Protein, Human (His) is 198 a.a., with molecular weight of ~30.0 kDa.
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., .
The CDK6ic complex is an important serine/threonine protein kinase that regulates cell cycle progression and differentiation, promoting the G1/S transition by phosphorylating substrates such as pRB/RB1 and NPM1. It interacts with D-type G1 cyclins during interphase to form active pRB/RB1 kinase, which controls cell cycle entry. CDK6-CCND1 Heterodimer Protein, Human (Sf9) is a recombinant protein dimer complex containing human-derived CDK6-CCND1 Heterodimer protein, expressed by Sf9 insect cells , with tag free.
The CCND1 protein is a regulatory component of the cyclin D1-CDK4 complex that coordinates phosphorylation and RB family inhibition to regulate the G(1)/S transition. This promotes the dissociation of E2F from the RB/E2F complex and promotes the transcription of E2F target genes critical for G(1) phase progression. CCND1 Protein, Human (His) is the recombinant human-derived CCND1 protein, expressed by E. coli , with N-6*His labeled tag. The total length of CCND1 Protein, Human (His) is 295 a.a., with molecular weight of ~37.7 kDa.
Ribociclib-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 cyclinB/CDK1 complex[1].
Ribociclib-d8 is the deuterium labeled Ribociclib[1]. Ribociclib (LEE01) 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 cyclinB/CDK1 complex[2].
Ribociclib-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 cyclinB/CDK1 complex[1].
Cyclin B1 Antibody is a non-conjugated and Rabbit origined polyclonal antibody about 48 kDa, targeting to Cyclin B1. It can be used for WB,IHC-F,IHC-P,ICC/IF,ELISA assays with tag free, in the background of Human, Mouse, Rat.
Cyclin B1 Antibody (YA486) is a non-conjugated and Rabbit origined monoclonal antibody about 48 kDa, targeting to Cyclin B1. It can be used for WB,ICC/IF,IHC-P,IP assays with tag free, in the background of Human.
Phospho-Cyclin B1 (Ser126) Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 48 kDa, targeting to Phospho-Cyclin B1 (Ser126). It can be used for WB,IP assays with tag free, in the background of Human.
Cyclin B2 Antibody is an unconjugated, approximately 45 kDa, anti-Cyclin B2 monoclonal antibody. Cyclin B2 Antibody can be used for: WB, IHC-P, ICC/IF, IP expriments in human, mouse, rat background without labeling.
Cyclin D1 Antibody is a non-conjugated and Rabbit origined polyclonal antibody about 34 kDa, targeting to Cyclin D1. It can be used for WB,IHC-P,IP assays with tag free, in the background of Human, Mouse, Rat.
