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Arctiin is an orally active inhibitor of NF-κB. Arctiin suppresses cyclin D1 protein expression in human tumor cells. Arctiin also reduces malondialdehyde and pro-in ammatory cytokines levels. Arctiin can used in study glomerulonephritis .
(R)-CR8, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 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 induces apoptosis and has neuroprotective effect . (R)-CR8 acts as a molecular glue degrader that depletes cyclin K .
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 Cyclin B1 and p-cdc2 expression. Flubendazole is an antitumor agent. Flubendazole can be used for worm and intestinal parasites .
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, cyclin B/CDK1 and TRKA, respectively.
Kenpaullone is a potent inhibitor of CDK1/cyclin B 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.
Alsterpaullone (9-Nitropaullone) is a potent CDK inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, 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-cyclin B, 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/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively .
KB-0742 is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 has potent anti-tumor activity .
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclinT1-CDK9, cyclin B1-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.
Avotaciclib (BEY1107) is an orally active cyclin-dependent kinase 1 (CDK1) inhibitor. Avotaciclib can inhibit the proliferation and induce apoptosis of tumor cells. Avotaciclib can be used in the research of cancer such as pancreatic cancer and lung cancer .
DIF-3 is an orally active anticancer agent. DIF-3 reduces the expression levels of cyclin D1 and c-Myc by facilitating their degradation via activation of GSK-3β. DIF-3 inhibits Wnt/β-catenin signaling pathway-related proteins in cells. DIF-3 induces reactive oxygen species (ROS) and autophagy. DIF suppresses the growth of Trypanosoma. cruzi in HT1080 cells. DIF-3 exerts antitumor effects both in vitro and in vivo .
FN-1501 is a potent inhibitor of FLT3 and 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. FN-1501 has anticancer activity.
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/cyclin B (IC50=86 uM) .
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-cyclin B, 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 .
HQ461 is a molecular glue that promotes CDK12-DDB1 interaction to trigger cyclin K degradation. HQ461-mediated degradation of cyclin K impairs CDK12 function, resulting in decreased CDK12 substrate phosphorylation, downregulation of DNA damage response genes, and cell death .
Aminopurvalanol A is a potent, selective, and cell permeable inhibitor of Cyclins/Cdk complexes. Aminopurvalanol A preferentially targets the G2/M-phase transition inhibiting cancer cell differentiation. Aminopurvalanol A causes the inhibition of sperm fertilizing ability via the inhibition of physiological capacitation-dependent actin polymerization .
Arcyriaflavin A is an indolo[2,3-a]carbazole compound and also a cyclin D1/CDK4 inhibitor. Arcyriaflavin A exists in the marine ascidian Eudistoma sp. and the slime mold Arcyria denudata. Arcyriaflavin A is applicable to research related to colon cancer and lung cancer .
Eurycomalactone is an active quassinoid could be isolated from Eurycoma longifolia Jack. Eurycomalactone is a potent NF-κB inhibitor with an IC50 value of 0.5 μM. Eurycomalactone inhibits protein synthesis and depletes cyclin D1. Eurycomalactone enhances radiosensitivity through arrest cell cycle at G2/M phase and delayed DNA double-strand break repair. Eurycomalactone inhibits the activation of AKT/NF-κB signaling, induces apoptosis and enhances chemosensitivity to Cisplatin (HY-17394) .
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 .
BSJ-5-63 is a potent CDK12, CDK7, CDK9 PROTAC degrader. BSJ-5-63 BSJ-5-63 decreases the protein expression of CDK12, CDK7, CDK9, RNAPII, Cyclin K. BSJ-5-63 decreases the mRNA expression of BRCA1, BRCA2. BSJ-5-63 shows anticancer activity and has the potential for the research of prostate cancer (Pink: ligand for target protein (HY-150948); black: linker (HY-W140827); Blue: E3 ligase ligand (HY-112078)) .
Briciclib (ON 014185) is a eukaryotic translation initiation factor 4E (eIF4E) inhibitor. Briciclib exhibits broad-spectrum anti-cancer activity, including in mantle cell leukemia, breast cancer, gastric cancer, and esophageal cancer cells. Briciclib reduces the expression of cyclin D1 and c-Myc, and enhances the expression of P53 and Cleaved Caspase 3 pro-apoptotic proteins. Briciclib can be used for the study of hematological system tumors and solid tumors .
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 .
K00546 is a potent CDK1 and CDK2 inhibitor with IC50s of 0.6 nM and 0.5 nM for CDK1/cyclin B 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 .
dCeMM2 (Compound 2) is a molecular glue-type degrader that targets cyclin K. dCeMM2 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 molecular glue degrader. dCeMM4 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex .
LCH-7749944 (GNF-PF-2356) is a potent PAK4 inhibitor with an IC50 of 14.93 μM. LCH-7749944 effectively suppresses the proliferation of human gastric cancer cells through downregulation of PAK4/c-Src/EGFR/cyclin D1 pathway and induces apoptosis .
CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity .
(R)-CR8 (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 . (R)-CR8 trihydrochloride acts as a molecular glue degrader that depletes cyclin K .
Dehydrozingerone is a ginger-derived component and cyclin D1 inhibitor that downregulates cyclin D1 expression and induces cell cycle G1 phase arrest. Dehydrozingerone reduces the proliferative capacity of castration-resistant prostate cancer cells under in vitro conditions. Dehydrozingerone reduces subcutaneous tumor growth by inhibiting cell proliferation and angiogenesis. Dehydrozingerone exerts antibacterial and antifungal activities via its α,β-unsaturated carbonyl conjugated system. Dehydrozingerone can be used in studies related to castration-resistant prostate cancer, bacterial infections, and food spoilage fungal infections .
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) .
Cyclin K degrader 1 (compound 40) is an AT7519 (HY-50940) based Cyclin K degrader with DC50 of 21 nM. Cyclin K degrader 1 has an affinity for cyclin K that is ~500-fold higher than its affinity for CDK12 .
PP-C8 is a potent and selective PROTAC CDK12-Cyclin K degrader. PP-C8 induces CDK12-Cyclin K degradation with DC50s of 416 and 412 nM for CDK12 and Cyclin K, respectively. PP-C8 demonstrates profound synergistic antiproliferative effects with PARP inhibitor in triple-negative breast cancer (TNBC) .
dCeMM3 (Compound 3) is a molecular glue degrader. dCeMM3 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex .
Avotaciclib (BEY1107) trihydrochloride is an orally active cyclin-dependent kinase 1 (CDK1) inhibitor. Avotaciclib trihydrochloride can inhibit the proliferation and induce apoptosis of tumor cells. Avotaciclib trihydrochloride can be used in the research of cancer such as pancreatic cancer and lung cancer .
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) .
Cyclin A/B RxL-IN-1 is a inhibitor targeting the Cyclin A/B RxL interaction at the hydrophobic patch (HP). Cyclin A/B RxL-IN-1 inhibits Cyclin A with an IC50 of 0.12 μM. Cyclin A/B RxL-IN-1 demonstrates antitumor efficacy in mouse cell line-derived xenograft (CDX) models. CDK-IN-19 can be used for the study of E2F-driven cancers such as small-cell lung cancer (SCLC) .
LCAHA (LCA hydroxyamide) is a deubiquitinase USP2a inhibitor with IC50s of 9.7 μM and 3.7μM in Ub-AMC Assay and Di-Ub Assay, respectively. LCAHA destabilizes Cyclin D1 and induces G0/G1 arrest by inhibiting deubiquitinase USP2a .
CDK4 inhibitor is a novel and specific CDK4/Cyclin D1 inhibitor with an IC50 of 10 nM; 1500 and 500 fold than CDK1/Cyclin B (IC50>15 uM) and CDK2/Cyclin A (IC50=5.265 uM) respectively.
CDK2-IN-40 is a CDK2 (Cyclin dependent kinase 2) inhibitor, extracted from patent WO 2024/254245 A1 (Example 1). CDK2-IN-40 inhibits CDK2/Cyclin E1 with an IC50 of ≤ 10 nM .
PPA-037 TFA is an orally active, highly potent and selective inhibitor of cyclin-dependent kinase 12 (CDK12). PPA-037 TFA induces the degradation of cyclin K (Cyclin K), enhancing antiproliferative effects on tumor cells. PPA-037 TFA is promising for research of cancers .
SR-1277 is a potent, selective and ATP competitive CK1δ/ε inhibitor, with IC50s of 49 nM and 260 nM, respectively. SR-1277 also inhibits FLT3, CDK4/cyclin D1, CDK6/cyclin D3 and CDK9/cyclin K, with IC50s of 305 nM, 1340 nM, 311 nM and 109 nM, respectively. SR-1277 can be used for the research of cancer .
β-catenin-IN-4 (Compound 39) is a β-catenin inhibitor with a Ki of 0.64 μM. β-catenin-IN-4 reduces the protein expression levels of cyclin D1 and c-Myc .
Avotaciclib (BEY1107) hydrochloride is an orally active cyclin-dependent kinase 1 (CDK1) inhibitor. Avotaciclib hydrochloride can inhibit the proliferation and induce apoptosis of tumor cells. Avotaciclib hydrochloride can be used in the research of cancer such as pancreatic cancer and lung cancer .
Cyclin K degrader 2 is a molecular glucose degrading agent that targets the cyclin K protein. Cyclin K degrader 2 has inhibitory activity against CDK1 and CDK9. Cyclin K degrader 2 causes a decrease in RNA polymerase II Ser2 phosphorylation levels, downregulation of DNA damage response gene expression, accumulation of DNA damage, G1 phase arrest of the cell cycle, and apoptosis. Cyclin K degrader 2 can be used for cancer research .
TR-213 is a potent molecular glue degrader that targets Cyclin K (CDK). TR-213 induces 91% and 56% decrease in CDK12 and Cyclin at 1 μM. TR-213 can inhibit RNA polymerase II activity and regulates alternative polyadenylation (APA) activity. TR-213 can be used for the research of cancer .
CDK-IN-9 (compound 24) is a potent CDK inhibitor, also as a molecular glue inducing an interaction between CDK12 and DDB1, with an IC50 values of 4 nM for CDK2/E. CDK-IN-9 leads to polyubiquitination of cyclin K and its subsequent degradation. CDK-IN-9 induce apoptosis through dephosphorylation of retinoblastoma protein and RNA polymerase II .
Olomoucine II is a potent CDK inhibitor with IC50 values of 0.06, 0.1, 0.45, 7.6, 19.8 µM for CDK9/cyclin T, CDK2/cyclin E, CDK7/cyclin H, CDK1/cyclin B, CDK4/cyclin D1, respectively. Olomoucine II shows antiproliferative activity .
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 .
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 cyclin B1, p-cdc2, and Bcl-2 protein levels and increases the expression of cleaved PARP .
(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) .
Bohemine is a purine analogue and is a synthetic and selective CDK inhibitor with IC50s of 4.6 μM, 83 μM, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. Bohemine also inhibits ERK2 with an IC50 of 52 μM and has less inhibitory effect on CDK1, CDK4 and CDK6. Bohemine has a broad spectrum anti-cancer activities .
Flubendazole (Standard) is the analytical standard of Flubendazole. This product is intended for research and analytical applications. 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 Cyclin B1 and p-cdc2 expression. Flubendazole is an antitumor agent. Flubendazole can be used for worm and intestinal parasites .
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/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 .
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 .
CDK12-Cyclin K ligand-1 is a ligand of PROTAC degrader that binds to the E3 ligase. CDK12-Cyclin K ligand-1 can be used in the synthesis of PROTAC degrader such as PP-C8 (HY-144691) .
CDK12-Cyclin K Ligand-Linker Conjugates 1 is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for CDK12-Cyclin K (HY-176790) and a PROTAC linker (HY-W244922), which recruits E3 ligases. CDK12-Cyclin K Ligand-Linker Conjugates 1 can be used for synthesis of PROTAC PP-C8 (HY-144691) .
PPA-037 is an orally active, highly potent and selective inhibitor of cyclin-dependent kinase 12 (CDK12). PPA-037 induces the degradation of cyclin K (Cyclin K), enhancing antiproliferative effects on tumor cells. PPA-037 is promising for research of cancers .
CDK9 degrader-1 (Compound AZ-9) is a selective CDK9 degrader (DC50: 0.4073 µM). CDK9 degrader-1 recruits ATG101 to initiate the autophagy-lysosome pathway and forms autophagosomes by recruiting LC3, which then fuses with lysosomes to degrade CDK9 and its partner protein Cyclin T1 (DC50: 1.215 µM). CDK9 degrader-1 induces caspase 3-mediated apoptosis. CDK9 degrader-1 has antitumor activity in a mouse HCT116 xenograft model .
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/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 .
PF-06842874 is a CDK4/Cyclin D1 and CDK6/Cyclin D3 inhibitor (Ki values are 62 and 130 nM, respectively). PF-06842874 can be used in the research of pulmonary arterial hypertension and cancer .
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 .
KB-0742 hydrochloride is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 hydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 hydrochloride has potent anti-tumor activity .
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) .
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).
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 cyclin B1. H1k can be used in research of cancer .
Aurora kinase-IN-1 (Compound 9) is a potent inhibitor of aurora kinase. Aurora kinase-IN-1 upregulates the expression of G1 cell cycle inhibitory proteins including p21 and p27, and G1 progressive cyclin D1, and downregulates G1-to-S progressive cyclins, resulting in cell cycle arrest at the G1/S boundary. Aurora kinase-IN-1 also induces apoptosis. Aurora kinase-IN-1 is a lead compound for chemotherapeutic agents .
Anticancer agent 50 (compound 6) is a potent ABCB1 efflux pump modulator. Anticancer agent 50 shows cytotoxic effects and antiproliferative effects. Anticancer agent 50 decreases the expression of cyclin D1 and induces p53 expression. Anticancer agent 50 has the potential for the research of T-lymphoma .
XH161-180 is a potent and orally active ubiquitin carboxyl-terminal hydrolase 2 (USP2) inhibitor. XH161-180 decreases the protein of cyclin D and ACE2. XH161-180 shows antiproliferative activity. XH161-180 has the potential for the research of cancer and virus infection depending on ACE2 .
Arctiin (Standard) is the analytical standard of Arctiin. This product is intended for research and analytical applications. Arctiin is an orally active inhibitor of NF-κB. Arctiin suppresses cyclin D1 protein expression in human tumor cells. Arctiin also reduces malondialdehyde and pro-in?ammatory cytokines levels. Arctiin can used in study glomerulonephritis .
Purvalanol A (Standard) is the analytical standard of Purvalanol A. This product is intended for research and analytical applications. Purvalanol A is a potent CDK inhibitor, which inhibits cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1, and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, resepctively.
R547 mesylate is a potent, selective and orally active ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively .
HJC0416 is a potent and orally active STAT3 inhibitor. HJC0416 shows antiprolifeative activity and induces Apoptosis. HJC0416 decreases the expression of p-STAT3 (Tyr-705), Cyclin D1 and increases the expression of cleaved caspase-3 protein. HJC0416 shows anti-tumor activity .
Avotaciclib (BEY1107) sulfate is an orally active cyclin-dependent kinase 1 (CDK1) inhibitor. Avotaciclib sulfate can inhibit the proliferation and induce apoptosis of tumor cells. Avotaciclib sulfate can be used in the research of cancer such as pancreatic cancer and lung cancer .
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 cyclin B1 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 .
SLM6 is a sangivamycin-like molecule. SLM6 is a CDK9 inhibitor. SLM6 inhibits CDK9/cyclin K and CDK9/cyclin T1 kinase activity with IC50s of 280 nM and 133 nM, respectively. SLM6 also inhibits CDK1/cyclin B and CDK2/
cyclin A with IC50s of less than 300 nM. SLM6 induces apoptosis in multiple myeloma (MM) cells .
Adamantane-Butyl alcohol is a selective and persistent degrader targeting the CDK8-cyclin C complex. Adamantane-Butyl alcohol is the linker for LL-K8-22 (PROTACCDK8-cyclin C, HY-149209) and HyT .
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 Cyclin B1. Autophagy inducer 2 has the potential for the research of breast cancer .
Milciclib (Standard) is the analytical standard of Milciclib. This product is intended for research and analytical applications. 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, cyclin B/CDK1 and TRKA, respectively.
2-Cyanoethylalsterpaullone (compound 7) is an Alsterpaullone (HY-108359) derivative, which exhibits potent and selective inhibitory activities against CDK1/Cyclin B and GSK-3β (GSK-3β: IC50=0.8 nM; CDK1/Cyclin B: IC50=0.23 nM) .
CIRc-014 is an orally active Cyclin A/B inhibitor with a Cyclin A IC50 of 0.05 μM, Cyclin A Kd of 2.7 nM, Cyclin B IC50 of less than 0.02 μM and Cyclin B Kd of 1.0 nM. CIRc-014 activates the spindle assembly checkpoint and promotes the formation of a complex between Cyclin B and CDK2 by blocking the RxL interaction of Cyclin A/B. CIRc-014 can induce replication stress, DNA damage, mitotic arrest and apoptosis in tumor cells. CIRc-014 showed tumor growth inhibition and regression in NCI-H69 and NCI-H446 small cell lung cancer xenograft models. CIRc-014 can be used for the research of small-cell lung cancer .
CID-078 is an orally active macrocyclic cyclin A and cyclin B inhibitor. CID-078 binds cyclin hydrophobic patches, disrupting interactions of cyclin A-Cdk2 with E2F1 and cyclin B-Cdk1 with Myt1, and selectively targets RxL binding motifs to block complex-substrate interactions. CID-078 induces DNA damage, G2/M cell cycle arrest, apoptosis, mitotic catastrophe, spindle assembly checkpoint activation, and neomorphic cyclin B-CDK2 complex formation, driving synthetic lethality in E2F-driven cancer cells. CID-078 can be used for the research of small cell lung cancer, non-small cell lung cancer, triple negative breast cancer, advanced solid tumors, luminal HR +/HER 2- breast cancer, RB1-altered solid tumors, and neuroblastoma .
Methoxyfenoterol is a β2-adrenergic receptor agonist. Methoxyfenoterol stimulates intracellular cAMP accumulation, inhibits tumor cell proliferation, induces G1 cell cycle arrest, upregulates cyclin-dependent kinase inhibitor p27, downregulates cyclin D1 and cyclin A, and inhibits Akt phosphorylation. Methoxyfenoterol crosses the blood-brain barrier and inhibits growth of astrocytoma xenografts. Methoxyfenoterol can be used for the research of astrocytoma, glioblastoma .
Anticancer agent 302 (Example 1) is an anticancer agent. Anticancer agent 302 has a DC50 value of 199 nM for Cyclin E1 and an IC50 value of 133 nM for pRB. Anticancer agent 302 can be used for tumor research .
GTGKT is a CAGE inhibitor. GTGKT binds to CAGE and blocks the binding of CAGE to GSK3β. GTGKT alters the localization of CAGE and inhibits the binding of CAGE to the promoter sequence of Cyclin D1. GTGKT enhances the Apoptotic effect of anticancer agents. GTGKT reduces the expression of Cyclin D1. GTGKT decreases the tumorigenic potential of melanoma and hepatocellular carcinoma cells .
GIT1-IN-1 is an inhibitor of ARF GTPase-activating protein 1 (GIT1) with a KD of 6.2 μM. GIT1-IN-1 induces apoptosis (apoptosis) in liver and colon cancer cells, arrests the cell cycle at the G2/M phase, and inhibits cell proliferation, colony formation and migration. GIT1-IN-1 inhibits the activities of MEK and ERK, reduces the expression level of cyclin D1, and stabilizes cyclin B1 protein in liver and colon cancer cells. GIT1-IN-1 can be used in the research of liver cancer and colon cancer .
AG-12286 is a pan-CDK inhibitor with an IC50 value of 2 nM against cdk1/cyclin B, 6 nM against cdk2/cyclin E, and 12 nM against cdk4/cyclin D. AG-12286 is 1000-fold more selective for the CDK family than for PKC. AG-12286 can be used in cancer research .
R547 (Standard) is the analytical standard of R547 (HY-10014). This product is intended for research and analytical applications. R547 is a potent, selective and orally active ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively .
Aminopurvalanol A (Standard) is the analytical standard of Aminopurvalanol A (HY-104013). This product is intended for research and analytical applications. Aminopurvalanol A is a potent, selective, and cell permeable inhibitor of Cyclins/Cdk complexes. Aminopurvalanol A preferentially targets the G2/M-phase transition inhibiting cancer cell differentiation. Aminopurvalanol A causes the inhibition of sperm fertilizing ability via the inhibition of physiological capacitation-dependent actin polymerization .
IHMT-15137 is a BMX inhibitor with an IC50 of 26.97 nM. IHMT-15137 covalently binds to BMX Cys496 within the ATP-binding pocket, inhibits BMX phosphorylation at Tyr566, and disrupts the BMX-ERK1/2-Cyclin D1/CDK4/6-E2F1 signaling axis. IHMT-15137 reduces E2F1 protein stability via decreased Ser332/337 phosphorylation, increased ubiquitination, and ubiquitin-proteasome pathway degradation. IHMT-15137 induces cell cycle arrest, apoptosis, DNA damage, and suppresses cell migration and invasion. IHMT-15137 can be used for the research of small cell lung cancer .
Briciclib (ON 014185) sodium is a eukaryotic translation initiation factor 4E (eIF4E) inhibitor. Briciclib sodium exhibits broad-spectrum anti-cancer activity, including in mantle cell leukemia, breast cancer, gastric cancer, and esophageal cancer cells. Briciclib sodium reduces the expression of cyclin D1 and c-Myc, and enhances the expression of P53 and Cleaved Caspase 3 pro-apoptotic proteins. Briciclib sodium can be used for the study of hematological system tumors and solid tumors .
TZ1104 is a PROTAC-based CDK7 degrader, with a DC50 of 0.88 nM. TZ1104 forms a ternary complex with VHL E3 ligase and CDK7 to trigger proteasome-dependent CDK7 degradation, destabilizing the CDK7-cyclin H-MAT1 complex. TZ1104 suppresses phosphorylation of RNA polymerase II CTD Ser5, CDK1 Thr161, and CDK2 Thr160. TZ1104 activates the p53-p21 axis and suppresses oncogenic Myc signaling. TZ1104 induces cell cycle arrest, apoptosis, and differentiation of acute leukemia cells. TZ1104 can be used for the research of acute leukemia .
Americanin A is a Neolignan. Americanin A can be isolated from the seeds of Phytolacca americana. Americanin A activates ATM and ATR, initiating the subsequent signal transduction cascades that include Chk1, Chk2, and tumor suppressor p53. Americanin A targets selectively Skp2 for degradation and thereby stabilizes p27. Americanin A suppresses the activity of Cyclin B1 and its partner cdc2 to prevent entry into Mitosis. Americanin A induces Apoptosis by producing excessive ROS. Americanin A has anti-cancer activity against colorectal cancer .
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclinT1-CDK9, cyclin B1-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.
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).
GSK-3β inhibitor 28 is selective and non-competitivea glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 14.82 nM. GSK-3β inhibitor 28 can upregulate the expression level of phosphorylated GSK-3β and downregulate the expression of p-NF-κB, P65, C-myc and Cyclin D1. GSK-3β inhibitor 28 can induce cells apoptosis, G1 phase arrest and inhibit migration. GSK-3β inhibitor 28 can be used for the research of cancer, such as colorectal cancer .
(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/cyclin B (IC50=2.4, 4.3, 63 μM) .
(E)-MS0019266 is a potent inhibitor of DNA damage repair. (E)-MS0019266 inhibits ribonucleotide reductase by generating reactive oxygen species. (E)-MS0019266 also reduces expression of genes related to cell cycle arrest and mitosis, including polo-like kinase 1, kinesin family member 20a, cyclin B1 and aurora kinase A. (E)-MS0019266 is promising for research of inhibitors of ribonucleotide reductase and polo-like kinase 1 .
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-dependent kinase 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 .
PP5-IN-2 is an orally active and selective protein phosphatase 5 (PP5) inhibitor with an IC50 value of 0.9 μM. PP5-IN-2 activates p53 and downregulates cyclin D1 and MGMT, which shows potency in cell cycle arrest and reverses Temozolomide (TMZ) (HY-17364) resistance in the U87 MG cell line. PP5-IN-2 effectively inhibits tumor growth in the xenograft mouse model .
GP-82996 (CINK4) is a pharmacological inhibitor of CDK4/6. GP-82996 has IC50s of 1.5, 5.6 and 25 μM for CDK4/cyclin D1, CDK6/cyclin D1 and Cdk5/p35, respectively. GP-82996 induces the apoptosis of cancer cells U2OS. GP-82996 can be used in the research of cancer .
PNU-292137 is an orally active, potent CDK2 inhibitor with IC50s of 37 nM and 92 nM for CDK2/cyclin A and CDK2/cyclin E, respectively. PNU-292137 makes interactions with the hydrophobic pocket at the back of the CDK2 ATP pocket. PNU-292137 efficiently inhibits tumor cell proliferation in human colon and prostate tumor cell lines. PNU-292137 exhibits antitumor activity (TGI>50%) in a mouse xenograft model .
DCB-3503 is an allosteric modulator of heat shock cognate protein HSC70 and an inhibitor of Cyclin D1. DCB-3503 inhibits Cyclin D1 translation by allosterically modulating the ATPase and chaperone activities of HSC70. DCB-3503 may inhibit malignancies such as hepatocellular carcinoma or breast cancer with elevated expression of cyclin D1 .
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 .
GAK-IN-3 is a cyclin G-associated kinase (GAK) inhibitor with an IC50 of 207 nM and a Ki of 66 nM. GAK-IN-3 inhibits kinase activity in the nanomolar range by binding to GAK’s ATP-binding site. GAK-IN-3 acts as a cytotoxic agent that reduces viability of Ewing sarcoma cells. GAK-IN-3 can be used for the research of ewing sarcoma .
K00546 (Standard) is the analytical standard of K00546 (HY-103647). This product is intended for research and analytical applications. K00546 is a potent CDK1 and CDK2 inhibitor with IC50s of 0.6 nM and 0.5 nM for CDK1/cyclin B 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 .
CGP-74514 hydrochloride is a highly selective cyclin-dependent kinase 1 (CDK1) inhibitor (IC50: 25 nM). CGP-74514 hydrochloride inhibits CDK1/cyclin B complex activity, arrests the cell cycle at G2/M phase and induces tumor cell apoptosis. CGP-74514 hydrochloride is promising for research of bladder cancer .
CA224 (Compound 1) is a selective and orally active Cdk4–cyclin D1 inhibitor with an IC50 of 6.2 µM. CA224 induces cell apoptosis and shows antitumor activity .
Riviciclib (P276-00 free base) is a potent cyclin-dependent kinase (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 .
CGP-74514 dihydrochloride is a highly selective cyclin-dependent kinase 1 (CDK1) inhibitor (IC50=25 nM). CGP-74514 dihydrochloride inhibits CDK1/cyclin B complex activity, arrests the cell cycle at G2/M phase and induces tumor cell apoptosis. CGP-74514 dihydrochloride is promising for research of bladder cancer .
BMT-090605 hydrochloride is a potent, selective the adapter protein-2 associated kinase 1 (AAK1) inhibitor with an IC50 value of 0.6 nM. BMT-090605 hydrochloride shows antinociceptive activity. BMT-090605 hydrochloride inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50 values of 45 nM and 60 nM, respectively. BMT-090605 hydrochloride can be used for the research of neuropathic pain .
BMT-090605 is a potent, selective the adapter protein-2 associated kinase 1 (AAK1) inhibitor with an IC50 value of 0.6 nM. BMT-090605 shows antinociceptive activity. BMT-090605 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50 values of 45 nM and 60 nM, respectively. BMT-090605 can be used for the research of neuropathic pain .
Riviciclib hydrochloride (P276-00) is a potent cyclin-dependent kinase (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 .
CGP-74514 (Compound 13) is a highly selective cyclin-dependent kinase 1 (CDK1) inhibitor (IC50=25 nM). CGP-74514 inhibits CDK1/cyclin B complex activity, arrests the cell cycle at G2/M phase and induces tumor cell apoptosis. CGP-74514 is promising for research of bladder cancer .
CDK9-IN-35 (compound 10j) is an inhibitor of CDK9/Cyclin T1 with an IC50 value of 10.2 nM and against the HCT-116 cell line with an IC50 value of 20 nM .
NSC 625987 is a specific and high-affinity CDK4 inhibitor with an IC50 of 0.2 μM for CDK4:cyclin D1. NSC 625987 shows >500-fold selectivity for CDK4 over CDK2 .
CDK1 is a cyclin-dependent kinase that functions as a serine/threonine protein kinase, and is a key player in cell cycle regulation. CDK1/CycB1 Recombinant Human Active Protein Kinase is an ortholog of CDK1. CDK1/cyclin B1 complexes initiates mitotic entry by phosphorylating a multitude of proteins to condense chromosomes, disrupt the nuclear envelope, and enable microtubules polymerization to attach and to segregate the chromosomes .
Contragestazol (DL111-IT) is a non-hormonal antifertility agent. Contragestazol reduces the expression of Cyclin D1 and CDK4, increases the expression of total retinoblastoma protein (pRb), and decreases the level of hyperphosphorylated pRb. Contragestazol induces G0/G1 phase cell cycle arrest. Contragestazol inhibits embryonic development by inducing luteal cell apoptosis and reducing intrauterine polyamine levels. Contragestazol exhibits antitumor activity against prostate cancer, S180 tumor and H22 tumor. Contragestazol shows extremely potent activity in terminating early pregnancy in animals .
Cdk1/2 Inhibitor III (compound 3n) is a highly potent and selective Cdk1/cyclin B and Cdk2/cyclin A inhibitor of with IC50s of 0.6 nM and 0.5 nM, respectively. Cdk1/2 Inhibitor III shows selectivity over VEGF-R2 (IC50 of 32 nM), GSK-3β (IC50 of 140 nM), and a other kinases. Cdk1/2 Inhibitor III inhibits in cell proliferation with IC50s of 20 nM, 35 nM and 92 nM for HCT-116, HeLa, and A375 cells, respectively .
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 cyclin B1.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 .
CDK4 has a well-established role in cell-cycle controland CDK4-cyclin complexes are commonly deregulated in tumorigenesis. CDK4/CycD1 Recombinant Human Active Protein Kinase is an ortholog of CDK4 .
CDK4 has a well-established role in cell-cycle controland CDK4-cyclin complexes are commonly deregulated in tumorigenesis. CDK4/CycD3 Recombinant Human Active Protein Kinase is an ortholog of CDK4 .
CDK4 has a well-established role in cell-cycle controland CDK4-cyclin complexes are commonly deregulated in tumorigenesis. CDK4/CycD2 Recombinant Human Active Protein Kinase is an ortholog of CDK4 .
TDZD-8 is an inhibitor of GSK-3β, with an IC50 of 2 μM; TDZD-8 shows less potent activities against Cdk-1/cyclin B, CK-II, PKA, and PKC, with all IC50s of >100 μM.
CDK4/6-IN-9 (compound 10) is a selective CDK4/6 inhibitor with an IC50 of 905 nM for CDK6/cyclin D1. CDK4/6-IN-9 has the potential for multiple myeloma (MM) research .
MeBIO (Standard) is the analytical standard of MeBIO (HY-103221). This product is intended for research and analytical applications. MeBIO is a potent AhR (aryl hydrocarbon receptor) agonist, with IC50 of 44 μM (GSK-3) and 55 μM (CDK1/cyclin B), respectively .
CDK-IN-16 (Compound 5g) is a CDK2/cyclin A2 inhibitor with an IC50 of 1.67 μM. CDK-IN-16 exhibits anticancer activity. The IC50 of CDK-IN-16 against the AGS cell line is 3.5 μM .
Eriocitrin is a flavonoid isolated from lemons that is a powerful antioxidant. Eriocitrin inhibits the proliferation of liver cancer cells by arresting the cell cycle in the S phase by upregulating p53, cyclin A, cyclin D3 and CDK6. Eriocitrin triggers apoptosis by activating intrinsic signaling pathways involving mitochondria .
MNK1/2-IN-11 is a potent, selective and orally active MNK1/2 inhibitor with MNK1IC50 of 1.2 nM, MNK2IC50 of 1.3 nM. MNK1/2-IN-11 reduces eukaryotic translation initiation factor 4E phosphorylation, decreases Mcl-1 and Cyclin D1 expression. MNK1/2-IN-11 inhibits tumor growth in mouse CT26 colorectal tumor models. MNK1/2-IN-11 can be used for the research of colorectal cancer .
BMT-090605 (hydrochloride) (Standard) is the analytical standard of BMT-090605 (hydrochloride) (HY-101290A). This product is intended for research and analytical applications. BMT-090605 hydrochloride is a potent, selective the adapter protein-2 associated kinase 1 (AAK1) inhibitor with an IC50 value of 0.6 nM. BMT-090605 hydrochloride shows antinociceptive activity. BMT-090605 hydrochloride inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50 values of 45 nM and 60 nM, respectively. BMT-090605 hydrochloride can be used for the research of neuropathic pain .
PI3Kα-IN-33 is an orally active and selective PI3Kα inhibitor with an IC50 of 9.9 nM. PI3Kα-IN-33 blocks the PI3K/Akt/mTOR signaling pathway. PI3Kα-IN-33 induces apoptosis and triggers G2/M-phase arrest via Cyclin B1 and CDK1 downregulation. PI3Kα-IN-33 can be used for the research of colorectal cancer .
5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase, with IC50s of 9, 20 and 25 nM, respectively .
ABC1183 is an orally active selective dual GSK3 and CDK9 inhibitor. ABC1183 inhibits GSK3β, GSK3α and CDK9/cyclin T1 with the IC50 values of 657 nM, 327 nM and 321 nM, respectively. ABC1183 has anti-inflammatory and anti-tumor activities .
FOXM1-IN-4 is a selective 5-HT7 receptor inhibitor with a Ki of 92 nM. FOXM1-IN-4 blocks 5-HT7 receptor signaling to reduce FOXM1, p-FOXM1, cyclin B1, and cdc25B levels. FOXM1-IN-4 acts as an antiproliferative, clonogenic inhibitor, and cell cycle inhibitor that induces G2/M arrest, reduces G0/G1 population. FOXM1-IN-4 can be used for the research of triple-negative breast cancer .
KGA-4066 is a novel non-ATP-competitive CDK2 inhibitor. KGA-4066 inhibits CDK2/Cyclin A2 with an IC50 value of 236.7 nM, disrupts their interaction, promots CDK2 degradation via the lysosomal pathway. KGA-4066 has anticancer activity against hepatocellular carcinoma .
(S)-(-)-Perillyl alcohol, a monoterpene, is an orally active farnesyl transferase and geranylgeranyl transferase inhibitor. (S)-(-)-Perillyl alcohol up-regulates the mannose-6-phosphate receptor, facilitating TGF-β1 activation and cytostasis,. (S)-(-)-Perillyl alcohol induces apoptosis in cancer cells, modulates cyclin D1 and AP-1 activity. (S)-(-)-Perillyl alcohol exhibits antitumor activity against sarcoma tumors in mice. (S)-(-)-Perillyl alcohol can be used for the research of squamous cell carcinoma of the esophagus and sarcoma 180 .
LL-K9-3 is a potent small-molecule degrader of CDK9-cyclin T1. LL-K9-3 has anti-proliferative and pro-apoptotic activities and suppresses downstream signaling of CDK9 and AR. Moreover, LL-K9-3 inhibits AR and Myc-driven oncogenic transcriptional programs .
NSC 625987 (Standard) is the analytical standard of NSC 625987 (HY-103380). This product is intended for research and analytical applications. NSC 625987 is a specific and high-affinity CDK4 inhibitor with an IC50 of 0.2 μM for CDK4:cyclin D1. NSC 625987 shows >500-fold selectivity for CDK4 over CDK2 .
(R)-DRF053 dihydrochloride is a potent casein kinases 1 (CK1), CDK1/cyclin B 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 .
FOXM1-IN-4 hydrochloride is a selective 5-HT7 receptor inhibitor with a Ki of 92 nM. FOXM1-IN-4 hydrochloride blocks 5-HT7 receptor signaling to reduce FOXM1, p-FOXM1, cyclin B1, and cdc25B levels. FOXM1-IN-4 hydrochloride acts as an antiproliferative, clonogenic inhibitor, and cell cycle inhibitor that induces G2/M arrest, reduces G0/G1 population. FOXM1-IN-4 hydrochloride can be used for the research of triple-negative breast cancer .
Thio-acridone (SACD) is a photosensitizer (HAF-PSs). Thio-acridone forms a long-lived triplet state upon excitation by 470 nm visible light,, ultimately generating singlet oxygen to damage the structures and functions of target cells such as cancer cells. Thio-acridone is promising for research of cancers . Thio-acridone is a CDK4/Cyclin D1 inhibitor (IC50 = 2 uM) .
Eriocitrin (Standard) is the analytical standard of Eriocitrin. This product is intended for research and analytical applications. Eriocitrin is a flavonoid isolated from lemons that is a powerful antioxidant. Eriocitrin inhibits the proliferation of liver cancer cells by arresting the cell cycle in the S phase by upregulating p53, cyclin A, cyclin D3 and CDK6. Eriocitrin triggers apoptosis by activating intrinsic signaling pathways involving mitochondria .
CDK20 is a major controller of cell cycle checkpoints, which regulate cell growth and proliferation and perform a role in the development of many malignancies. CDK20 is thought to have Cyclin-dependent activating kinase (CAK) activity for CDK2 when it is complexed with Cyclin H. CDK20/CycT1 Recombinant Human Active Protein Kinase is an ortholog of CDK20 .
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 .
ZM484 is a potent dual p53-MDM2/TOP1 inhibitor that exhibits antiproliferative and antitumor activity both in vitro and in vivo. ZM484 effectively upregulates p53 and MDM2 proteins and maintains TOP1 inhibitory activity by the release of camptothecin (CPT) and a potent p53-MDM2 inhibitor. ZM484 induces cell cycle arrest and apoptosis by regulating the expression of key apoptosis- and cycle-related proteins, including caspase-3, Bcl-2, and Cyclin B1. ZM484 can be used for colorectal cancer research .
TDZD-8 (Standard) is the analytical standard of TDZD-8. This product is intended for research and analytical applications. TDZD-8 is an inhibitor of GSK-3β, with an IC50 of 2 μM; TDZD-8 shows less potent activities against Cdk-1/cyclin B, CK-II, PKA, and PKC, with all IC50s of >100 μM.
A-800141 is an orally active, selective, sulfonamide-based MetAP2 inhibitor (IC50=12 nM) that binds reversibly to MetAP2 and interacts with its manganese ions. A-800141 induces the production of N-terminal methionine-unprocessed GAPDH variants, which in turn triggers G1-phase cell cycle arrest, elevates p21 levels, and reduces the levels of phosphorylated Rb and total cyclin A. A-800141 exhibits anti-angiogenic and tumor growth inhibitory effects, and produces synergistic effects when combined with cytotoxic inhibitors or BCL-2 inhibitors. A-800141 has been widely used in scientific research related to B-cell lymphoma, neuroblastoma, prostate cancer, colon cancer, melanoma and other fields .
Antitumor agent-174 (Compound 10) directly engages the N-terminal site of Hsp90 and promotes the degradation of β-catenin, thereby suppressing the Wnt/β-catenin signaling. Antitumor agent-174 effectively inhibits proliferation, induce S and G2/M phases arrest and block the clonogenic ability in CRC cells. Antitumor agent-174 down-regulates CDK1, Cyclin D1, c-Myc, Cyclin B1, and Cyclin A2, and upregulaties P21 proteins. Antitumor agent-174 has significant anti-tumor efficacy against colorectal cancer (CRC) with excellent pharmacokinetics and low toxicity .
CDK20 is a major controller of cell cycle checkpoints, which regulate cell growth and proliferation and perform a role in the development of many malignancies. CDK20 is thought to have Cyclin-dependent activating kinase (CAK) activity for CDK2 when it is complexed with Cyclin H. CDK20/CycH Recombinant Human Active Protein Kinase can be used to study the function of CDK20/CycH .
Garcinone D is an activator of the STAT3/Cyclin D1 and Nrf2/HO-1 pathways, and an inhibitor of CDK2/CyclinE1 (IC50 for CDK2/CyclinE1 is 28.23 μM). Garcinone D promotes neural stem cell proliferation by activating STAT3 phosphorylation and Cyclin D1 expression and enhancing the Nrf2/HO-1 signaling pathway. In addition, Garcinone D blocks the tumor cell cycle by inhibiting CDK2/CyclinE1. Garcinone D can promote the proliferation of C17.2 neural stem cells and inhibit prostate and breast cancer .
CDK2-IN-50 is a CDK2 inhibitor (IC50 = 0.77 nM). CDK2-IN-50 can induce G1 phase arrest, indicating that it has an effective CDK2/cyclin E targeting mechanism. CDK2-IN-50 also has a significant pro-apoptotic effect. CDK2-IN-50 can be used for the study of breast cancer .
MC180295 ((rel)-MC180295) is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC50 of 5 nM, at least 22-fold more selective for CDK9 over other CDKs. MC180295 also inhibits GSK-3α and GSK-3β. MC180295 ((rel)-MC180295) has potent anti-tumor effect .
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/cyclin B, with IC50s of 100 and 180 nM.
Cdc2 kinase substrate is a biological active peptide. (The native peptide HATPPKKKRK is a substrate for cyclin-dependent protein kinase 1 (CDC2; CDK1).)
Metuzumab (Licartin) is a human-mouse chimeric IgG1 monoclonal antibody targeting CD147. Metuzumab induces Apoptosis, reduces levels of Cyclin D1, full-length Caspase-3, and Bcl-2, and increases Bax expression. Metuzumab enhances the sensitivity of non-small cell lung cancer (NSCLC) cells to Gemcitabine (HY-17026). Metuzumab is applicable for research on hepatocellular carcinoma and non-small cell lung cancer [1][2].
CDK7/CycH/MAT1 Recombinant Human Active Protein Kinase acts as a cyclin-dependent kinase activating kinase. CDK7 exists in several forms including a core tri-partite CDK7/CycH/MAT1 complex known as CAK (cyclin-dependent kinase activating kinase), as a component in the general transcription factor TFIIH and as a component of larger complexes containing pol II and other transcription factors .
ABC1183 (Standard) is the analytical standard of ABC1183 (HY-100950). This product is intended for research and analytical applications. ABC1183 is an orally active selective dual GSK3 and CDK9 inhibitor. ABC1183 inhibits GSK3β, GSK3α and CDK9/cyclin T1 with the IC50 values of 657 nM, 327 nM and 321 nM, respectively. ABC1183 has anti-inflammatory and anti-tumor activities .
CDKI-IN-1 (Compound SNX12) is a cyclin-dependent kinase inhibitor (CDKI) inhibitor that can be used for research into degenerative diseases of the central nervous system .
SNX7 is a Cyclin-Dependent Kinase Inhibitor (CDKI) pathway inhibitor. SNX7 can be used for research of senescence-related and other CDKI-related diseases .
6:2 Fluorotelomer alcohol (6:2 FTOH) is an orally active, blood-brain barrier-permeable modulator of cyclin D1 and ETS1. 6:2 Fluorotelomer alcohol downregulates cyclin D1 expression, upregulates ETS1 via the TNF-α/ERK 1/2 pathway, impairs mitochondrial membrane potential and respiratory function, increases reactive oxygen species levels, disrupts calcium homeostasis and activates endoplasmic reticulum stress markers, and induces cell proliferation inhibition and endothelial-mesenchymal transition. Furthermore, 6:2 Fluorotelomer alcohol induces morphological abnormalities in zebrafish embryos and liver developmental damage, while disrupting the brain immune microenvironment in mice, causing systemic toxicity and delayed pup maturation in CD-1 mice. 6:2 Fluorotelomer alcohol also induces cortical neuron apoptosis, glial cell activation, synaptic abnormalities, colonic barrier damage, intestinal dysbiosis and autism spectrum disorder-like symptoms in mice. 6:2 Fluorotelomer alcohol shows no mutagenic, clastogenic, primary skin/eye irritation or skin sensitizing effects, exhibits no selective reproductive toxicity in CD-1 mice, and is classified as GHS Category 4 for acute oral toxicity. 6:2 Fluorotelomer alcohol can be used in studies of neurodevelopmental disorders and autism spectrum disorders .
XC219 (compound 43) is a cyclin-dependent kinase CDK) inhibitor, that covalently binds to CDK active site Lys. XC219 can be used in antifungal research .
CDK10/CycQ Recombinant Human Active Protein Kinase is a cyclin-dependent kinase, which is important for neural development and can act as a tumour suppressor .
FIT-039 is a selective, ATP-competitive and orally active CDK9 inhibitor with an IC50 of 5.8 μM for CKD9/cyclin T1. FIT-039 does not inhibit other CDKs and other kinases. FIT-039 inhibits replication of HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human CMV. FIT-039 is a promising antiviral agent for inhibiting drug-resistant HSVs and other DNA viruses.
AKCI is a type of AURKC-IκBα interaction inhibitor, with an IC50 value of 24.9 μM. In MDA-MB-231 cells, AKCI can induce G2/M cell cycle arrest by regulating the p53/p21/CDC2/cyclin B1 pathway, inhibit cell migration and invasion, and reduce colony formation and tumor growth. AKCI can be used for research on breast cancer .
CDK9-IN-44 (Compound 7) is a selective CDK9 inhibitor (IC50=7.6 μM). CDK9-IN-44 inhibits CDK9/cyclin T1 kinase activity, blocking transcriptional elongation, reducing the expression of pro-cancer proteins (such as MCL1, c-MYC), and inducing tumor cell apoptosis. CDK9-IN-44 is promising for research of glioblastoma (GBM) and central nervous system (CNS) disorders .
NSC139021 (ERGi-USU) is a RIOK2 inhibitor with anticancer activity. RIOK2 can highly selectively inhibit the growth of ERG-positive cancer cells with IC50s of 30-400 nM against cell lines. RIOK2 also causes cell cycle arrest and apoptosis in glioblastoma via induction of Skp2 and Skp2-p27/p21-Cyclin E/CDK2-pRb signaling .
PLK1-IN-10 (Compound 4Bb) is an orally active PLK1 PBD (polo-box domain) inhibitor. PLK1-IN-10 blocks the interaction of PLK1 with the cell division regulator protein 1 (PRC1) and decreases the protein expression of the CDK1-Cyclin B1 complex. PLK1-IN-10 reacts with glutathione (GSH) to increase cellular oxidative stress, ultimately leading to cell death .
CDK2 is a cyclin-dependent kinase involved in the control of the cell cycle. CDK2/CycO Recombinant Human Active Protein Kinase is an ortholog of CDK2 .
AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd of 8.2 nM. AUZ 454 (K03861) inhibits CDK2 activity by competing with binding of activating cyclins.
CDK16/CycY Recombinant Human Active Protein Kinase is a PCTAIRE kinase and its activity is dependent on the Cyclin Y (CCNY) family. CCNY is an oncoprotein in various cancers .
LL-K12-18 is a CDK12 kinase inhibitor and a dual-site molecular glue. LL-K12-18 inhibits human CDK12 with an IC50 value of 283.9 nM, and selectively degrades cyclin K via the ubiquitin-proteasome system by stabilizing the CDK12-DDB1 complex. LL-K12-18 downregulates DNA damage response genes, reduces the phosphorylation level of CTD Ser2 in RNA polymerase II, and modulates biomarkers such as ATM, RAD51, γ-H2AX and cleaved PARP, thereby effectively inducing apoptosis and inhibiting proliferation of breast cancer cells. LL-K12-18 exhibits high target selectivity and serves as a research tool for studies on triple-negative breast cancer .
NU6140 (Standard) is the analytical standard of NU6140 (HY-107419). This product is intended for research and analytical applications. 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 .
CDK2 is a cyclin-dependent kinase involved in the control of the cell cycle. CDK2/CycE1 Recombinant Human Active Protein Kinase is an ortholog of CDK2 .
Metralindole hydrochloride is an inhibitor of human cyclin-dependent kinase CDK2 and human protein kinase CK2 holoenzyme. Metralindole hydrochloride shows good potential as a non-small cell lung cancer inhibitor .
CDK2 is a cyclin-dependent kinase involved in the control of the cell cycle. CDK2/CycE2 Recombinant Human Active Protein Kinase is an ortholog of CDK2 .
CDK2 is a cyclin-dependent kinase involved in the control of the cell cycle. CDK2/CycD1 Recombinant Human Active Protein Kinase is an ortholog of CDK2 .
Metralindole is an inhibitor of human cyclin-dependent kinase CDK2 and human protein kinase CK2 holoenzyme. Metralindole shows good potential as a non-small cell lung cancer inhibitor .
CDK2 is a cyclin-dependent kinase involved in the control of the cell cycle. CDK2/CycA1 Recombinant Human Active Protein Kinase is an ortholog of CDK2 .
CDK2 is a cyclin-dependent kinase involved in the control of the cell cycle. CDK2/CycA2 Recombinant Human Active Protein Kinase is an ortholog of CDK2 .
PU02, a derivative of 6-MP (HY-13677), is a negative allosteric modulator (NAM) of 5-HT3 receptor, with IC50 values of 0.36 and 0.73 μM in HEK293 cells transfected with human 5-HT3A and 5-HT3AB receptors respectively .
Garcinone D (Standard) is the analytical standard of Garcinone D (HY-N6953). This product is intended for research and analytical applications. Garcinone D is an activator of the STAT3/Cyclin D1 and Nrf2/HO-1 pathways, and an inhibitor of CDK2/CyclinE1 (IC50 for CDK2/CyclinE1 is 28.23 μM). Garcinone D promotes neural stem cell proliferation by activating STAT3 phosphorylation and Cyclin D1 expression and enhancing the Nrf2/HO-1 signaling pathway. In addition, Garcinone D blocks the tumor cell cycle by inhibiting CDK2/CyclinE1. Garcinone D can promote the proliferation of C17.2 neural stem cells and inhibit prostate and breast cancer .
SH514 is an orally active IRF4 inhibitor (IC50= 2.63 μM). SH514 binds to the IRF4-DBD domain, thereby inhibiting the interaction of IRF4 protein with DNA (KD = 1.28 μM). SH514 can inhibit the proliferation of IRF4-high-expressing NCI-H929 and MM.1R cells, and displays no cytotoxicity for normal cells. SH514 significantly downregulates the expression of IRF4 downstream target genes concentration-dependently. SH514 inhibits the expression of cell cycle-related proteins CDC2, Cyclin B1, Cyclin D1, Cyclin E1, and CMYC in Multiple Myeloma cells. SH514 can induce DNA damage and increase the expression of γH2AX. SH514 effectively inhibits the proliferation of multiple myeloma tumors .
CDK1-IN-9 is an orally active and selective CDK1 inhibitor with an IC50 of 5.5 nM. CDK1-IN-9 exhibits broad antiproliferative activity, particularly against HCT116 colon cancer cells. CDK1-IN-9 induces G2/M phase arrest and downregulates CDK1, cyclin B1, and the replication initiation factor CDC45. CDK1-IN-9 induces severe DNA replication stress, subsequently activating the p53 signaling pathway to trigger apoptosis. CDK1-IN-9 can be used for research on colon cancer, liver cancer and gastric cancer .
(Z)-4EGI-1 is the Z-isomer of 4EGI-1 and is an inhibitor of eIF4E/eIF4G interaction and of translation initiation. (Z)-4EGI-1 effectively binds to eIF4E with an IC50 of 43.5 μM and a Kd value of 8.74 μM. (Z)-4EGI-1 has anticancer activity .
BMS-357075 is a pan-CDK inhibitor with CDK1IC50 18 nM, CDK2IC50 3 nM, CDK4IC50 26 nM. BMS-357075 induces cytotoxicity in human ovarian cancer A2780 cells. BMS-357075 exhibits anticancer activity in mice against P388 murine leukemia. BMS-357075 can be used for the research of leukemia .
CDK12 R722C/CycK Recombinant Human Active Protein Kinase is a cyclin-dependent kinase and regulates the expression of genes involved in DNA repair and is required for the maintenance of genomic stability .
Aloisine B (compound 9) is a cyclin-dependent kinase (CDK) inhibitor. Aloisine B inhibits cell proliferation by arresting cells in both G1 and G2 via competing with ATP-binding pocket .
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 .
GAK inhibitor 49 hydrochloride is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 hydrochloride also shows binding to RIPK2 .
N9-Isopropylolomoucine is a mitotic cyclin dependent kinase (CDK) inhibitor. N9-Isopropylolomoucine targets CCNB 1/CDK1 and can be used for cancer research .
GAK inhibitor 49 is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 also shows binding to RIPK2 .
12-Deoxyphorbol 13-palmitate is a traditional Chinese medicine monomer with antitumor activity that can be isolated from the root of Euphorbia fischeriana. 12-Deoxyphorbol 13-palmitate induces gastric cancer cell cycle arrest and apoptosis by regulating key cell cycle regulators such as cyclinB、cyclin A and CDC2. In addition, 12-Deoxyphorbol 13-palmitate can significantly weaken APOL2–SERCA2–PERK–HES1 signaling and slow liver fibrosis by targeting APOL2 .
Sutopin-2 is a topoisomerase II inhibitor. Suptopin-2 affects cell cycle progression and stability of microtubules. Sutopin-2 induces cell cycle arrest by regulating the nucleocytoplasmic transport of cyclin B1 .
CDK1 is a cyclin-dependent kinase that functions as a serine/threonine protein kinase, and is a key player in cell cycle regulation. CDK1/CycO Recombinant Human Active Protein Kinase is an ortholog of CDK1 .
CDK8-IN-10 (compound 2) is a potent, selective cyclin-dependent kinase (CDK8) inhibitor with an IC50 value of 8.25 nM. CDK8-IN-10 can be used for research of cancer .
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 .
CDK7-IN-31 (compound 13) is a potent and orally active cyclin-dependent kinase 7 (CDK7) inhibitor with a Kd value of 0.18 nM. CDK7-IN-31 shows anticancer activity .
GW8510 is a potent cyclin-dependent kinase-2 (CDK2) inhibitor. GW8510 is also a ribonucleotide reductase M2 (RRM2) inhibitor. GW8510 exhibits neuroprotective and anticancer activities .
Lenoremycin (Ro 21-6150) is a microbial metabolite. Lenoremycin decreases β-catenin and cyclin D1 proteins levels. Lenoremycin decreases cancer stem cells (CSCs) populations via inducing reactive oxygen species production .
[Ala92]-p16 (84-103) is a peptide derived from the p16CDKN2/INK4a (p16) tumor suppressor protein. [Ala92]-p16 (84-103) binds to both cdk4 and cdk6 and inhibits cdk4-cyclin D1 kinase activity in vitro (IC50: 1.5 μM). [Ala92]-p16 (84-103) blocks cell cycle progression through the G1 phase .
CDK9-IN-7 (compound 21e) is a selective, highly potent, and orally active CDK9/cyclin T inhibitor (IC50=11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD=148 nM; CDK6/cyclinD=145 nM). CDK9-IN-7 shows antitumor activity without obvious toxicity. CDK9-IN-7 induces NSCLC cell apoptosis, arrests the cell cycle in the G2 phase, and suppresses the stemness properties of NSCLC .
FIT-039 (Standard) is the analytical standard of FIT-039. This product is intended for research and analytical applications. FIT-039 is a selective, ATP-competitive and orally active CDK9 inhibitor with an IC50 of 5.8 μM for CKD9/cyclin T1. FIT-039 does not inhibit other CDKs and other kinases. FIT-039 inhibits replication of HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human CMV. FIT-039 is a promising antiviral agent for inhibiting drug-resistant HSVs and other DNA viruses.
Licoisoflavone A is an orally active isoflavone. Licoisoflavone A inhibits proliferation, induces apoptosis, and causes G1/S phase arrest in colorectal cancer (CRC) cells. Licoisoflavone A inhibits the CDK2-CyclinE1 axis. Licoisoflavone A inhibits lipid peroxidation with an IC50 of 7.2 μM. Licoisoflavone A shows a dose-dependent inhibition effect on SARS-CoV-2 infection. Licoisoflavone A exhibits significant anti-tumor efficacy in mice bearing CT26 cell subcutaneous xenografts. Licoisoflavone A can be used for the study of colorectal cancer and SARS-CoV-2 infection .
CDK1 is a cyclin-dependent kinase that functions as a serine/threonine protein kinase, and is a key player in cell cycle regulation. CDK1/CycE2 Recombinant Human Active Protein Kinase is an ortholog of CDK1 .
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 .
CDK1 is a cyclin-dependent kinase that functions as a serine/threonine protein kinase, and is a key player in cell cycle regulation. CDK4/CycD2 Recombinant Human Active Protein Kinase is an ortholog of CDK1 .
CDK1 is a cyclin-dependent kinase that functions as a serine/threonine protein kinase, and is a key player in cell cycle regulation. CDK1/CycA1 Recombinant Human Active Protein Kinase is an ortholog of CDK1 .
CDK1 is a cyclin-dependent kinase that functions as a serine/threonine protein kinase, and is a key player in cell cycle regulation. CDK1/CycA1 Recombinant Human Active Protein Kinase is an ortholog of CDK1 .
GAK inhibitor 2 (Compound 14g) is a potent cyclin G-associated kinase (GAK) inhibitor with an IC50 of 0.024 μM. GAK inhibitor 2 shows antiviral activity with an EC50 of 1.049 μM against dengue virus (DENV) .
Flavone is an anti-tumor compound that targets cell cycle regulatory proteins (such as cyclin B1) and apoptosis-related factors (such as p21waf1, PIG3). Flavone selectively induces mitochondrial-mediated apoptosis pathways in tumor cells, inhibits cyclin B1 protein expression, upregulates p21waf1, and activates p63/p73 proteins. Flavone has immunomodulatory functions that enhance natural killer cell (NK cell) activity and lymphocyte proliferation. Flavone is used in cancer research, especially for its inhibitory potential in solid tumor models such as esophageal cancer and liver cancer .
CDK7-IN-27 (Compound 37) is a selective inhibitor for cyclin-dependent kinase 7 (CDK7), with Ki of 3 nM. CDK7-IN-27 arrests the cell cycle at G0/G1 phase .
PF-06873600 is a selective and orally bioavailable inhibitor of cyclin-dependent kinase (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 .
HZ1 is an orally active first-in-class cyclin-dependent kinase like 3 (CDKL3)-specific inhibitor. HZ1 shows a strong tumor-suppressing effect, and has the potential to overcome the resistance of CDK4/6 inhibitor .
Cucurbitacin E (Standard) is the analytical standard of Cucurbitacin E. This product is intended for research and analytical applications. Cucurbitacin E is a natural compound which from Cucurbitaceae plants. Cucurbitacin E significantly suppresses the activity of the cyclin B1/CDC2 complex.
DK419 is a potent and orally active Wnt/β-catenin signaling inhibitor, with an IC50 of 0.19 μM. DK419 reduces protein lelvels of Axin2, β-catenin, c-Myc, Cyclin D1 and Survivin and induces production of pAMPK .
Cdc25A (80-93) (human) is a polypeptide that controls the cell proliferation and tumorigenesis by a change in expression of proteins involved in cyclin D1 regulation and G1/S transition. Cdc25A (80-93) (human) can be used in cancer research .
[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) .
CDK2/FLT4/PDGFRA-IN-1 (Compound 4a) is a potent inhibitor of CDK2/cyclin A, FLT4 (VEGFR3) and PDGFRA, with IC50s of 1.672, 0.554, and 0.629 μM, respectively. CDK2/FLT4/PDGFRA-IN-1 exhibits potent antiproliferative effects against cancer cells (lung EBC-1, pancreatic ductal adenocarcinoma AsPC-1, colorectal HT-29 cells). CDK2/FLT4/PDGFRA-IN-1 can also induce apoptosis in cancer cells .
LL-K8-22 is a potent, selective and durable PROTAC CDK8-cyclin C dual degrader, with DC50 values of 2.52 and 2.64 μM, respectively. LL-K8-22 also suppresses STAT1 Ser 727 phosphorylation. LL-K8-22 inhibits E2F- and MYC-driven carcinogenic transcriptional programs. LL-K8-22 can be used for triplenegative breast cancer (TNBC) research. (Pink: Ligand for target protein (HY-168683); Black: Linker (HY-Y0340); Blue: Ligand for E3 ligase (HY-N2427)) .
CDK12/CycK Recombinant Human Active Protein Kinase is a cyclin-dependent kinase that phosphorylates the C-terminal domain (CTD) of RNA polymerase II (Pol II), thereby regulating different phases of the transcription cycle from transcription initiation to elongation and termination .
Tubulin inhibitor 25 is a potent tubulin inhibitor with an IC50 value of 0.98 μM. Tubulin inhibitor 25 exhibits remarkable activity against cancer cell line HT29. Tubulin inhibitor 25 displays the potent inhibition on cell migration and tube formation that contributes to the anti-angiogenesis .
Dimethyl bisphenolate (Compound DMB) is a natural neolignan derivative with orally active anti-tumor activity. Dimethyl bisphenolate can inhibit cancer cells proliferation, invasion and migration. Dimethyl bisphenolate can activate the p53 signaling pathway, upregulate the expression of p21 protein, inhibit the activity of the CDK1-cyclin B1 complex, and cause cells to stall at the G2/M phase. Dimethyl bisphenolate can induce ROS production, upregulate pro-apoptotic proteins Noxa and Bim, downregulate anti-apoptotic protein Bcl-2, activate caspase-9 and caspase-3, and ultimately induce cell apoptosis. Dimethyl bisphenolate can be used for research of glioblastoma .
Epmedin C (Epimedin-C; Baohuoside-VI) is an orally active anti-inflammatory agent and immunomodulator that binds to multiple key proteins including UCP1, Caspase-1, CDK2 and Keap1. Epmedin C inhibits epithelial cell proliferation by disrupting the complex function of CDK2/Cyclin E. Epmedin C also upregulates Nrf2 expression, reduces ROS levels and inhibits pro-inflammatory cytokine secretion, thereby effectively restoring antibody production and alleviating tissue damage. Epmedin C has good safety with no hepatotoxicity or skin sensitization, and it has been used in studies on diseases such as obesity, Deoxynivalenol (HY-N6684)-induced immunotoxicity and mammary hyperplasia .
RRibociclib (LEE011) hydrochloride is an ATP-competitive and orally active CDK4/6 inhibitor that crosses the blood-brain barrier with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex .
PROTAC CDK2 Degrader-1 (Compound 41) is a PROTAC degrader for cyclin-dependent kinase 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 .
RRibociclib (LEE011) is an ATP-competitive and orally active CDK4/6 inhibitor that crosses the blood-brain barrier with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex .
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 .
RRibociclib (LEE011) succinate hydrate is an ATP-competitive and orally active CDK4/6 inhibitor that crosses the blood-brain barrier with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex .
RRibociclib (LEE011) succinate is an ATP-competitive and orally active CDK4/6 inhibitor that crosses the blood-brain barrier with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex .
Ribociclib-d8 is the deuterium labeled Ribociclib . 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 cyclin B/CDK1 complex .
3-ATA (NSC 680434) is a selective inhibitor of cyclin-dependent kinase 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 .
BML-259 (Standard) is the analytical standard of BML-259 (HY-108348). This product is intended for research and analytical applications. BML-259 is a potent cyclin-dependent Kinase 5 (Cdk5) inhibitor, with IC50s of 64 and 98 nM for Cdk5 and Cdk2, respectively .
CK2-IN-14 (Compound 10b) is an inhibitor for cyclin kinase 2α with an IC50 of 36.7 nM. CK2-IN-14 inhibits the growth of cancer cell 786-O and U937 with GI50 of 7.3 μM and 7.5 μM .
Anticancer agent 299 (compound P12) is a cell-cycle inhibitor, senescence inducer, apoptosis inducer, and antiproliferative agent. Anticancer agent 299 exhibits selective activity against cancer cells with minimal effects on non-tumoral chondrocyte cells at relevant concentrations. Anticancer agent 299 can be used for the research of ER+/HER2− breast cancer and BRAF-mutant melanoma .
VMY-1-103 is an inhibitor for cyclin/Cdk complex, that arrests the cell cycle at G1 phase. VMY-1-103 reduces mitochondrial membrane potential, induces p53 phosphorylation and and PARP cleavage, activates caspase-3, and thus induces apoptosis in prostate cancer cell LNCaP .
BMT-124110 is a potent, selective AAK1 inhibitor with an IC50 of 0.9 nM. BMT-124110 shows antinociceptive activity. BMT-090605 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50s of 17 and 99 nM, respectively .
Ribociclib (Standard) is the analytical standard of Ribociclib. This product is intended for research and analytical applications. 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 cyclin B/CDK1 complex .
1D228 is a c-Met/TRK inhibitor with antitumor activity. 1D228 inhibits cyclin D1 to induce G0/G1 arrest and inhibit cancer cell proliferation and migration. 1D228 can be used in the study of gastric, liver and vascular tumors .
CXJ2080 is a selective PROTAC-based CDK7 degrader with a DC50 of 0.88 nM. CXJ2080 recruits VHL E3 ligase to induce ubiquitin-proteasome-dependent CDK7 degradation, disrupts the CDK7-cyclin H-MAT1 complex, suppresses CDK7-dependent phosphorylation of RNA polymerase II CTD Ser5, CDK1 Thr161, and CDK2 Thr160. CXJ2080 activates the p53-p21 axis, suppresses MYC-driven signaling, induces leukemia cell cycle arrest, apoptosis, and differentiation, reduces CD117 expression, spares platelets and normal PBMCs, maintains sustained CDK7 degradation post-washout. CXJ2080 can be used for the research of acute leukemia .
Zinc (Zinc (II)) acetate, 99.99% trace metals basis is a heme oxygenase 1 (HO-1) activator and apoptosis inducer with cytotoxic and anticancer activities. Zinc acetate, 99.99% trace metals basis enhances HO-1 expression, alters the microRNA profile, and increases the level of caspase-cleaved cytokeratin 18. Zinc acetate, 99.99% trace metals basis also regulates the expression of Cdk2/cyclin E and interferes with cell cycle progression. Zinc acetate, 99.99% trace metals basis effectively inhibits cancer cell proliferation and induces their rapid death, with no significant cytotoxicity to non-tumor tissues. Zinc acetate, 99.99% trace metals basis has been widely used in studies related to hepatocellular carcinoma, prostate cancer, and other conditions .
CDK4/6-IN-14 is a potent and highly selective CDK4 and CDK6 (CDK) inhibitor with IC50s of 10 nM and 16 nM, respectively. CDK4/6-IN-14 exhibits more than 60-fold selectivity over CDKs 1, 2, 7, and 9, and shows high selectivity among other 205 kinases .
SW106065 is an apoptosis inducer in malignant peripheral nerve sheath tumors (MPNST). SW106065 inhibits ATP consumption of sMPNST and other models of MPNST with an EC50 of 1 µM. SW106065 can be used for MPNST research .
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 .
Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2 . Obatoclax Mesylate induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax Mesylate has anti-cancer and broad-spectrum antiparasitic activity .
BMT-124110 formic is a potent, selective AAK1 inhibitor, with an IC50 of 0.9 nM. BMT-124110 shows antinociceptive activity. BMT-124110 formic inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50s of 17 and 99 nM, respectively .
JTK-101 is a selective HIV inhibitor. JTK-101 selectively reduces HIV-1 mRNA synthesis by inhibiting Tat cofactors, including CDK9 and cyclin T1, thereby suppressing the transcriptional activity of HIV-1. JTK-101 may be used in the field of anti-HIV virus research .
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-dependent kinase 2 (CDK2) .
VCC972839:01 is an inhibitor for cyclin dependent kinase(CDK9), with IC50 of 7 nM. VCC972839:01 inhibits the cell viability of SCLC cells in nanomolar levels. VCC972839:01 induces apoptosis through an intrinsic pathway. VCC972839:01 exhibits antitumor activity in mouse model .
CCT036477 is a Wnt/β-catenin pathway inhibitor. CCT036477 blocks transcription at β-catenin without altering its levels. CCT036477 inhibits proliferation of various cancer cells, development of embryos, and expression of Wnt target genes (PPARδ, Cyclin D1, TCF4, and ID2) .
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 .
Ribociclib succinate (Standard) is the analytical standard of Ribociclib succinate. This product is intended for research and analytical applications. 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 cyclin B/CDK1 complex.
Obatoclax (GX15-070), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2 . Obatoclax induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax has anti-cancer and broad-spectrum antiparasitic activity .
SKLB70326 is a small molecule inhibitor of cell cycle progression that induces cell cycle arrest and apoptosis in human hepatocellular carcinoma cells. SKLB70326 is involved in downregulating cyclin-dependent kinase (CDK) 2, CDK4, and CDK6, while also activating PARP, caspase-3, caspase-9, and Bax, and downregulating Bcl-2.
CDK9-IN-2 is a special cyclin-dependent kinase 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.
CDK9-IN-39 (1-7a-B1) is an orally active cyclin-dependent kinase 9(CDK9) inhibitor with an IC50 of 6.51 nM. CDK9-IN-39 induces cell apoptosis by inhibiting the phosphorylation of RNA polymerase II at Ser2 and can be used for study of colorectal cancer .
Ribociclib-d6 (LEE011-d6) is a deuterium labeled Ribociclib (HY-15777). 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 .
CDK8/19-IN-2 (compound 12) is an orally active and potent cyclin-dependent kinase 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 .
CKD-712 is an orally active multi-target tetrahydroisoquinoline derivatived and a potent inhibitor of the NF-κB pathway . CKD-712 selectively inhibits MMP-9 with no effect on MMP-2, downregulates the expression of TNF-α, IL-6, cyclin A, cyclin B, CDK-1 and other proteins, and activates the PI3K/Akt signaling pathway . CKD-712 blocks the activation and nuclear translocation of NF-κB, downregulates inflammatory factors and pro-tumor metastatic proteins, and induces G2/M phase arrest in tumor cells and thereby inhibits the invasion of cancer cells . CKD-712 can be used for the research of sepsis, myocardial ischemia-reperfusion injury and non-small cell lung cancer .
Epmedin C (Standard) is the analytical standard of Epmedin C. This product is intended for research and analytical applications. Epmedin C (Epimedin-C; Baohuoside-VI) is an orally active anti-inflammatory agent and immunomodulator that binds to multiple key proteins including UCP1, Caspase-1, CDK2 and Keap1. Epmedin C inhibits epithelial cell proliferation by disrupting the complex function of CDK2/Cyclin E. Epmedin C also upregulates Nrf2 expression, reduces ROS levels and inhibits pro-inflammatory cytokine secretion, thereby effectively restoring antibody production and alleviating tissue damage. Epmedin C has good safety with no hepatotoxicity or skin sensitization, and it has been used in studies on diseases such as obesity, Deoxynivalenol (HY-N6684)-induced immunotoxicity and mammary hyperplasia .
LA-CB1 is an Abemaciclib (HY-16297A) derivative that targets CDK4/6 and promotes its degradation via the ubiquitin-proteasome pathway, thereby disrupting the CDK4/6-Cyclin D1-Rb-E2F axis and inducing G0/G1 cell cycle arrest and apoptosis. LA-CB1 exhibits antiproliferative activity against MDA-MB-231 cells, with an IC50 of 0.27 µM, and effectively inhibits epithelial-mesenchymal transition (EMT), cell migration, invasion, and angiogenesis. In highly aggressive models such as triple-negative breast cancer (TNBC), LA-CB1 significantly suppresses tumor growth in a dose-dependent manner. LA-CB1 holds potential for research in the field of breast cancer .
Lixazinone (RS-82856) is a selective inhibitor of cGMP-inhibited phosphodiesterase (PDE3) with an IC50 value of 22 nM. Lixazinone exhibits positive inotropic effects, afterload reduction and antithrombotic properties. Lixazinone increases cyclic adenosine monophosphate (cAMP) levels in human platelets, inhibits thrombin-induced aggregation of human platelets, and blocks the photolabeling of PDE3 active sites by [ 32P]cGMP. Lixazinone can be used in the research of polycystic kidney disease and congestive heart failure .
CDK4/6-IN-12 is a potent cyclin-dependent kinase 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 .
Ribociclib (Standard) (LEE011(Standard)) hydrochloride is the analytical standard of Ribociclib hydrochloride (HY-15777A). This product is intended for research and analytical applications. 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 cyclin B/CDK1 complex.
CDK7-IN-4 (compound I) is a potent CDK7 (Cyclin-dependent kinase 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 .
1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC (PC(18:0/22:4)) is an inhibitor of cyclin-dependent kinases (CDKs). 1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC induces apoptosis and inhibits the growth of various cancer cell lines .
Aurora kinase-IN-2 (compound 12Aj) is a potent Aurora kinase inhibitor with IC50 values of 90 and 152 nM for Aurora A and Aurora B. Aurora kinase-IN-2 arrests cell cycle at G2/M phase by regulating cyclin B1 and cdc2. Aurora kinase-IN-2 can be used for cancer research .
(-)-Hinesol (Hinesol) is a potent anticancer agent. (-)-Hinesol induces apoptosis and cell cycle arrest at G0/G1 phase. (-)-Hinesol downregulates MEK/ERK pathway and NF-κB pathway and mediates theexpression of cyclin D1, Bax and Bcl-2. (-)-Hinesol has the potential for the research of non–small cell lung cancer .
CLM3, a pyrazolopyrimidine derivative, is a multiple tyrosine kinase inhibitor. CLM3 shows antiproliferative and proapoptotic activity on endothelial and cancer cells, synergistically enhanced by SN38 (HY-13704). These effects are mainly due to its inhibition of phosphorylation of VEGFR-2, EGFR and RET tyrosine kinases and their related signaling pathways .
(Rac)-Roscovitine ((Rac)-Seliciclib) is a selective cyclin-dependent kinases (CDKs) inhibitor. (Rac)-Roscovitine binds to the active sites of CDKs competitively with ATP, inhibiting the phosphorylation activity of CDKs. (Rac)-Roscovitine induces apoptosis in cancer cells. (Rac)-Roscovitine is promising for research of cancers or other diseases associated with CDK dysregulation, such as neurodegenerative diseases, cardiac disorders, viral and protozoan infections, glomerulonephritis, and chronic inflammation .
CDC20-IN-2 (14c), a Cdc20 inhibitor (KD: 7.65 μM), causes G2/M phase arrest and promotes DNA damage accumulation. CDC20-IN-2 (14c) stabilizes key substrates such as Cyclin B1 and Bim, leading to enhanced apoptosis and suppression of tumor cell proliferation and migration .
Cucurbitacin E is a CDK1 inhibitor that significantly inhibits the activity of the cyclin B1/CDC2 complex. Cucurbitacin E also induces PANoptosis in adrenocortical carcinoma cells in a ZBP1-dependent manner. Cucurbitacin E exhibits synergistic effects with Mitotane (HY-13690); when used in combination, they effectively eliminate tumors .
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 .
Milciclib (PHA-848125) maleate is a cyclin-dependent kinase 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.
MFH290 is a potent and highly selective cyclin-dependent kinase 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 .
CDK2-IN-52 (Compound Cpb No 39) is a selective cyclin-dependent kinase 2 (CDK2) inhibitor with a DC50 value of 1-10 nM. CDK2-IN-52 induces cell cycle arrest and suppresses tumor cell proliferation. CDK2-IN-52 is promising for research of CDK2-overexpressing malignancies such as breast and ovarian cancers .
ML364 is a selective ubiquitin specific peptidase 2 (USP2) inhibitor (IC50=1.1 μM) with anti-proliferative activity, which direct binds to USP2 (Kd=5.2 μM), induces an increase in cellular cyclin D1 degradation and causes cell cycle arrest. ML364 increases the levels of mitochondrial ROS and decreases in the intracellular content of ATP .
Indisulam (E 7070) is a carbonic anhydrase inhibitor with anticancer activity. Indisulam (E 7070) is a sulfonamide agent that targets the G1 phase of the cell cycle. Indisulam (E 7070) causes a blockade in the G1/S transition through inhibition of the activation of both CDK2 and cyclin E. Indisulam (E 7070) targets splicing by inducing RBM39 degradation via recruitment to DCAF15 .
PKN3-IN-1 (compound 16) inhibits PKN3 (serine/threonine protein kinase 3) and GAK (cyclin G-associated kinase) with IC50 of 0.014 μM and Ki of 0.0044 μM respectively. PKN3-IN-1 is a potential tool compound to study the cell biology of PKN3 and its role in pancreatic and prostate cancer and T-cell acute lymphoblastic leukemia .
NCT02 is a molecular glue degrader based on the E3 ubiquitin ligase DDB1 that targets CDK12 and its binding partner CCNK. NCT02 triggers the ubiquitination and proteasomal degradation of CCNK, thereby downregulating CDK12 protein levels and inhibiting its downstream signaling pathways. NCT02 can induce tumor cell apoptosis, arrest the cell cycle, and selectively inhibit the proliferation of colorectal cancer cells carrying TP53 defects or belonging to the consensus molecular subtype CMS4. NCT02 has the potential to inhibit tumor growth in in vitro and in vivo models .
Yatein is a lignan isolated from A. chilensis, with antiproliferative activity . Yatein suppresses herpes simplex virus type 1 (HSV-1 ) replication by interruption the immediate-early gene expression .
MAPK-IN-3 (Compound 4a) is an anti-proliferative agent that shows particularly strong inhibitory effects on KYSE 30, HCT 116, and HGC 27, with IC50 values of 0.57 μM, 3.27 μM, and 2.28 μM, respectively. MAPK-IN-3 blocks the cell cycle via a p53-dependent mechanism and induces cell apoptosis through a p53-independent mechanism. MAPK-IN-3 downregulates the expression of cell cycle-related proteins like Cyclin D1 and cyclin B1, upregulates pro-apoptotic proteins such as cleaved PARP, cleaved caspase-7, and cleaved caspase-9, and reduces the expression of anti-apoptotic proteins like Bcl-2. Additionally, MAPK-IN-3 increases the intracellular level of ROS in KYSE 30 cells and upregulates the expression of members of the MAPK signaling pathway associated with ROS, such as p-ERK, p-p38 and p-JNK .
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 .
OBHSA is a selective estrogen receptor (ERα) degrader. OBHSA blocks the cell cycle by degrading cyclin D1, thereby overcoming Tamoxifen (HY-13757A) resistance. OBHSA also triggers excessive activation of the unfolded protein response (UPR) by inducing an increase in intracellular reactive oxygen species, ultimately leading to cell apoptosis. In addition, OBHSA can also be used as an ERα ligand to synthesize PROTAC degraders .
CDK4-IN-3 (Compound 389) is a potent irreversible cyclin-dependent kinase 4 (CDK4) inhibitor (IC50=25 nM, >10-fold selective over CDK6). CDK4-IN-3 arrests the cell cycle at G₁ phase, and induces tumor cell apoptosis. CDK4-IN-3 is promising for research of solid tumors such as breast and lung cancers .
CDK2-IN-44 (Compound 46) is an inhibitor of cyclin-dependent kinase 2 (CDK2). CDK2-IN-44 can effectively inhibit the proliferation of cancer cells and exert its activity in inhibiting cancer cell growth by arresting the cell cycle, promoting Apoptosis, and inducing cellular senescence. CDK2-IN-44 holds promise for use in the research of ovarian cancer and breast cancer .
Ubiquitin Conjugating enzyme E2C (EC 2.3.2.24) is a member of the E2 ubiquitin-conjugating enzyme family, and it is the principal regulator of pathways for protein degradation in eukaryotes. Ubiquitin Conjugating enzyme E2C is involved in the tumorigenesis of various malignancies. Ubiquitin Conjugating enzyme E2C is also involved in mitotic cyclin disruption, affecting cell cycle progression. Ubiquitin Conjugating enzyme E2C is a prognostic indicator for cholangiocarcinoma .
ZSNI-21 is a ADAM17/HDAC2 inhibitor with ADAM17IC50 0.939 μM and HDAC2IC50 0.844 μM. ZSNI-21 regulates the expression of apoptosis-related proteins (Bax, Bcl-2) and Cyclin D1, and induces apoptosis.. ZSNI-21 can be used for the research of hepatocellular carcinoma, breast cancer, and non-small cell lung cancer .
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-dependent kinase inhibitor Rocovitine .
CAIX/CDK-2-IN-1 is a dual-acting inhibitor of carbonic anhydrase IX (CA IX) and cyclin-dependent kinase-2 (CDK-2) with IC50 values of 0.29 μM and 0.32 μM. The zein nanoparticls of CAIX/CDK-2-IN-1 can induce cancer cells apoptosis. CAIX/CDK-2-IN-1 can be used for the research of cancer, such as lung cancer .
Akt/mTOR-IN-1 (Compound 8r) is an AKT/mTOR signaling pathway inhibitor exhibiting an IC50 value of 0.8 µM with anticancer activity. Akt/mTOR-IN-1 can decrease the expression of Caspase 3 and increase the expression of the autophagic protein Cyclin B1, thereby inducing cell autophagy and apoptosis. Akt/mTOR-IN-1 can be used in research related to non-small cell lung cancer (NSCLC) .
Tubulin-IN-65 (Compound Imp-18) is a Tubulin inhibitor. Tubulin-IN-65 exhibits tubulin-disrupting activity. Tubulin-IN-65 disrupts microtubule integrity. Tubulin-IN-65 induces Apoptosis and increases the expression of CDK1 and Cyclin B1. Tubulin-IN-65 possesses anticancer activity against breast cancer and colorectal cancer. Tubulin-IN-65 can be used in research related to triple-negative breast cancer and colorectal adenocarcinoma .
Decursin ((+)-Decursin) is a potent anti-tumor agent. Decursin also is a cytotoxic agent and a potent protein kinase C activator. Decursin induces apoptosis and cell cycle arrest at G1 phase. Decursin decreases the expression of CDK2, CDK4, CDK6, cyclin D1 protein at 48 h. Decursin inhibits cell proliferation and migration. Decursin shows anti-tumor, anti-inflammatory and analgesic activities .
Bisindolylmaleimide X hydrochloride(Ro 31-8425 hydrochloride, BIM-X hydrochloride) is a cell-penetrating PKC inhibitor. Bisindolylmaleimide X hydrochloride is a potent cyclin-dependent kinase 2 (CDK2) antagonist with an IC50 of 200 nM. Bisindolylmaleimide X hydrochloride inhibits the proliferation of CD4 T cells in vitro. Bisindolylmaleimide X hydrochloride inhibits eNOS-Ser1177 phosphorylation in human embryonic vein endothelial cells. Bisindolylmaleimide X hydrochloride can be used for research on the immune system and cardiovascular diseases .
Bisindolylmaleimide X (Ro 31-8425, BIM-X) is a cell-penetrating PKC inhibitor. Bisindolylmaleimide X is a potent cyclin-dependent kinase 2 (CDK2) antagonist with an IC50 of 200 nM. Bisindolylmaleimide X inhibits the proliferation of CD4 T cells in vitro. Bisindolylmaleimide X inhibits eNOS-Ser1177 phosphorylation in human embryonic vein endothelial cells. Bisindolylmaleimide X can be used for research on the immune system and cardiovascular diseases .
HER2-IN-23 is a selective HER2 inhibitor. HER2-IN-23 reduces in total HER2 expression rather than in phosphorylated HER2 (p-HER2). HER2-IN-23 reduces cyclin D1 level and stimulates PARP cleavage. HER2-IN-23 can be used for the study of HER2-positive breast cancer .
BMS-265246 is a potent and selective cyclin-dependent kinaseCDK1 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 .
CDK1-IN-1 is a potent CDK1 inhibitor (CDK1/CycB IC50=161.2 nM) with potential antiproliferative activity and selectivity for cancer tissues. CDK1-IN-1 induces apoptosis in p53 dependent manner through the intrinsic apoptotic pathway. CDK1-IN-1 is a potential targeted antitumor agent .
O6-Benzylguanine, a guanine analog, is the DNA repair enzyme O6-alkylguanine-DNA alkyltransferase (MGMT/AGT) inhibitor. O6-Benzylguanine acts as an AGT substrate, which transfers its benzyl group to the AGT cysteine residue, thereby irreversibly inactivating AGT and preventing DNA repair. O6-Benzylguanine induces tumor cell apoptosis. Antineoplastic activity .
ZLY025 is a potent and orally active CCNK molecular glue degrader with an DC50 of 42.7 nM. ZLY025 exhibits broad-spectrum antiproliferative activity against various tumor cells with IC50 values ranging from 0.08 to 2.45 μM. ZLY025 can induce cells apoptosis and G1 phase arrest. ZLY025 can be used for the research of cancer, such as lung cancer .
O6-Benzylguanine, a guanine analog, is the DNA repair enzyme O6-alkylguanine-DNA alkyltransferase (MGMT/AGT) inhibitor. O6-Benzylguanine acts as an AGT substrate, which transfers its benzyl group to the AGT cysteine residue, thereby irreversibly inactivating AGT and preventing DNA repair. O6-Benzylguanine induces tumor cell apoptosis. Antineoplastic activity .
KPT-6566 is a selective and covalent prolyl isomerase PIN1 inhibitor, covalently binds to the catalytic site of PIN1, selectively inhibits and degrades PIN1. KPT-6566 shows an IC50 value of 640 nM and a Ki value of 625.2 nM for PIN1 PPIase domain. KPT-6566 can be used for the research of cancer .
Ascochlorin (Ilicicolin D), an isoprenoid antibiotic, mediates its anti-tumor effects predominantly through the suppression of STAT3 signaling cascade. Ascochlorin induces apoptosis. Anti-inflammatory activity .
CDK9-IN-14 is a potent and selective CDK9 inhibitor with IC50 of 6.92 nM. CDK9-IN-14 has a relatively strong inhibitory effect on MV4;11 cells and in vivo tumor models, and has a good selectivity and a low toxicity and few side effects .
CDK8 modulates the transcriptional output from distinct transcription factors involved in oncogenic control, including the Wnt/β-catenin pathway, Notch, p53, and transforming growth factor β. Abnormal activity ofCDK8 along with its partner protein cyclin C (CycC) is a common feature of many diseases including colorectal cancer. CDK8/CycC Recombinant Human Active Protein Kinase can be used to study the function of CDK8/CycC .
2,5-Dimethylcelecoxib is an analogue of celecoxib (HY-14398) with anticancer activity but without COX-2 inhibitory activity. 2,5-Dimethylcelecoxib exerts its anti-cancer cell proliferation effect by inhibiting the core mechanism of the Wnt/β-catenin signaling pathway. 2,5-Dimethylcelecoxib also inhibits T-cell factor-dependent transcriptional activity and inhibits expression of the Wnt/β-catenin target gene products cyclin D1 and survivin .
Lacto-N-fucopentaose I (LNFPI) is a human milk oligosaccharide (HMO), possessing antiviral and antibacterial activity. Lacto-N-fucopentaose I can reduce capsid protein VP1 to block virus adsorption, promote CDK2 and reduce cyclin E to recover cell cycle S phase block. Lacto-N-fucopentaose I inhibits ROS production and apoptosis in virus-infected cells. Lacto-N-fucopentaose I can also regulate intestinal microbiota to affect immune system development .
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-dependent kinase 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 .
FLT3/CDKs ligand-1 (Compound 14) is a ligand for target protein, which promotes the degradation of cyclin-dependent kinase (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) .
CDK9 autophagic degrader 1 (Compound 28) is a ATTEC degrader that can be used to degrade CDK9 and also affects the levels of the associated Cyclin T1. CDK9 autophagic degrader 1 shows over 80% CDK9 inhibition rate at 100 nM . ( Pink: LC3B ligand (HY-168897); Black: linker (HY-W017758); Blue: target protein ligand (HY-10008); linker + target protein ligand (HY-168898))
Isosilybin B is a flavonolignan. Isosilybin B can be isolated from Silybum marianum. Isosilybin B can regulate cell cycle-related proteins (e.g., reduce cyclins (D3, D1, A, E), Cdk4, Cdk2, Cdc25A), and activate Caspases(Caspase-9 and Caspase-3). Isosilybin B can promote Apoptosis, reduce androgen receptor (AR) and PSA. Isosilybin B has anticancer activity against prostate cancer .
HDAC-IN-46 (compound 12c) is a potent HDAC inhibitor with an IC50 value of 0.21 μM and 0.021 μM for HDAC1 and HDAC6, respectively. HDAC-IN-46 upregulates p-p38, and downregulates Bcl-xL and cyclin D1 in MDA-MB-231 cells. HDAC-IN-46 induces significant G2 phase arrest and apoptosis. HDAC-IN-46 can be used for researching triple-negative breast cancer (TNBC) .
Indisulam (Standard) is the analytical standard of Indisulam. This product is intended for research and analytical applications. Indisulam (E 7070) is a carbonic anhydrase inhibitor with anticancer activity. Indisulam (E 7070) is a sulfonamide agent that targets the G1 phase of the cell cycle. Indisulam (E 7070) causes a blockade in the G1/S transition through inhibition of the activation of both CDK2 and cyclin E. Indisulam (E 7070) targets splicing by inducing RBM39 degradation via recruitment to DCAF15 .
LP-922761 hydrate is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 hydrate also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 hydrate shows less activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors .
LP-922761 is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 exhibits no significant activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors .
AR/AR-V7 degrader-1 is an orally active AR and AR-V7 degrader. AR/AR-V7 degrader-1 disrupts the interaction between AR/AR-V7 and HSP90, leading to their ubiquitination and degradation in castration-resistant prostate cancer cells. AR/AR-V7 degrader-1 regulates the expression of cell cycle-related proteins in prostate cancer cells (downregulates CDK4, CDK6, Cyclin D1, Cyclin E1; upregulates P21) and induces G0/G1 phase arrest. AR/AR-V7 degrader-1 inhibits the proliferation and migration of prostate cancer cells. AR/AR-V7 degrader-1 suppresses the growth of castration-resistant prostate cancer tumors in nude mice and induces the degradation of AR and AR-V7 in tumor tissues. AR/AR-V7 degrader-1 is applicable to the research of castration-resistant prostate cancer .
CDK8-IN-6 (compound 9) is a potent cyclin-dependent kinase 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 .
P-gp/CDK2-IN-1 (Compound 4j) is an inhibitor for is inhibitor for P-glycoprotein (P-gp) and for cyclin-dependent kinase-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 .
KW-2478 is an HSP90 inhibitor (IC50 = 3.8 nM). KW-2478 inhibits the growth and induces apoptosis in chronic myeloid leukemia (CML) cells and liver cancer cells. KW-2478 weakens the BCR/ABL and MAPK signaling pathways, leading to increased p27 and p21 expression and decreased cyclin B1 expression. KW-2478 downregulates STAT3 expression. KW-2478 may be used in research on cancers such as CML and liver cancer .
ML364 (Standard) is the analytical standard of ML364 (HY-100900). This product is intended for research and analytical applications. ML364 is a selective ubiquitin specific peptidase 2 (USP2) inhibitor (IC50=1.1 μM) with anti-proliferative activity, which direct binds to USP2 (Kd=5.2 μM), induces an increase in cellular cyclin D1 degradation and causes cell cycle arrest. ML364 increases the levels of mitochondrial ROS and decreases in the intracellular content of ATP .
LLL3 (CLT-005) is a STAT3 inhibitor. LLL3 inhibits dimerization and phosphorylation of STAT3, thereby preventing intraconuclear transfer of STAT3 and inhibits the expression of STAT3 dependent genes, which encode proteins such as Bcl-xL and cyclin D1. In addition, LLL3 can induce cell growth inhibition and apoptosis in human breast cancer and rhabdomyosarcoma cells via the caspase pathway. LLL3 can be used in the study of STAT3 persistent activation types of cancer .
Decursin (Standard) is the analytical standard of Decursin. This product is intended for research and analytical applications. Decursin ((+)-Decursin) is a potent anti-tumor agent. Decursin also is a cytotoxic agent and a potent protein kinase C activator. Decursin induces apoptosis and cell cycle arrest at G1 phase. Decursin decreases the expression of CDK2, CDK4, CDK6, cyclin D1 protein at 48 h. Decursin inhibits cell proliferation and migration. Decursin shows anti-tumor, anti-inflammatory and analgesic activities [4].
NVP-2 is a potent and selective ATP-competitive cyclin dependent kinase 9(CDK9) probe, inhibits CDK9/CycT activity with an IC50 of 0.514 nM. NVP-2 displays inhibitory effcts on CDK1/CycB, CDK2/CycA and CDK16/CycY kinases with IC50 values of 0.584 μM, 0.706 μM, and 0.605 μM, respectively. NVP-2 induces cell apoptosis.
CDK12 ligand-3 is a molecular glucose degrading agent that targets the CDK12 protein (DC50 = 35 nM). CDK12 ligand-3 degrades CDK12, CDK13 and their regulatory subunit Cyclin K in a concentration dependent manner, and inhibits RNA polymerase II CTD (Ser2) phosphorylation. CDK12 ligand-3 exhibits potent anti proliferative activity against Jurkat cells. CDK12 ligand-3 can be used for research on cancers such as leukemia .
CDK/HDAC-IN-4 is a high selective dual cyclin-dependent kinase (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 .
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-dependent kinase 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 .
KW-2478 hydrochloride is an HSP90 inhibitor (IC50 = 3.8 nM). KW-2478 hydrochloride inhibits the growth and induces apoptosis in chronic myeloid leukemia (CML) cells and liver cancer cells. KW-2478 hydrochloride weakens the BCR/ABL and MAPK signaling pathways, leading to increased p27 and p21 expression and decreased cyclin B1 expression. KW-2478 hydrochloride downregulates STAT3 expression. KW-2478 hydrochloride may be used in research on cancers such as CML and liver cancer .
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].
CDK8-IN-7 (compound 12) is a potent and selective cyclin-dependent kinase 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 .
MG-002 is an orally active eIF4A inhibitor. MG-002 non-productively traps the eukaryotic translation initiation factor 4A (eIF4A) onto RNA, hindering the recruitment and scanning of ribosomes, thereby inhibiting mRNA translation. MG-002 selectively inhibits the growth and metastasis formation of triple-negative breast cancer (TNBC) tumors and induces cell apoptosis. MG-002 significantly inhibits the protein expression of c-MYC and cyclin D1. MG-002 can be used for research on TNBC .
Gomisin G is a lignin from S. chinesis with anti-HIV (EC50 = 0.006 μg/mL), anti-liver cancer and anti-inflammatory activities. Gomisin G has an AKT-cyclin D1 dependent mechanism against triple-negative breast cancer (TNBC) cells through suppressing phosphorylation rather than inducing apoptosis. Gomisin G can inhibit AKT phosphorylation. Gomisin G can cause cell cycle arrest in the G1 phase. Gomisin G can be studied in research for diseases such as HIV, breast and liver cancers .
Decursin-d6 ((+)-Decursin-d6) is the deuterium labeled Decursin (HY-18981). Decursin ((+)-Decursin) is a potent anti-tumor agent. Decursin also is a cytotoxic agent and a potent protein kinase C activator. Decursin induces apoptosis and cell cycle arrest at G1 phase. Decursin decreases the expression of CDK2, CDK4, CDK6, cyclin D1 protein at 48 h. Decursin inhibits cell proliferation and migration. Decursin shows anti-tumor, anti-inflammatory and analgesic activities .
CDK12-IN-8 (Compound Cpd143) is an orally active and highly selective inhibitor of cyclin-dependent kinase 12 (CDK12). CDK12-IN-8 inhibits CDK12-mediated phosphorylation of the C-terminal domain (CTD) serine 2 of RNA polymerase II, interfering with gene transcription elongation and DNA damage repair pathways. CDK12-IN-8 is promising for research of cancers with high CDK12 expression such as small cell lung cancer and triple-negative breast cancer .
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 .
XSJ151 is a topoisomerase I inhibitor, stabilizing the DNA-Topo I covalent complex and inducing DNA double-strand breaks. XSJ151-induces DNA damage activates the p53-p21 signaling pathway, specifically regulating the expression of cyclins, leading to G2/M phase cell cycle arrest and disrupting the dynamic homeostasis of Bcl-2 family proteins, thereby triggering apoptosis in gastric cancer cells. XSJ151 can be used for the study of gastric cancer .
9-cis-Retinoic acid (Standard) is the analytical standard of 9-cis-Retinoic acid. This product is intended for research and analytical applications. 9-cis-Retinoic acid (ALRT1057), a vitamin A derivative, is a potent RAR/RXR agonist. 9-cis-Retinoic acid induces apoptosis, regulates cell cycle and has anticancer, anti-inflammatory and neuroprotection activities[1][2][3][4][5].
9-cis-Retinoic acid (ALRT1057), a vitamin A derivative, is a potent RAR/RXR agonist. 9-cis-Retinoic acid induces apoptosis, regulates cell cycle and has anticancer, anti-inflammatory and neuroprotection activities .
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 .
SGC-CDKL2/AAK1/BMP2K-1 (Compound 9) is a potent and selective CDKL2 (Cyclin-dependent kinase-like 2) inhibitor with an IC50 value of 460 nM. CDKL2 is involved in various biological processes such as tumorigenesis, development, and viral infections. SGC-CDKL2/AAK1/BMP2K-1 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 .
GDC-4198 (RGT-419B) is an orally active CDK4/2 inhibitor with desired degrees of selectivity against kinases such as CDK6, CDK9 and GSK3β. GDC-4198 inhibits the activity of cyclin-CDK complexes, blocks phosphorylation of the retinoblastoma protein (pRb), arresting the cell cycle transition from G1 to S phase. GDC-4198 is promising for research of cancers, such as breast cancer (especially hormone receptor-positive, HER2-negative type), lung cancer, and colorectal cancer .
Resibufogenin is an orally active anticancer agent. Resibufogenin can be extracted from toad venom. Resibufogenin blocks signaling pathways such as PI3K/Akt, NF-κB, AP-1, activates GSK-3β, and regulates cyclin D1. Resibufogenin can activate central neurons. Resibufogenin has anti-inflammatory activity. Resibufogenin has anti-tumor effects on a variety of tumors such as multiple myeloma, renal cancer, colorectal cancer, pancreatic cancer, and glioma [9].
β,β-Dimethylacrylalkannin (Arnebin 1) is an orally active FGFR1 inhibitor (IC50=2.5 μM) and the main active component of Lithospermum erythrorhizon. β,β-Dimethylacrylalkannin blocks downstream signaling by binding to the ATP pocket of FGFR1, and regulates the CDK1/Cdc25C pathway and ROS-JNK axis, thereby inducing G2/M phase arrest, necrosis and apoptosis in cancer cells, and inhibiting tumor proliferation. β,β-Dimethylacrylalkannin also acts as a colistin adjuvant to disrupt the cell membrane of Gram-negative bacteria. β,β-Dimethylacrylalkannin exhibits significant tumor-inhibitory effects with no obvious toxicity in PDX models, but chronic exposure to high doses may alter the relative lung/liver weights of rats, while acute exposure to high doses causes responses such as reduced motor activity. β,β-Dimethylacrylalkannin finds wide application in studies related to hepatocellular carcinoma, colorectal cancer, colistin-resistant bacterial infections, hepatitis and psoriasis .
PARP1-IN-50 is a selective and orally active PARP-1 inhibitor with an IC50 of 64.98 nM. PARP1-IN-50 can inhibit PAR formation and induce DNA double strand breaks, thereby causing DNA damage. PARP1-IN-50 can induce G2/M phase arrest and cancer cells apoptosis. PARP1-IN-50 demonstrates significant antiproliferative activity against various cancer cells. PARP1-IN-50 can be used for the research of cancer, such as breast cancer .
GSPT1 degrader-1 is a highly selective degrader targeting GSPT1. GSPT1 degrader-1 induces degradation via the ubiquitin-proteasome system. GSPT1 degrader-1 induces G0/G1 phase arrest, apoptosis (apoptosis) and inhibits proliferation in leukemia cells. GSPT1 degrader-1 reduces the levels of CDK6 and Cyclin B1, while increases the levels of activated caspase-3 and caspase-9 in leukemia cells. GSPT1 degrader-1 can be used in leukemia research .
Hexamethylquercetagetin (Hexa-O-methylquercetagetin; Quercetagetin hexamethyl ether; 3,5,6,7,3',4'-Hexamethoxyflavone) is an orally active NF-κB inhibitor. Hexamethylquercetagetin inhibits NF-κB-derived luciferase activity, reduces phosphorylated p65 and IκBα, Cyclin D1, Bcl-2 and blocks TNFα-induced NF-κB activation. Hexamethylquercetagetin inhibits survival and proliferation of cervical carcinoma cells. Hexamethylquercetagetin suppresses tumor volume and weight in BALB/c nude mouse xenograft models of cervical carcinoma. Hexamethylquercetagetin can be used for the research of cancer, such as cervical carcinoma .
Sulindac sulfone is an orally active metabolite of Sulindac (HY-B0008). Sulindac sulfone activates PPARγ and drives transcriptional induction of SSAT by binding to the PPRE-2 element. Sulindac sulfone induces Apoptosis. Sulindac sulfone negatively regulates the function of VDAC1/2 to inhibit the mTORC1 pathway, reduces Cyclin D1 levels, and induces G1 cell cycle arrest in colon cancer cells. Sulindac sulfone exerts colon cancer preventive effects through a COX-independent mechanism. Sulindac sulfone can be used in research related to colon cancer .
Butrin is a compound found in Butea monosperma flowers. Butrin reduces expression of SIRT1, AURKB, cyclin D1, pAKT, GSK-3β, β-catenin, and TGF-3β expression, enhances apoptosis and ROS production in cancer cells. Butrin downregulates Wnt and NF-κB signaling, mitigates oxidative stress, reduces proinflammatory cytokine (TNF-α, IL-6 and IL-8) production and suppresses neuroinflammation. Butrin inhibits IKK enzyme activity. Butrin can be used for the researches of colorectal cancer, Alzheimer’s disease, and rheumatoid arthritis .
Tubulin polymerization-IN-85 (Compound C21) is a tubulin polymerization inhibitor (IC50 = 1.59 μM) targeting the colchicine binding site. Tubulin polymerization-IN-85 can cause cancer cells G2/M phase arrest and induce apoptosis. Tubulin polymerization-IN-85 downregulates the expression of Bcl-2, Bcl-xl, Mcl-1, Cyclin B1, cdc25, cdc2 protein and upregulates P53, P21, Bad and Bax levels. Tubulin polymerization-IN-85 can be used for the research of cancer, such as cervical cancer .
Fluacrypyrim, a Miticide, is a STAT3 inhibitor. Fluacrypyrim significantly increases the protein tyrosine phosphatases(PTPs) activity. Fluacrypyrim inhibits the growth of leukemia cells by a predominant G1 arrest with significant decrease of the protein and mRNA levels of cyclin D1. Fluacrypyrim selectively inhibits STAT3 signaling, inducing growth arrest and apoptosis in STAT3-dependent cancer cells. Fluacrypyrim mitigates IR-induced hematopoietic system injury mainly by preventing apoptosis in the HSCs. Fluacrypyrim demonstrates significant analgesic and anti-inflammatory effects by inhibiting uterine smooth muscle contraction and inflammatory responses .
Isosilybin B (Standard) is the analytical standard of Isosilybin B (HY-N7045). This product is intended for research and analytical applications. Isosilybin B is a flavonolignan. Isosilybin B can be isolated from Silybum marianum. Isosilybin B can regulate cell cycle-related proteins (e.g., reduce cyclins (D3, D1, A, E), Cdk4, Cdk2, Cdc25A), and activate Caspases(Caspase-9 and Caspase-3). Isosilybin B can promote Apoptosis, reduce androgen receptor (AR) and PSA. Isosilybin B has anticancer activity against prostate cancer .
Hsp90-Cdc37-IN-2 (Compound 41) is an inhibitor for the interaction between heat shock protein 90 (Hsp90) and cyclin 37 (Cdc37). Hsp90-Cdc37-IN-2 inhibits the proliferation of cancer cell A549, MCF-7, HOS and HepG2 with IC50 of 0.41-0.94 μM. Hsp90-Cdc37-IN-2 decreases the mitochondrial membrane potential, induces apoptosis, and arrest cell cycle at G0/G1 phase in A549 .
CST651 (PROTAC CDK4/6 degrader 34) is a selective cyclin dependent kinase CDK4/6 PROTAC degrader. CST651 can degrade CDK4 and CDK6 in MM.1S cells with DC50 values of 20 and 5.1 nM. CST651 can inhibit cancer cells proliferation and migration. CST651 can be used for the research of cancer, such as acute lymphoblastic leukemia . (Structure Note: Pink: CDK4/6 ligand (HY-50767); Blue: VHL ligand (HY-125905); Black: linker (HY-W017440))
Gomisin G (Standard) is the analytical standard of Gomisin G. This product is intended for research and analytical applications. Gomisin G is a lignin from S. chinesis with anti-HIV (EC50 = 0.006 μg/mL), anti-liver cancer and anti-inflammatory activities. Gomisin G has an AKT-cyclin D1 dependent mechanism against triple-negative breast cancer (TNBC) cells through suppressing phosphorylation rather than inducing apoptosis. Gomisin G can inhibit AKT phosphorylation. Gomisin G can cause cell cycle arrest in the G1 phase. Gomisin G can be studied in research for diseases such as HIV, breast and liver cancers .
SC-60 is a derivative of Sorafenib (HY-10201). SC-60 exerts its anti-tumor effect by activating the phosphatase activity of SHP-1, thereby inhibiting the STAT3 signaling pathway. SC-60 exhibits strong proliferation inhibitory activity in various hepatocellular carcinoma (HCC) cell lines. SC-60 downregulates the expression of downstream anti-apoptotic proteins (such as Bcl-2, Cyclin D1, Survivin), ultimately inducing caspase-dependent apoptosis. SC-60 significantly inhibits tumor growth in xenograft tumor models. SC-60 can be used for the study of HCC .
EGFR-IN-182 (Compound 4) is an EGFR inhibitor with an IC50 value of 199 nM. EGFR-IN-182 inhibits HSP90 and PI3K, with IC50 values of 5.007 and 13.596 μM respectively. EGFR-IN-182 exhibits strong anti-proliferative activity against MCF-7 and MDA-MB-231 cells. EGFR-IN-182 downregulates Cyclin D1, inducing cell cycle arrest; it enhances the activity of caspase-9, inducing cell apoptosis. EGFR-IN-182 downregulates the expressions of ERK and AKT. EGFR-IN-182 can be used for research on breast cancer .
(S)-(-)-Perillyl alcohol (Standard) is the analytical standard of (S)-(-)-Perillyl alcohol (HY-116514). This product is intended for research and analytical applications. (S)-(-)-Perillyl alcohol, a monoterpene, is an orally active farnesyl transferase and geranylgeranyl transferase inhibitor. (S)-(-)-Perillyl alcohol up-regulates the mannose-6-phosphate receptor, facilitating TGF-β1 activation and cytostasis,. (S)-(-)-Perillyl alcohol induces apoptosis in cancer cells, modulates cyclin D1 and AP-1 activity. (S)-(-)-Perillyl alcohol exhibits antitumor activity against sarcoma tumors in mice. (S)-(-)-Perillyl alcohol can be used for the research of squamous cell carcinoma of the esophagus and sarcoma 180.
Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt . Guggulsterone, a farnesoid X receptor (FXR) antagonist, with IC50s of 24.06 μM and 39.05 μM for (-)-(E)-Guggulsterone (HY-N7781) and (Z)-Guggulsterone (HY-110066), respectively .
Resibufogenin (Standard) is the analytical standard of Resibufogenin. This product is intended for research and analytical applications. Resibufogenin is an orally active anticancer agent. Resibufogenin can be extracted from toad venom. Resibufogenin blocks signaling pathways such as PI3K/Akt, NF-κB, AP-1, activates GSK-3β, and regulates cyclin D1. Resibufogenin can activate central neurons. Resibufogenin has anti-inflammatory activity. Resibufogenin has anti-tumor effects on a variety of tumors such as multiple myeloma, renal cancer, colorectal cancer, pancreatic cancer, and glioma [9].
Halcinonide (SQ-18566) is an orally active Smoothened (Smo) agonist. Halcinonide activates the Hedgehog signaling pathway by binding to Smo and promoting its internalization and expression, thereby activating Gli transcription factors. Halcinonide not only stimulates cell proliferation, increases the expression of cyclin D2/CDK6 and inhibits the degradation of caspase-3, but also suppresses Bcl-2/Bax-mediated apoptosis, oxidative stress and inflammatory responses. Halcinonide activates RxRγ to upregulate the expression of myelin genes, thereby reducing cerebral infarction and improving behavioral deficits. Halcinonide has been used in studies related to multiple sclerosis and ischemic stroke .
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 .
STAT3-IN-53 (Compound L20) is a STAT3 inhibitor with a Kd value of 6.16 μM. STAT3-IN-53 binds directly to the SH2 domain of STAT3, inhibits phosphorylation at the Y705 site without affecting the total STAT3 protein level, and suppresses the IL-6/JAK/STAT3 pathway. STAT3-IN-53 downregulates the transcription and expression of cyclin-D1 and c-Myc. STAT3-IN-53 induces cell cycle arrest and promotes Apoptosis. STAT3-IN-53 exhibits anticancer activity against colorectal cancer .
LC3B recruiter 2 (34R) is an LC3B recruiter and a component of the autophagy-lysosome pathway degradation system (ATTEC, Autophagy-Tethering Compounds), which directly binds to LC3B. LC3B recruiter 2 binds to CDK9 inhibitor SNS-032 (HY-10008) through a linker, forming an ATTEC that targets the degradation of the CDK9 and Cyclin T1 complex (with inhibitory effects on both). Therefore, LC3B recruiter 2 exerts activity through the LC3B-dependent autophagy-lysosome pathway, interfering with the cell cycle of cancer cells, thus exhibiting antitumor activity .
CDK2-IN-51 is a pyrazolopyridine derivative, a CDK2 inhibitor with an IC50 of 23.47 nM. CDK2-IN-51 does not have a pro-apoptotic effect and had no significant effect on CDK2 protein expression. CDK2-IN-51 reduces expression of DNA replication factors (Polα, MCM7, ORC2, and ORC4) and pre-G1 cell cycle arrest. CDK2-IN-51 can be used for the research of colorectal cancer .
P1D-34 is a Pin1PROTAC degrader with a DC50 value of 177 nM. P1D-34 also down-regulates Pin1 client proteins such as Cyclin D1, Rb, Mcl-1, Akt, and c-Myc. P1D-34 shows anti-proliferative activities in a panel of acute myeloid leukemia (AML) cell lines. P1D-34 induces cell DNA damage and apoptosis by releasing ROS generation. Pink: PIN1 ligand (HY-171442A), Blue: CRBN ligand (HY-14658), Black: Linker (HY-W014883) .
Guggulsterone (Standard) is the analytical standard of Guggulsterone (HY-107738). This product is intended for research and analytical applications. Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt. Guggulsterone, a farnesoid X receptor (FXR) antagonist, with IC50s of 24.06 μM and 39.05 μM for (-)-(E)-Guggulsterone (HY-N7781) and (Z)-Guggulsterone (HY-110066), respectively.
CDC20/HSP90-IN-1 (Compound 2b) is a Cdc20/Hsp90 inhibitor with a Kd of 16.2 μM for Cdc20 and a Kd of 0.241 μM for Hsp90α. CDC20/HSP90-IN-1 exerts potent antitumor activity through reducing p53-mediated Cdc20, upregulating Bim, downregulating Cyclin B1 expression, and disturbing B-Raf and AKT pathways via destroying Hsp90 chaperone function. CDC20/HSP90-IN-1 overcomes Vemurafenib (HY-12057)-induced resistant melanoma .
Sotetsuflavone is a flavonoid that can be isolated from Cycas revolute. Sotetsuflavone inhibits phosphorylation of PI3K, Akt, mTOR, JNK, and p38 MAPK; modulates expression of Cyclin D1, CDK4, Bcl-2, Bax, cleaved caspases 3/9, MMP-9, TGF-β, STAT3, and β-catenin. Sotetsuflavone induces G0/G1 cell cycle arrest, apoptosis, autophagy, and intracellular ROS elevation, inhibits cancer cell proliferation. Sotetsuflavone inhibits tumor growth in mouse tumor xenograft models. Sotetsuflavone can be used for the research of non-small cell lung cancer and Crohn’s disease .
DHI1 is an anti-leukemia agent with high selectivity for Jurkat (IC50 = 21.83 μM) and HL-60 (IC50 = 19.14 μM) leukemia cells and has low toxicity to non-cancerous cells. DHI1 can induce G2/M phase cell arrest in Jurkat and HL-60 leukemia cells, as well as S phase arrest in HL-60 cells, and has significant effects on cell cycle signaling molecules Wee1, cyclin B1, cdc2 on Tyr15, and Chk1. DHI1 inhibits the migration and invasion of Jurkat and HL-60 cells by disrupting cytoskeletal actin filaments. DHI1 can be used to study hematological malignancies .
CDK8-IN-20 (Compound 67j) is a selective, potent and orally active type I CDK8 inhibitor with an IC50 of 70.5 nM. CDK8-IN-20 shows IC50 values of 147.8, 726.9 and 217.4 nM for homologous kinase CDK19, CDK7 and CDK9. CDK8-IN-20 can inhibit the Wnt/β-catenin pathway and downregulate the expression of β-catenin, Cyclin D1, and c-Myc. CDK8-IN-20 can induce ROS production and cause G2/M and S phase arrest. CDK8-IN-20can be used for the research of cancer, such as colon cancer .
SY-5102 is a potent, selective and orally active cyclin-dependent kinase (CDK7) inhibitor with a Kd of 0.03 nM. SY-5102 shows anti-proliferative activity against HCC70 cells with an EC50 of 9 nM. SY-5102 can inhibit CDK7-mediated CAK function (downregulate CDK2 Thr160 phosphorylation) and TFIIH transcription function (downregulate RNA polymerase II Ser5 phosphorylation). SY-5102 can induce G2/M cell cycle arrest, downregulate the expression of the oncogene c-Myc, and ultimately trigger cancer cell apoptosis. SY-5102 can be used for the research of triple-negative breast cancer (TNBC) .
Anticancer agent 264 (Compound 5w) is an anticancer agent that exhibits significant antiproliferative activity across tumor cell lines, with an IC50 range of 7.5-33.67 μM.
Anticancer agent 264 significantly induces G2/M phase arrest in MDA-MB-231, MIA PaCa-2, and DU-145 cell lines.
Anticancer agent 264 reduces the expression of key cell cycle proteins, including CDK1, CDK2, and Cyclin B1, in a dose-dependent manner, and shows strong binding affinity with inhibitor of differentiation (ID) proteins and DNA-binding proteins.
Anticancer agent 264 can be used for research in the field of cancer-related diseases .
MPT0L145 is a PIK3C3/FGFR inhibitor, with a Kd value of 0.53 nM for PIK3C3. MPT0L145 decreases the phosphorylation of FGFR1, FGFR3 and their downstream proteins (FRS2, ERK and Akt). MPT0L145 induces G0/G1 cell cycle arrest and decreased protein levels of cyclin E. MPT0L145 promotes mitochondrial dysfunction, ROS production, and DNA damage. MPT0L145 is an autophagy inhibitor. MPT0L145 significantly sensitizes cancer cells to targeted or chemotherapeutic agents. MPT0L145 can be used for cancer research, such as bladder cancer and NSCLC .
WR-S-462 is a STAT3 inhibitor. WR-S-462 effectively suppresses STAT3 phosphorylation and biological functions in vitro. WR-S-462 inhibits MDA-MB-231 cells with an IC50 of 0.03 μM. WR-S-462 displays a strong binding affinity towards the STAT3 protein with a Kd of 58 nM. WR-S-462 inhibits the nuclear translocation of p-STAT3, selectively inhibits the expression of p-STAT3 Tyr705 and downstream target genes regulated by STAT3 in MDA-MB-231 cells such as Cyclin D1, Bcl-2, and Bcl-xl. WR-S-462 inhibits TNBC (triple-negative breast cancer) growth and metastasis .
Apcin-A is a small molecule inhibitor that selectively targets the cell division cycle protein Cdc20 and is a derivative of Apcin (HY-110287). Apcin-A competitively binds to the D-box binding pocket of Cdc20 and inhibits substrate ubiquitination mediated by the anaphase promoting complex APC/C-Cdc20. Apcin-A also blocks the binding of Cdc20 to substrates (such as securin and cyclin B1), inhibiting anaphase initiation and cell cycle exit. Apcin-A can promote or prolong mitotic slippage in coordination with p31 comet under conditions of high spindle assembly checkpoint (SAC) activity. Apcin-A can be used to develop anti-mitotic drugs and overcome tumor chemotherapy resistance. Apcin-A can be used to synthesize PROTAC CP5V (HY-130257)[1][2][3].
VMY-1-101 is a fluorescent cyclin-dependent kinase (CDK) inhibitor, with an excitation of 410 nm and emission of 512 nm. VMY-1-101 competitively inhibits ATP binding to CDKs. VMY-1-101 induces G2/M cell cycle arrest in human breast cancer cells. VMY-1-101 induces modest apoptosis in human breast cancer cells. VMY-1-101 blocks proliferation of human breast cancer cells, including multidrug resistance-positive cells, and is not a substrate for p-glycoprotein. VMY-1-101 localizes to the cytoplasm of human breast cancer cells. VMY-1-101 shows increased binding to human breast cancer tissue compared to fluorophore alone. VMY-1-101 can be used for the research of breast cancer .
HER4/HER2-IN-1 (Compound 4b) is a HER4/HER2 inhibitor. HER4/HER2-IN-1 inhibits the proliferation of HER2-positive cells. HER4/HER2-IN-1 reduces the total expression level of HER2 in A431 cells, while the phosphorylated HER2 (p-HER2) does not decrease. HER4/HER2-IN-1 lowers the level of cell cycle protein D1 (cyclin D1) and stimulates the cleavage of PARP. HER4/HER2-IN-1 can be used for the study of cancer, such as breast cancer .
FPP29 is a potent peptide-based FOXM1PROTAC degrader. FPP29 induces ubiquitination and degradation of FOXM1. FPP29 inhibits FOXM1 via the ubiquitin-proteasome degradation pathway. FPP29 induces Apoptosis. FPP29 suppresses tumor growth in hepatocellular carcinoma xenograft models. FPP29 can be used in the research of hepatocellular carcinoma (cell-penetrating peptide: (HY-P0133); VHL ligase ligand: (HY-P11493); linker: (HY-W013664); FOXM1 ligand: (HY-P11494)) .
PROTAC CDK2-pRb degrader-1 is an orally active PROTAC-class degrader of CDK2. PROTAC CDK2-pRb degrader-1 effectively inhibits the phosphorylation of retinoblastoma protein (Rb) at serine residues 807/811 by inducing ubiquitination and proteasomal degradation of CDK2. PROTAC CDK2-pRb degrader-1 exhibits significant activity against human cells (with EC50 values of 12 nM and 125 nM, respectively). In xenograft models, PROTAC CDK2-pRb degrader-1 effectively inhibits tumor growth and induces tumor stasis, making it suitable for research related to CCNE1-amplified cancers (such as ovarian cancer, gastric cancer, and breast cancer) .
Rafutrombopag (tautomerism) (Hetrombopag) is an orally active nonpeptide thrombopoietin receptor (TPOR/MPL) agonist. Rafutrombopag can chelate iron and alleviate iron overload while promoting haematopoiesis. Rafutrombopag specifically stimulates proliferation and differentiation of human TPOR‐expressing cells, including 32D‐ MPL and human hematopoietic stem cells through stimulation of STAT, PI3K and ERK signalling pathways. Rafutrombopag effectively up-regulates G1-phase-related proteins, including p-RB, Cyclin D1 and CDK4/6, normalizes progression of the cell cycle, and prevents apoptosis by modulating BCL-XL/BAK expression in 32D-MPL cells. Rafutrombopag protects cardiomyocyte survival from oxidative stress damage as an enhancer of stem cells. Rafutrombopag can be used for the study of immune thrombocytopenia and oxidative stress-related cardiovascular disease .
Sorafenib (Bay 43-9006) is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib inhibits tumor growth and metastasis in mouse and rat models. Sorafenib can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma .
Rafutrombopag (Hetrombopag) is an orally active nonpeptide thrombopoietin receptor (TPOR/MPL) agonist. Rafutrombopag can chelate iron and alleviate iron overload while promoting haematopoiesis. Rafutrombopag specifically stimulates proliferation and differentiation of human TPOR-expressing cells, including 32D-MPL and human hematopoietic stem cells through stimulation of STAT, PI3K and ERK signalling pathways. Rafutrombopag effectively up-regulates G1-phase-related proteins, including p-RB, Cyclin D1 and CDK4/6, normalizes progression of the cell cycle, and prevents apoptosis by modulating BCL-XL/BAK expression in 32D-MPL cells. Rafutrombopag protects cardiomyocyte survival from oxidative stress damage as an enhancer of stem cells. Rafutrombopag can be used for the study of immune thrombocytopenia and oxidative stress-related cardiovascular disease .
PROTAC FLT3/CDKs degrader-1 (Compound C3) is a degrader for cyclin-dependent kinases (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))
Apoptosis inducer 50 (Compound 5e) is an apoptosis inducer as well as an autophagy inducer agent. Apoptosis inducer 50 exhibits potent and selective anti-cancer activity against triple-negative breast cancer cells and metastatic colon cancer cells. Apoptosis inducer 50 upregulates the expression of pro-apoptotic proteins (Bax, Bim, cleaved Caspase-9) and downregulates the expression of the anti-apoptotic protein (BCL-XL). Apoptosis inducer 50 upregulates key autophagy markers such as Beclin-1 and ATG5, and enhances the conversion of LC3-I to LC3-II., Apoptosis inducer 50 arrests cancer cells in the G1/S phase by upregulating the expression of p21 and p27 while downregulating Cyclin D1. Apoptosis inducer 50 increases the level of ROS .
Sorafenib (Bay 43-9006) tosylate is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib tosylate induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib tosylate inhibits tumor growth and metastasis in mouse and rat models. Sorafenib tosylate can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma .
Nur77 modulator 6 is a Nur77 modulator with a Kd of 0.40 μM. Nur77 modulator 6 functionally modulates Nur77 to induce mitotic arrest and apoptosis in colorectal tumor cells. Nur77 modulator 6 suppresses colorectal cancer cell proliferation via Nur77-dependent mitotic arrest induction. Nur77 modulator 6 exhibits anti-proliferative activity against colorectal tumor cells. Nur77 modulator 6 can be used for the research of colorectal cancer .
OKI-005 is an orally active inhibitor of Class I HDACs, with primary targeting of HDAC1, HDAC2 and HDAC3. OKI-005 is a prodrug of OKI-006 (HY-144893). OKI-005 increases histone acetylation levels, induces apoptosis and inhibits cancer cell proliferation. OKI-005 can be used in research related to triple-negative breast cancer and colorectal cancer .
Cyproheptadine hydrochloride sesquihydrate acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine hydrochloride sesquihydrate mediates cell cycle arrest via G1 phase arrest, G1/S transition arrest, G0/G1 phase arrest, reduced expression of cyclinsD1/D2/D3, upregulated expression of HBP1, p16, p21, p27, and decreased phosphorylation of retinoblastoma protein. Cyproheptadine hydrochloride sesquihydrate induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine hydrochloride sesquihydrate inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine hydrochloride sesquihydrate can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia .
BRD4/AKT-IN-1 is a BRD4/AKT inhibitor with BRD4IC50 66.12 nM and AKT1IC50 143.81 nM. BRD4/AKT-IN-1 blocks BRD4-mediated c-Myc transcriptional regulation, modulates AKT1 signaling, decouples AKT phosphorylation from pro-survival effectors. BRD4/AKT-IN-1 induces G0/G1 cell cycle arrest via downregulated phosphorylated RB, cyclin E1, CDK2. BRD4/AKT-IN-1 elevates LC3B levels to promote autophagy. BRD4/AKT-IN-1 promotes apoptosis in cancer cells. BRD4/AKT-IN-1 can be used for the research of metastatic castration-resistant prostate cancer .
S-Petasin is a phosphodiesterase (PDE) inhibitor with IC50 values of 25.5 μM and 17.5 μM for PDE3 and PDE4, respectively. S-Petasin inhibits cholesterol side-chain cleavage enzyme, 11β-hydroxylase, PPAR-γ, and iNOS induction at RNA and protein levels. S-Petasin induces apoptosis, activates caspases, cleaves PARP, modulates mitochondrial membrane permeability, and regulates BCL2/BAX, p53, Bcl-XL, MMP-2, MMP-9, p21, CDK4, and cyclin D1 expression. S-Petasin reduces inflammatory cell accumulation, cytokine and IgE levels, and enhances serum IgG2a levels. S-Petasin relaxes isolated sensitized guinea pig trachealis and exhibits gastrointestinal anti-spasmodic activity. S-Petasin reduces tonsillitis severity and asthmatic attack frequency. S-Petasin can be used for the research of prostate cancer, obesity, melanoma, allergic asthma, asthma, and peritonitis .
EGFR-IN-212 is an EGFR inhibitor with human IC50 values of 1.83 μM. EGFR-IN-212 reduces EGFR mRNA expression and induces apoptosis. EGFR-IN-212 can be used for the research of non-small cell lung carcinoma .
Secoxyloganin is an orally effective iridoid derivative. Secoxyloganin can be isolated from the flower buds of L. japonica. Secoxyloganin induces Apoptosis by inhibiting the expression of Bcl-2. Secoxyloganin potently inhibits the proliferation of breast cancer cells, while exerting weak activity against normal mammary epithelial cells. Secoxyloganin inhibits the decrease in tail vein blood flow associated with allergic reactions .
CDK2/4/6-IN-2 is a selective CDK2/4/6 inhibitor with IC50 values <1 μM. CDK2/4/6-IN-2 inhibits cells proliferation and phosphorylation of retinoblastoma protein at Ser807/811 in breast cancer cells. CDK2/4/6-IN-2 can be used for the research of cancer, such as breast cancer .
HRV-3C protease fuses with GST is a recombinant protease fused with HRV-3C protease and GST, which recognizes the LEVLFQGP polypeptide sequence. HRV-3C protease fuses with GST precisely cleaves between glutamine and glycine-proline residues to remove fusion tags from target proteins. HRV-3C protease fuses with GST exhibits cleavage activity both in vitro in silkworm fat body lysates and in vivo in silkworm larval fat bodies, and achieves functional expression in E. coli and silkworm-baculovirus expression systems. HRV-3C protease fuses with GST can be applied to recombinant protein-related research .
CDK2 degrader 3 is a selective CDK2 molecular glue-like degrader. CDK2 degrader 3 induces G1 cell cycle arrest in CCNE1-amplified cancer cells. CDK2 degrader 3 is applicable to breast cancer-related research .
CDK8-IN-2 is an orally active CDK8 inhibitor of an IC50 values of 0.010 μM. CDK8-IN-2 shows a CDK19IC50 value of 0.026 μM. CDK8-IN-2 inhibits phospho-STAT1, a pharmacodynamic biomarker of CDK8. CDK8-IN-2 inhibits WNT pathway activity. CDK8-IN-2 can be used for the research of colorectal carcinoma .
UNC-CA359 is a potent epidermal growth factor receptor (EGFR) inhibitor, with an IC50 value of 18 nM. UNC-CA359 exhibits strong anti-tumor activity, can be used to Chordoma research . UNC-CA359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
DHQZ-17 is a HNF4A inhibitor. DHQZ-17 triggers apoptosis in head and neck squamous cell carcinoma cells. DHQZ-17 can be used for the research of head & neck squamous cell carcinoma .
(10E,12Z)-Octadeca-10,12-dienoic acid (trans-10,cis-12 CLA2) is an orally active PPARα activator and inhibits adipocyte differentiation. (10E,12Z)-Octadeca-10,12-dienoic acid and its downstream metabolites have various antioxidant and antitumor activities. (10E,12Z)-Octadeca-10,12-dienoic acid can induce proinflammatory cytokines and chemokines, which would lead to decreased adipogenesis and insulin resistance in adipose tissue. (10E,12Z)-Octadeca-10,12-dienoic acid can affect many aspects of milk fat synthesis. (10E,12Z)-Octadeca-10,12-dienoic acid reduces expression of lipogenic enzymes and inhibits the desaturation of fatty acids. (10E,12Z)-Octadeca-10,12-dienoic acid can reduce lipoprotein lipase (LPL) activity in cultured 3T3-L1 adipocytes and enhance triacylglycerol release from these cells. (10E,12Z)-Octadeca-10,12-dienoic acid decreases the expression of hepatic stearoyl-CoA desatyrase mRNA in mice. (10E,12Z)-Octadeca-10,12-dienoic acid is associated with changes in mucosal NF-κB and Cyclin D1 protein levels in mice .
SF-3-030 is a potent, selective and non-ATP competitive ERK1/2 inhibitor. SF-3-030 selectively induces apoptosis in melanoma cells containing mutated BRaf and constitutively active ERK1/2 signalling. SF-3-030 mitigates multiple features of asthma in a murine model of asthma. SF-3-030 can be used for the research of asthma and melanomasup .
Zinc (Zinc (II)) acetate, 99.99% trace metals basis is a heme oxygenase 1 (HO-1) activator and apoptosis inducer with cytotoxic and anticancer activities. Zinc acetate, 99.99% trace metals basis enhances HO-1 expression, alters the microRNA profile, and increases the level of caspase-cleaved cytokeratin 18. Zinc acetate, 99.99% trace metals basis also regulates the expression of Cdk2/cyclin E and interferes with cell cycle progression. Zinc acetate, 99.99% trace metals basis effectively inhibits cancer cell proliferation and induces their rapid death, with no significant cytotoxicity to non-tumor tissues. Zinc acetate, 99.99% trace metals basis has been widely used in studies related to hepatocellular carcinoma, prostate cancer, and other conditions .
FPP29 is a potent peptide-based FOXM1PROTAC degrader. FPP29 induces ubiquitination and degradation of FOXM1. FPP29 inhibits FOXM1 via the ubiquitin-proteasome degradation pathway. FPP29 induces Apoptosis. FPP29 suppresses tumor growth in hepatocellular carcinoma xenograft models. FPP29 can be used in the research of hepatocellular carcinoma (cell-penetrating peptide: (HY-P0133); VHL ligase ligand: (HY-P11493); linker: (HY-W013664); FOXM1 ligand: (HY-P11494)) .
[Ala92]-p16 (84-103) is a peptide derived from the p16CDKN2/INK4a (p16) tumor suppressor protein. [Ala92]-p16 (84-103) binds to both cdk4 and cdk6 and inhibits cdk4-cyclin D1 kinase activity in vitro (IC50: 1.5 μM). [Ala92]-p16 (84-103) blocks cell cycle progression through the G1 phase .
Cdc2 kinase substrate is a biological active peptide. (The native peptide HATPPKKKRK is a substrate for cyclin-dependent protein kinase 1 (CDC2; CDK1).)
[pSer2, pSer5, pSer7]-CTD, 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) .
TAT-p16 (p16INK4a peptide) is a peptide mimic of p16INK4a that can induce an early G phase cell cycle arrest in the absence of active cyclin E:Cdk2 complex .
Cdc25A (80-93) (human) is a polypeptide that controls the cell proliferation and tumorigenesis by a change in expression of proteins involved in cyclin D1 regulation and G1/S transition. Cdc25A (80-93) (human) can be used in cancer research .
[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) .
GTGKT is a CAGE inhibitor. GTGKT binds to CAGE and blocks the binding of CAGE to GSK3β. GTGKT alters the localization of CAGE and inhibits the binding of CAGE to the promoter sequence of Cyclin D1. GTGKT enhances the Apoptotic effect of anticancer agents. GTGKT reduces the expression of Cyclin D1. GTGKT decreases the tumorigenic potential of melanoma and hepatocellular carcinoma cells .
MCE BM-Cyclin mainly contains Tiamulin fumarate and Minocycline hydrochloride, can effectively inhibit and remove mycoplasma contamination widespread in cell cultures. It is also effective against some common bacteria.
Metuzumab (Licartin) is a human-mouse chimeric IgG1 monoclonal antibody targeting CD147. Metuzumab induces Apoptosis, reduces levels of Cyclin D1, full-length Caspase-3, and Bcl-2, and increases Bax expression. Metuzumab enhances the sensitivity of non-small cell lung cancer (NSCLC) cells to Gemcitabine (HY-17026). Metuzumab is applicable for research on hepatocellular carcinoma and non-small cell lung cancer [1][2].
9-cis-Retinoic acid (ALRT1057), a vitamin A derivative, is a potent RAR/RXR agonist. 9-cis-Retinoic acid induces apoptosis, regulates cell cycle and has anticancer, anti-inflammatory and neuroprotection activities .
Eriocitrin is a flavonoid isolated from lemons that is a powerful antioxidant. Eriocitrin inhibits the proliferation of liver cancer cells by arresting the cell cycle in the S phase by upregulating p53, cyclin A, cyclin D3 and CDK6. Eriocitrin triggers apoptosis by activating intrinsic signaling pathways involving mitochondria .
Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt . Guggulsterone, a farnesoid X receptor (FXR) antagonist, with IC50s of 24.06 μM and 39.05 μM for (-)-(E)-Guggulsterone (HY-N7781) and (Z)-Guggulsterone (HY-110066), respectively .
Arctiin is an orally active inhibitor of NF-κB. Arctiin suppresses cyclin D1 protein expression in human tumor cells. Arctiin also reduces malondialdehyde and pro-in ammatory cytokines levels. Arctiin can used in study glomerulonephritis .
Decursin ((+)-Decursin) is a potent anti-tumor agent. Decursin also is a cytotoxic agent and a potent protein kinase C activator. Decursin induces apoptosis and cell cycle arrest at G1 phase. Decursin decreases the expression of CDK2, CDK4, CDK6, cyclin D1 protein at 48 h. Decursin inhibits cell proliferation and migration. Decursin shows anti-tumor, anti-inflammatory and analgesic activities .
Resibufogenin is an orally active anticancer agent. Resibufogenin can be extracted from toad venom. Resibufogenin blocks signaling pathways such as PI3K/Akt, NF-κB, AP-1, activates GSK-3β, and regulates cyclin D1. Resibufogenin can activate central neurons. Resibufogenin has anti-inflammatory activity. Resibufogenin has anti-tumor effects on a variety of tumors such as multiple myeloma, renal cancer, colorectal cancer, pancreatic cancer, and glioma [9].
Flavone is an anti-tumor compound that targets cell cycle regulatory proteins (such as cyclin B1) and apoptosis-related factors (such as p21waf1, PIG3). Flavone selectively induces mitochondrial-mediated apoptosis pathways in tumor cells, inhibits cyclin B1 protein expression, upregulates p21waf1, and activates p63/p73 proteins. Flavone has immunomodulatory functions that enhance natural killer cell (NK cell) activity and lymphocyte proliferation. Flavone is used in cancer research, especially for its inhibitory potential in solid tumor models such as esophageal cancer and liver cancer .
Epmedin C (Epimedin-C; Baohuoside-VI) is an orally active anti-inflammatory agent and immunomodulator that binds to multiple key proteins including UCP1, Caspase-1, CDK2 and Keap1. Epmedin C inhibits epithelial cell proliferation by disrupting the complex function of CDK2/Cyclin E. Epmedin C also upregulates Nrf2 expression, reduces ROS levels and inhibits pro-inflammatory cytokine secretion, thereby effectively restoring antibody production and alleviating tissue damage. Epmedin C has good safety with no hepatotoxicity or skin sensitization, and it has been used in studies on diseases such as obesity, Deoxynivalenol (HY-N6684)-induced immunotoxicity and mammary hyperplasia .
Cucurbitacin E is a CDK1 inhibitor that significantly inhibits the activity of the cyclin B1/CDC2 complex. Cucurbitacin E also induces PANoptosis in adrenocortical carcinoma cells in a ZBP1-dependent manner. Cucurbitacin E exhibits synergistic effects with Mitotane (HY-13690); when used in combination, they effectively eliminate tumors .
Lacto-N-fucopentaose I (LNFPI) is a human milk oligosaccharide (HMO), possessing antiviral and antibacterial activity. Lacto-N-fucopentaose I can reduce capsid protein VP1 to block virus adsorption, promote CDK2 and reduce cyclin E to recover cell cycle S phase block. Lacto-N-fucopentaose I inhibits ROS production and apoptosis in virus-infected cells. Lacto-N-fucopentaose I can also regulate intestinal microbiota to affect immune system development .
Arcyriaflavin A is an indolo[2,3-a]carbazole compound and also a cyclin D1/CDK4 inhibitor. Arcyriaflavin A exists in the marine ascidian Eudistoma sp. and the slime mold Arcyria denudata. Arcyriaflavin A is applicable to research related to colon cancer and lung cancer .
Eurycomalactone is an active quassinoid could be isolated from Eurycoma longifolia Jack. Eurycomalactone is a potent NF-κB inhibitor with an IC50 value of 0.5 μM. Eurycomalactone inhibits protein synthesis and depletes cyclin D1. Eurycomalactone enhances radiosensitivity through arrest cell cycle at G2/M phase and delayed DNA double-strand break repair. Eurycomalactone inhibits the activation of AKT/NF-κB signaling, induces apoptosis and enhances chemosensitivity to Cisplatin (HY-17394) .
(S)-(-)-Perillyl alcohol, a monoterpene, is an orally active farnesyl transferase and geranylgeranyl transferase inhibitor. (S)-(-)-Perillyl alcohol up-regulates the mannose-6-phosphate receptor, facilitating TGF-β1 activation and cytostasis,. (S)-(-)-Perillyl alcohol induces apoptosis in cancer cells, modulates cyclin D1 and AP-1 activity. (S)-(-)-Perillyl alcohol exhibits antitumor activity against sarcoma tumors in mice. (S)-(-)-Perillyl alcohol can be used for the research of squamous cell carcinoma of the esophagus and sarcoma 180 .
Garcinone D is an activator of the STAT3/Cyclin D1 and Nrf2/HO-1 pathways, and an inhibitor of CDK2/CyclinE1 (IC50 for CDK2/CyclinE1 is 28.23 μM). Garcinone D promotes neural stem cell proliferation by activating STAT3 phosphorylation and Cyclin D1 expression and enhancing the Nrf2/HO-1 signaling pathway. In addition, Garcinone D blocks the tumor cell cycle by inhibiting CDK2/CyclinE1. Garcinone D can promote the proliferation of C17.2 neural stem cells and inhibit prostate and breast cancer .
Isosilybin B is a flavonolignan. Isosilybin B can be isolated from Silybum marianum. Isosilybin B can regulate cell cycle-related proteins (e.g., reduce cyclins (D3, D1, A, E), Cdk4, Cdk2, Cdc25A), and activate Caspases(Caspase-9 and Caspase-3). Isosilybin B can promote Apoptosis, reduce androgen receptor (AR) and PSA. Isosilybin B has anticancer activity against prostate cancer .
Gomisin G is a lignin from S. chinesis with anti-HIV (EC50 = 0.006 μg/mL), anti-liver cancer and anti-inflammatory activities. Gomisin G has an AKT-cyclin D1 dependent mechanism against triple-negative breast cancer (TNBC) cells through suppressing phosphorylation rather than inducing apoptosis. Gomisin G can inhibit AKT phosphorylation. Gomisin G can cause cell cycle arrest in the G1 phase. Gomisin G can be studied in research for diseases such as HIV, breast and liver cancers .
β,β-Dimethylacrylalkannin (Arnebin 1) is an orally active FGFR1 inhibitor (IC50=2.5 μM) and the main active component of Lithospermum erythrorhizon. β,β-Dimethylacrylalkannin blocks downstream signaling by binding to the ATP pocket of FGFR1, and regulates the CDK1/Cdc25C pathway and ROS-JNK axis, thereby inducing G2/M phase arrest, necrosis and apoptosis in cancer cells, and inhibiting tumor proliferation. β,β-Dimethylacrylalkannin also acts as a colistin adjuvant to disrupt the cell membrane of Gram-negative bacteria. β,β-Dimethylacrylalkannin exhibits significant tumor-inhibitory effects with no obvious toxicity in PDX models, but chronic exposure to high doses may alter the relative lung/liver weights of rats, while acute exposure to high doses causes responses such as reduced motor activity. β,β-Dimethylacrylalkannin finds wide application in studies related to hepatocellular carcinoma, colorectal cancer, colistin-resistant bacterial infections, hepatitis and psoriasis .
Licoisoflavone A is an orally active isoflavone. Licoisoflavone A inhibits proliferation, induces apoptosis, and causes G1/S phase arrest in colorectal cancer (CRC) cells. Licoisoflavone A inhibits the CDK2-CyclinE1 axis. Licoisoflavone A inhibits lipid peroxidation with an IC50 of 7.2 μM. Licoisoflavone A shows a dose-dependent inhibition effect on SARS-CoV-2 infection. Licoisoflavone A exhibits significant anti-tumor efficacy in mice bearing CT26 cell subcutaneous xenografts. Licoisoflavone A can be used for the study of colorectal cancer and SARS-CoV-2 infection .
1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC (PC(18:0/22:4)) is an inhibitor of cyclin-dependent kinases (CDKs). 1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC induces apoptosis and inhibits the growth of various cancer cell lines .
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 .
Yatein is a lignan isolated from A. chilensis, with antiproliferative activity . Yatein suppresses herpes simplex virus type 1 (HSV-1 ) replication by interruption the immediate-early gene expression .
Secoxyloganin is an orally effective iridoid derivative. Secoxyloganin can be isolated from the flower buds of L. japonica. Secoxyloganin induces Apoptosis by inhibiting the expression of Bcl-2. Secoxyloganin potently inhibits the proliferation of breast cancer cells, while exerting weak activity against normal mammary epithelial cells. Secoxyloganin inhibits the decrease in tail vein blood flow associated with allergic reactions .
Eriocitrin (Standard) is the analytical standard of Eriocitrin. This product is intended for research and analytical applications. Eriocitrin is a flavonoid isolated from lemons that is a powerful antioxidant. Eriocitrin inhibits the proliferation of liver cancer cells by arresting the cell cycle in the S phase by upregulating p53, cyclin A, cyclin D3 and CDK6. Eriocitrin triggers apoptosis by activating intrinsic signaling pathways involving mitochondria .
(-)-Hinesol (Hinesol) is a potent anticancer agent. (-)-Hinesol induces apoptosis and cell cycle arrest at G0/G1 phase. (-)-Hinesol downregulates MEK/ERK pathway and NF-κB pathway and mediates theexpression of cyclin D1, Bax and Bcl-2. (-)-Hinesol has the potential for the research of non–small cell lung cancer .
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 .
Cucurbitacin E (Standard) is the analytical standard of Cucurbitacin E. This product is intended for research and analytical applications. Cucurbitacin E is a natural compound which from Cucurbitaceae plants. Cucurbitacin E significantly suppresses the activity of the cyclin B1/CDC2 complex.
Ascochlorin (Ilicicolin D), an isoprenoid antibiotic, mediates its anti-tumor effects predominantly through the suppression of STAT3 signaling cascade. Ascochlorin induces apoptosis. Anti-inflammatory activity .
Hexamethylquercetagetin (Hexa-O-methylquercetagetin; Quercetagetin hexamethyl ether; 3,5,6,7,3',4'-Hexamethoxyflavone) is an orally active NF-κB inhibitor. Hexamethylquercetagetin inhibits NF-κB-derived luciferase activity, reduces phosphorylated p65 and IκBα, Cyclin D1, Bcl-2 and blocks TNFα-induced NF-κB activation. Hexamethylquercetagetin inhibits survival and proliferation of cervical carcinoma cells. Hexamethylquercetagetin suppresses tumor volume and weight in BALB/c nude mouse xenograft models of cervical carcinoma. Hexamethylquercetagetin can be used for the research of cancer, such as cervical carcinoma .
Guggulsterone (Standard) is the analytical standard of Guggulsterone (HY-107738). This product is intended for research and analytical applications. Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt. Guggulsterone, a farnesoid X receptor (FXR) antagonist, with IC50s of 24.06 μM and 39.05 μM for (-)-(E)-Guggulsterone (HY-N7781) and (Z)-Guggulsterone (HY-110066), respectively.
Sotetsuflavone is a flavonoid that can be isolated from Cycas revolute. Sotetsuflavone inhibits phosphorylation of PI3K, Akt, mTOR, JNK, and p38 MAPK; modulates expression of Cyclin D1, CDK4, Bcl-2, Bax, cleaved caspases 3/9, MMP-9, TGF-β, STAT3, and β-catenin. Sotetsuflavone induces G0/G1 cell cycle arrest, apoptosis, autophagy, and intracellular ROS elevation, inhibits cancer cell proliferation. Sotetsuflavone inhibits tumor growth in mouse tumor xenograft models. Sotetsuflavone can be used for the research of non-small cell lung cancer and Crohn’s disease .
Arctiin (Standard) is the analytical standard of Arctiin. This product is intended for research and analytical applications. Arctiin is an orally active inhibitor of NF-κB. Arctiin suppresses cyclin D1 protein expression in human tumor cells. Arctiin also reduces malondialdehyde and pro-in?ammatory cytokines levels. Arctiin can used in study glomerulonephritis .
Garcinone D (Standard) is the analytical standard of Garcinone D (HY-N6953). This product is intended for research and analytical applications. Garcinone D is an activator of the STAT3/Cyclin D1 and Nrf2/HO-1 pathways, and an inhibitor of CDK2/CyclinE1 (IC50 for CDK2/CyclinE1 is 28.23 μM). Garcinone D promotes neural stem cell proliferation by activating STAT3 phosphorylation and Cyclin D1 expression and enhancing the Nrf2/HO-1 signaling pathway. In addition, Garcinone D blocks the tumor cell cycle by inhibiting CDK2/CyclinE1. Garcinone D can promote the proliferation of C17.2 neural stem cells and inhibit prostate and breast cancer .
Lenoremycin (Ro 21-6150) is a microbial metabolite. Lenoremycin decreases β-catenin and cyclin D1 proteins levels. Lenoremycin decreases cancer stem cells (CSCs) populations via inducing reactive oxygen species production .
Epmedin C (Standard) is the analytical standard of Epmedin C. This product is intended for research and analytical applications. Epmedin C (Epimedin-C; Baohuoside-VI) is an orally active anti-inflammatory agent and immunomodulator that binds to multiple key proteins including UCP1, Caspase-1, CDK2 and Keap1. Epmedin C inhibits epithelial cell proliferation by disrupting the complex function of CDK2/Cyclin E. Epmedin C also upregulates Nrf2 expression, reduces ROS levels and inhibits pro-inflammatory cytokine secretion, thereby effectively restoring antibody production and alleviating tissue damage. Epmedin C has good safety with no hepatotoxicity or skin sensitization, and it has been used in studies on diseases such as obesity, Deoxynivalenol (HY-N6684)-induced immunotoxicity and mammary hyperplasia .
Decursin (Standard) is the analytical standard of Decursin. This product is intended for research and analytical applications. Decursin ((+)-Decursin) is a potent anti-tumor agent. Decursin also is a cytotoxic agent and a potent protein kinase C activator. Decursin induces apoptosis and cell cycle arrest at G1 phase. Decursin decreases the expression of CDK2, CDK4, CDK6, cyclin D1 protein at 48 h. Decursin inhibits cell proliferation and migration. Decursin shows anti-tumor, anti-inflammatory and analgesic activities [4].
9-cis-Retinoic acid (Standard) is the analytical standard of 9-cis-Retinoic acid. This product is intended for research and analytical applications. 9-cis-Retinoic acid (ALRT1057), a vitamin A derivative, is a potent RAR/RXR agonist. 9-cis-Retinoic acid induces apoptosis, regulates cell cycle and has anticancer, anti-inflammatory and neuroprotection activities[1][2][3][4][5].
Isosilybin B (Standard) is the analytical standard of Isosilybin B (HY-N7045). This product is intended for research and analytical applications. Isosilybin B is a flavonolignan. Isosilybin B can be isolated from Silybum marianum. Isosilybin B can regulate cell cycle-related proteins (e.g., reduce cyclins (D3, D1, A, E), Cdk4, Cdk2, Cdc25A), and activate Caspases(Caspase-9 and Caspase-3). Isosilybin B can promote Apoptosis, reduce androgen receptor (AR) and PSA. Isosilybin B has anticancer activity against prostate cancer .
Resibufogenin (Standard) is the analytical standard of Resibufogenin. This product is intended for research and analytical applications. Resibufogenin is an orally active anticancer agent. Resibufogenin can be extracted from toad venom. Resibufogenin blocks signaling pathways such as PI3K/Akt, NF-κB, AP-1, activates GSK-3β, and regulates cyclin D1. Resibufogenin can activate central neurons. Resibufogenin has anti-inflammatory activity. Resibufogenin has anti-tumor effects on a variety of tumors such as multiple myeloma, renal cancer, colorectal cancer, pancreatic cancer, and glioma [9].
Gomisin G (Standard) is the analytical standard of Gomisin G. This product is intended for research and analytical applications. Gomisin G is a lignin from S. chinesis with anti-HIV (EC50 = 0.006 μg/mL), anti-liver cancer and anti-inflammatory activities. Gomisin G has an AKT-cyclin D1 dependent mechanism against triple-negative breast cancer (TNBC) cells through suppressing phosphorylation rather than inducing apoptosis. Gomisin G can inhibit AKT phosphorylation. Gomisin G can cause cell cycle arrest in the G1 phase. Gomisin G can be studied in research for diseases such as HIV, breast and liver cancers .
(S)-(-)-Perillyl alcohol (Standard) is the analytical standard of (S)-(-)-Perillyl alcohol (HY-116514). This product is intended for research and analytical applications. (S)-(-)-Perillyl alcohol, a monoterpene, is an orally active farnesyl transferase and geranylgeranyl transferase inhibitor. (S)-(-)-Perillyl alcohol up-regulates the mannose-6-phosphate receptor, facilitating TGF-β1 activation and cytostasis,. (S)-(-)-Perillyl alcohol induces apoptosis in cancer cells, modulates cyclin D1 and AP-1 activity. (S)-(-)-Perillyl alcohol exhibits antitumor activity against sarcoma tumors in mice. (S)-(-)-Perillyl alcohol can be used for the research of squamous cell carcinoma of the esophagus and sarcoma 180.
Americanin A is a Neolignan. Americanin A can be isolated from the seeds of Phytolacca americana. Americanin A activates ATM and ATR, initiating the subsequent signal transduction cascades that include Chk1, Chk2, and tumor suppressor p53. Americanin A targets selectively Skp2 for degradation and thereby stabilizes p27. Americanin A suppresses the activity of Cyclin B1 and its partner cdc2 to prevent entry into Mitosis. Americanin A induces Apoptosis by producing excessive ROS. Americanin A has anti-cancer activity against colorectal cancer .
12-Deoxyphorbol 13-palmitate is a traditional Chinese medicine monomer with antitumor activity that can be isolated from the root of Euphorbia fischeriana. 12-Deoxyphorbol 13-palmitate induces gastric cancer cell cycle arrest and apoptosis by regulating key cell cycle regulators such as cyclinB、cyclin A and CDC2. In addition, 12-Deoxyphorbol 13-palmitate can significantly weaken APOL2–SERCA2–PERK–HES1 signaling and slow liver fibrosis by targeting APOL2 .
Butrin is a compound found in Butea monosperma flowers. Butrin reduces expression of SIRT1, AURKB, cyclin D1, pAKT, GSK-3β, β-catenin, and TGF-3β expression, enhances apoptosis and ROS production in cancer cells. Butrin downregulates Wnt and NF-κB signaling, mitigates oxidative stress, reduces proinflammatory cytokine (TNF-α, IL-6 and IL-8) production and suppresses neuroinflammation. Butrin inhibits IKK enzyme activity. Butrin can be used for the researches of colorectal cancer, Alzheimer’s disease, and rheumatoid arthritis .
S-Petasin is a phosphodiesterase (PDE) inhibitor with IC50 values of 25.5 μM and 17.5 μM for PDE3 and PDE4, respectively. S-Petasin inhibits cholesterol side-chain cleavage enzyme, 11β-hydroxylase, PPAR-γ, and iNOS induction at RNA and protein levels. S-Petasin induces apoptosis, activates caspases, cleaves PARP, modulates mitochondrial membrane permeability, and regulates BCL2/BAX, p53, Bcl-XL, MMP-2, MMP-9, p21, CDK4, and cyclin D1 expression. S-Petasin reduces inflammatory cell accumulation, cytokine and IgE levels, and enhances serum IgG2a levels. S-Petasin relaxes isolated sensitized guinea pig trachealis and exhibits gastrointestinal anti-spasmodic activity. S-Petasin reduces tonsillitis severity and asthmatic attack frequency. S-Petasin can be used for the research of prostate cancer, obesity, melanoma, allergic asthma, asthma, and peritonitis .
Cyclin A1 protein is a key regulator in the cell cycle, affecting G1/S and G2/M transitions and playing a major role in the germline meiotic cell cycle. It interacts with CDK2 and CDC2 kinase to form a holoenzyme complex that participates in the regulatory pathways of E2F-1 and RB proteins. Cyclin A1 Protein, Human (sf9, His) is the recombinant human-derived Cyclin A1 protein, expressed by Sf9 insect cells , with N-His labeled tag.
Cyclin E controls the G1/S transition of the cell cycle. Cyclin E Protein, Human (sf9) is the recombinant human-derived Cyclin E, expressed by Sf9 insect cells , with tag Free labeled tag.
Cyclin E controls the G1/S transition of the cell cycle. Cyclin E Protein, Human (SF9, His-GST) is the recombinant human-derived Cyclin E protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag.
Cyclin E, a vital regulator in cell cycle control, governs the G1/S transition by forming a potent serine/threonine kinase complex with CDK2. This complex, featuring UHRF2, CDK2, and CCNE1, involves Cyclin E's direct interaction with UHRF2, leading to CCNE1 ubiquitination independently of phosphorylation. Cyclin E's intricate dance with CDK2, CABLES1, and CCNA1 highlights its crucial role in tightly regulated cell cycle progression. Cyclin E Protein, Mouse (sf9, His-GST) is the recombinant mouse-derived Cyclin E protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag.
The CDK15ic protein, functioning as an antiapoptotic kinase, counteracts TRAIL/TNFSF10-induced apoptosis by phosphorylating BIRC5 at 'Thr-34'. This regulatory role crucially inhibits programmed cell death triggered by TRAIL/TNFSF10, highlighting the heterodimer's active contribution to antiapoptotic signaling. CDK15-CCNY Heterodimer Protein, Human (sf9) is a recombinant protein dimer complex containing human-derived CDK15-CCNY Heterodimer protein, expressed by sf9 insect cells , with tag free.
PCNA, an atypical member of the sulfotransferase family, displays notably low affinity for 3'-phospho-5'-adenylyl sulfate (PAPS) and minimal catalytic activity towards substrates like L-triiodothyronine, thyroxine, estrone, p-nitrophenol, 2-naphthylamine, and 2-beta-naphthol. Its precise function remains elusive, but PCNA is suggested to participate in drug and neurotransmitter metabolism within the central nervous system (CNS). PCNA Protein, Human (sf9, His) is the recombinant human-derived PCNA protein, expressed by Sf9 insect cells , with N-His labeled tag.
The FGF-9 protein undergoes autoproteolysis and cholesterol attachment in the endoplasmic reticulum. It acts as a morphogen during development, inducing ventral cell fate, participating in limb bud patterning, and aiding in axon guidance. FGF-9 binds to the PTCH1 receptor and activates target gene transcription when in association with SMO, while PTCH1 represses SMO signaling in the absence of FGF-9. CDK1-CCNE1 Heterodimer Protein, Human (sf9, His-GST) is a recombinant protein dimer complex containing human-derived CDK1-CCNE1 Heterodimer protein, expressed by Sf9 insect cells , with N-10*His, N-GST labeled tag. CDK1-CCNE1 Heterodimer Protein, Human (sf9, His-GST), has molecular weight of ~109.7 (60.4+49.3) kDa.
CDK3 protein is a serine/threonine protein kinase that plays a key role in regulating the eukaryotic cell cycle, especially affecting the G0-G1 and G1-S transitions. It interacts with CCNC/cyclin-C during interphase and phosphorylates substrates such as histone H1, ATF1, RB1, and CABLES1. CDK3-CCNE1 Heterodimer Protein, Human (sf9) is a recombinant protein dimer complex containing human-derived CDK3-CCNE1 Heterodimer protein, expressed by sf9 insect cells , with tag free.
CDK3 protein is a serine/threonine protein kinase that plays a key role in regulating the eukaryotic cell cycle, especially affecting the G0-G1 and G1-S transitions. It interacts with CCNC/cyclin-C during interphase and phosphorylates substrates such as histone H1, ATF1, RB1, and CABLES1. CDK3-CCNC Protein, Human (Active, sf9, GST, Flag, His) is the recombinant human-derived CDK3-CCNC, expressed by Sf9 insect cells, with N-Flag, N-His, N-GST labeled tag.
CDK3 protein is a serine/threonine protein kinase that plays a key role in regulating the eukaryotic cell cycle, especially affecting the G0-G1 and G1-S transitions. It interacts with CCNC/cyclin-C during interphase and phosphorylates substrates such as histone H1, ATF1, RB1, and CABLES1. CDK3-CCNE2 Protein, Human (sf9, GST, Flag, His) is the recombinant human-derived CDK3-CCNE2, expressed by Sf9 insect cells, with N-His, N-GST, N-Flag labeled tag.
The CDK9 protein plays a central role in transcriptional regulation, promoting the transition from ineffective to efficient elongation by phosphorylating POLR2A, SUPT5H, and RDBP. As part of the CDK9/cyclin-T complex, it participates in phosphorylation events affecting EP300, MYOD1, RPB1/POLR2A, AR, DSIF, and NELFE. CDK9-CCNT1 Heterodimer Protein, Human (sf9) is a recombinant protein dimer complex containing human-derived CDK9-CCNT1 Heterodimer protein, expressed by sf9 insect cells , with tag free.
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 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.
CDK3 protein is a serine/threonine protein kinase that plays a key role in regulating the eukaryotic cell cycle, especially affecting the G0-G1 and G1-S transitions. It interacts with CCNC/cyclin-C during interphase and phosphorylates substrates such as histone H1, ATF1, RB1, and CABLES1. CDK3-CCNE1 Heterodimer Protein, Human (sf9, GST, FLAG, His) is a recombinant protein dimer complex containing human-derived CDK3-CCNE1 Heterodimer protein, expressed by sf9 insect cells , with N-6*His, N-Flag, N-GST labeled tag.
CDK19 plays a key role in cellular homeostasis and developmental programming. CDK19 can interact with p53 to inhibit p53-mediated transcription of p21, and regulates the proliferation of hematopoietic stem cells and acute myeloid leukemia cells. Besides, CDK19 is the paralog of CDK8. CDK8 and CDK19 can cooperate with each other in stimulating NFκB-induced transcription and Dengue virus replication. CDK19-CCNC-MED12 Protein, Human (sf9, GST, Flag, His) is the recombinant human-derived CDK19-CCNC-MED12, expressed by Sf9 insect cells, with N-6*His, N-GST, N-Flag labeled tag.
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-CCND3 Heterodimer Protein, Human (sf9) is a recombinant protein dimer complex containing human-derived CDK6-CCND3 Heterodimer protein, expressed by sf9 insect cells , with tag free.
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 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-CCND3 Heterodimer Protein, Human (sf9, GST, His) is a recombinant protein dimer complex containing human-derived CDK6-CCND3 Heterodimer protein, expressed by sf9 insect cells , with N-10*His, N-GST labeled tag.
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, GST, Flag, His) is the recombinant human-derived CDK6-CCND1 Heterodimer, expressed by Sf9 insect cells, with N-Flag, N-His, N-GST labeled tag.
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-CCND2 Heterodimer Protein, Human (sf9, GST, FLAG, His) is a recombinant protein dimer complex containing human-derived CDK6-CCND2 Heterodimer protein, expressed by sf9 insect cells , with N-Flag, N-8*His, N-GST labeled tag.
Together with its regulatory partners CCNH and MNAT1, CDK7 functions as an important serine/threonine kinase in cell cycle regulation and RNA polymerase II-mediated transcription. As the catalytic subunit of the CDK-activated kinase (CAK) complex, CDK7 plays a key role in activating CDK1/cyclin-B and CDK2/cyclin during cell cycle transitions. CDK7-CCNH-MNAT1 Protein, Human (sf9) is the recombinant human-derived CDK7-CCNH-MNAT1 protein, expressed by sf9 insect cells , with tag free.
The CDKN2C protein (also known as p18) interacts strongly with CDK6 and weakly with CDK4. Its functional effects inhibit cell growth and proliferation and are significantly related to the presence of endogenous retinoblastoma protein RB. CDKN2C Protein, Human (His) is the recombinant human-derived CDKN2C protein, expressed by E. coli , with N-6*His labeled tag.
CDKN2A Protein, a potent negative regulator of cell proliferation, forms strong interactions with CDK4 and CDK6, hindering their association with cyclins D and retinoblastoma protein phosphorylation. Acting in a heterodimeric manner, predominantly with CDK6, CDKN2A inhibits cyclin D-CDK4 kinase activity and interacts with ISCO2, contributing to its cell cycle regulatory role. CDKN2A Protein, Human is the recombinant human-derived CDKN2A protein, expressed by E. coli , with tag free.
The CDK8-CCNC-MED12 protein is an important component of the mediator complex, acting as a bridge for gene transcription regulation, transmitting information from gene-specific regulatory factors to RNA polymerase II. It is recruited to the promoter, assembles a preinitiation complex, and promotes transcription. CDK8 Protein, Human ( Unactive, sf9, GST) is the recombinant human-derived CDK8, expressed by Sf9 insect cells, with GST labeled tag. The total length of CDK8 Protein, Human ( Unactive, sf9, GST) is 464 a.a..
Cyclin-dependent kinase-like 2 (CDKL2), is a member of the CDC2-related serine/threonine protein kinase family. CDKL2 is tightly associated with tumor progression and is a regulator of epithelial-mesenchymal transition (EMT). CDKL2 also plays a role in cognitive functions, emotion, and neurological disorders. CDKL2 Protein, Human (sf9, His) is the recombinant human-derived CDKL2 protein, expressed by Sf9 insect cells , with N-His labeled tag.
The CDK9 protein plays a central role in transcriptional regulation, promoting the transition from ineffective to efficient elongation by phosphorylating POLR2A, SUPT5H, and RDBP. As part of the CDK9/cyclin-T complex, it participates in phosphorylation events affecting EP300, MYOD1, RPB1/POLR2A, AR, DSIF, and NELFE. CDK9-CCNK Heterodimer Protein, Human (sf9) is a recombinant protein dimer complex containing human-derived CDK9-CCNK Heterodimer protein, expressed by sf9 insect cells , with tag free.
The CDK8-CCNC-MED12 protein is an important component of the mediator complex, acting as a bridge for gene transcription regulation, transmitting information from gene-specific regulatory factors to RNA polymerase II. It is recruited to the promoter, assembles a preinitiation complex, and promotes transcription. CDK8-CCNC Protein, Human (Active, sf9, His-GST) is the recombinant human-derived CDK8-CCNK, expressed by Sf9 insect cells, with N-6*His and N-GST labeled tag.
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 CDK9 protein plays a central role in transcriptional regulation, promoting the transition from ineffective to efficient elongation by phosphorylating POLR2A, SUPT5H, and RDBP. As part of the CDK9/cyclin-T complex, it participates in phosphorylation events affecting EP300, MYOD1, RPB1/POLR2A, AR, DSIF, and NELFE. CDK9-CCNK Heterodimer Protein, Human (sf9, GST, FLAG) is a recombinant protein dimer complex containing human-derived CDK9-CCNK Heterodimer protein, expressed by sf9 insect cells , with N-Flag, N-GST labeled tag.
The p19INK4d protein, a potent inhibitor, strongly interacts with CDK4 and CDK6, effectively impeding their activity. Specifically interacting with CDK6, p19INK4d reinforces its role as a regulator of cyclin-dependent kinase activity. This crucial role in cell cycle regulation involves restraining CDK4 and CDK6 functions, contributing to the modulation of key cellular processes. p19INK4d Protein, Human (GST) is the recombinant human-derived p19INK4d protein, expressed by E. coli , with N-GST labeled tag.
The CDK12 protein is a cyclin-dependent kinase that critically phosphorylates the C-terminal domain of POLR2A, thereby regulating transcription elongation. It selectively targets "Ser-5" phosphorylated at "Ser-7" in the CTD repeat and can also target "Ser-2". CDK12-CCNK Heterodimer Protein, Human (sf9) is a recombinant protein dimer complex containing human-derived CDK12-CCNK Heterodimer protein, expressed by sf9 insect cells , with tag free.
The CDK9 protein plays a central role in transcriptional regulation, promoting the transition from ineffective to efficient elongation by phosphorylating POLR2A, SUPT5H, and RDBP. As part of the CDK9/cyclin-T complex, it participates in phosphorylation events affecting EP300, MYOD1, RPB1/POLR2A, AR, DSIF, and NELFE. CDK9-CCNT2 Heterodimer Protein, Human (sf9) is a recombinant protein dimer complex containing human-derived CDK9-CCNT2 Heterodimer protein, expressed by sf9 insect cells , with tag free.
The CDK9 protein plays a central role in transcriptional regulation, promoting the transition from ineffective to efficient elongation by phosphorylating POLR2A, SUPT5H, and RDBP. As part of the CDK9/cyclin-T complex, it participates in phosphorylation events affecting EP300, MYOD1, RPB1/POLR2A, AR, DSIF, and NELFE. CDK9-CCNT1 Heterodimer Protein, Human (sf9, GST, His) is the recombinant human-derived CDK9-CCNT1, expressed by Sf9 insect cells, with N-His, N-GST labeled tag.
The CDK9 protein plays a central role in transcriptional regulation, promoting the transition from ineffective to efficient elongation by phosphorylating POLR2A, SUPT5H, and RDBP. As part of the CDK9/cyclin-T complex, it participates in phosphorylation events affecting EP300, MYOD1, RPB1/POLR2A, AR, DSIF, and NELFE. CDK9-CCNT2 Heterodimer Protein, Human (sf9, GST, Flag, His) is the recombinant human-derived CDK9-CCNT2, expressed by Sf9 insect cells, with N-His, N-GST, N-Flag labeled tag.
The CDK12 protein is a cyclin-dependent kinase that critically phosphorylates the C-terminal domain of POLR2A, thereby regulating transcription elongation. It selectively targets "Ser-5" phosphorylated at "Ser-7" in the CTD repeat and can also target "Ser-2". CDK12-CCNK Heterodimer Protein, Human (sf9, GST, FLAG) is a recombinant protein dimer complex containing human-derived CDK12-CCNK Heterodimer protein, expressed by sf9 insect cells , with N-Flag, N-GST labeled tag.
The CDK12 protein is a cyclin-dependent kinase that critically phosphorylates the C-terminal domain of POLR2A, thereby regulating transcription elongation. It selectively targets "Ser-5" phosphorylated at "Ser-7" in the CTD repeat and can also target "Ser-2". CDK12-CCNT1 Protein, Human (sf9, GST, Flag, His) is the recombinant human-derived CDK12-CCNT1, expressed by Sf9 insect cells, with N-His, N-GST, N-Flag labeled tag.
The CDK12 protein is a cyclin-dependent kinase that critically phosphorylates the C-terminal domain of POLR2A, thereby regulating transcription elongation. It selectively targets "Ser-5" phosphorylated at "Ser-7" in the CTD repeat and can also target "Ser-2". CDK12-CCNK Heterodimer Protein, Human (sf9) is a recombinant protein dimer complex containing human-derived CDK12-CCNK Heterodimer protein, expressed by sf9 insect cells , with tag free.
PCTAIRE1 protein is a multifunctional kinase that plays a key role in vesicle-mediated transport and regulation of GH1 release, emphasizing neuroendocrine function. Its involvement includes NSF phosphorylation, influencing vesicle dynamics, and important contributions to spermatogenesis and reproductive processes. PCTAIRE1 Protein, Human (sf9, GST) is the recombinant human-derived PCTAIRE1 protein, expressed by Sf9 insect cells , with N-GST labeled tag.
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 Protein, Human (Sf9, His-Avi) is the recombinant human-derived CDK6, expressed by Sf9 insect cells, with N-His, N-Avi labeled tag. The total length of CDK6 Protein, Human (Sf9, His-Avi) is 326 a.a..
The CDK1/CDC2-cyclin-B complex is a key regulator in the cell cycle. It plays an important role in cell division and development and regulates a variety of cellular activities, including chromosome segregation, nuclear membrane rupture, cytokinesis, etc. The activity of CDK1 is regulated by a variety of phosphorylation and dephosphorylation, thereby controlling the progression of the cell cycle and the DNA repair process. CDK1 Protein, Human (sf9) is the recombinant human-derived CDK1, expressed by Sf9 insect cells, with tag-free. The total length of CDK1 Protein, Human (sf9) is 297 a.a..
The CDK1/CDC2-cyclin-B complex is a key regulator in the cell cycle. It plays an important role in cell division and development and regulates a variety of cellular activities, including chromosome segregation, nuclear membrane rupture, cytokinesis, etc. The activity of CDK1 is regulated by a variety of phosphorylation and dephosphorylation, thereby controlling the progression of the cell cycle and the DNA repair process. CDK1 Protein, Human (sf9, GST) is the recombinant human-derived CDK1 protein, expressed by Sf9 insect cells , with N-GST labeled tag.
The CDK1 protein centrally controls the eukaryotic cell cycle, coordinating the G2-M transition and mitotic events. It interacts with a variety of cell cycle proteins, phosphorylates a variety of substrates, and affects cell cycle regulation, DNA repair, and apoptosis. CDK1 Protein, Mouse (sf9, His-GST) is the recombinant mouse-derived CDK1 protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag.
Together with its regulatory partners CCNH and MNAT1, CDK7 functions as an important serine/threonine kinase in cell cycle regulation and RNA polymerase II-mediated transcription. As the catalytic subunit of the CDK-activated kinase (CAK) complex, CDK7 plays a key role in activating CDK1/cyclin-B and CDK2/cyclin during cell cycle transitions. CDK7-CCNH-MNAT1 Protein, Human (sf9, GST, His, Flag) is the recombinant human-derived CDK7-CCNH-MNAT1, expressed by Sf9 insect cells, with N-His, N-GST, N-Flag labeled tag.
CDK2 is an important serine/threonine protein kinase that plays a critical regulatory role in the cell cycle, especially during meiosis. It phosphorylates various substrates (CTNNB1, USP37, p53/TP53, NPM1, CDK7, RB1, BRCA2, MYC, NPAT, EZH2) and coordinates centrosome duplication and initiation of DNA synthesis at the G1-S transition. CDK2 Protein, Human (His) is the recombinant human-derived CDK2 protein, expressed by E. coli , with N-6*His labeled tag.
CDK19 plays a key role in cellular homeostasis and developmental programming. CDK19 can interact with p53 to inhibit p53-mediated transcription of p21, and regulates the proliferation of hematopoietic stem cells and acute myeloid leukemia cells. Besides, CDK19 is the paralog of CDK8. CDK8 and CDK19 can cooperate with each other in stimulating NFκB-induced transcription and Dengue virus replication. CDK19-CCNC-MED12 Protein, Human (sf9) is the recombinant human-derived CDK19-CCNC-MED12 protein, expressed by sf9 insect cells , with tag free. ,
CDK4 protein, acting as a Ser/Thr kinase in the cyclin D-CDK4 complex, critically regulates the G(1)/S transition by phosphorylating and inhibiting RB family members. This activity, specifically hypophosphorylation of RB1 during early G(1) phase, releases E2F and promotes transcription of genes that drive G(1) progression. CDK4-CCND3 Protein, Human (sf9, GST, His) is the recombinant human-derived CDK4-CCND3, expressed by Sf9 insect cells, with N-His, N-GST labeled tag.
CDK4 protein, acting as a Ser/Thr kinase in the cyclin D-CDK4 complex, critically regulates the G(1)/S transition by phosphorylating and inhibiting RB family members. This activity, specifically hypophosphorylation of RB1 during early G(1) phase, releases E2F and promotes transcription of genes that drive G(1) progression. CDK4-CCND1 Protein, Human (sf9, GST, Flag, His) is the recombinant human-derived CDK4-CCND1, expressed by Sf9 insect cells, with N-His, N-GST, N-Flag labeled tag.
CDK4 protein, acting as a Ser/Thr kinase in the cyclin D-CDK4 complex, critically regulates the G(1)/S transition by phosphorylating and inhibiting RB family members. This activity, specifically hypophosphorylation of RB1 during early G(1) phase, releases E2F and promotes transcription of genes that drive G(1) progression. CDK4-CCND2 Protein, Human (sf9, GST, Flag, His) is the recombinant human-derived CDK4-CCND2, expressed by Sf9 insect cells, with N-His, N-GST, N-Flag labeled tag.
ZNHIT1 is a key chromatin remodeling protein that regulates gene expression by promoting the incorporation of histone variants H2AZ1/H2A.Z. In muscle differentiation, ZNHIT1 is recruited to the MYOG promoter, mediating H2AZ1 binding and inducing muscle-specific gene expression. ZNHIT1 Protein, Human (His) is the recombinant human-derived ZNHIT1 protein, expressed by E. coli , with N-6*His labeled tag.
CDK2 is an important serine/threonine protein kinase that plays a critical regulatory role in the cell cycle, especially during meiosis. It phosphorylates various substrates (CTNNB1, USP37, p53/TP53, NPM1, CDK7, RB1, BRCA2, MYC, NPAT, EZH2) and coordinates centrosome duplication and initiation of DNA synthesis at the G1-S transition. CDK2-CCNA2 Protein, Human (sf9, GST, His) is the recombinant human-derived CDK2-CCNA2, expressed by Sf9 insect cells, with N-6*His, N-GST labeled tag.
CDK2 is an important serine/threonine protein kinase that plays a critical regulatory role in the cell cycle, especially during meiosis. It phosphorylates various substrates (CTNNB1, USP37, p53/TP53, NPM1, CDK7, RB1, BRCA2, MYC, NPAT, EZH2) and coordinates centrosome duplication and initiation of DNA synthesis at the G1-S transition. CDK2-CCNO Protein, Human (sf9, GST, Flag, His) is the recombinant human-derived CDK2-CCNO, expressed by Sf9 insect cells, with N-GST, N-Flag, N-His labeled tag.
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.
CDK2 is an important serine/threonine protein kinase that plays a critical regulatory role in the cell cycle, especially during meiosis. It phosphorylates various substrates (CTNNB1, USP37, p53/TP53, NPM1, CDK7, RB1, BRCA2, MYC, NPAT, EZH2) and coordinates centrosome duplication and initiation of DNA synthesis at the G1-S transition. CDK2-CCND1 Protein, Human (sf9, GST, Flag, His) is the recombinant human-derived CDK2-CCND1, expressed by Sf9 insect cells, with N-His, N-GST, N-Flag labeled tag.
CDK2 is an important serine/threonine protein kinase that plays a critical regulatory role in the cell cycle, especially during meiosis. It phosphorylates various substrates (CTNNB1, USP37, p53/TP53, NPM1, CDK7, RB1, BRCA2, MYC, NPAT, EZH2) and coordinates centrosome duplication and initiation of DNA synthesis at the G1-S transition. CDK2-CCNE1 Protein, Human (sf9, GST, His, Flag) is the recombinant human-derived CDK2-CCNE1, expressed by Sf9 insect cells, with N-His, N-GST, N-Flag labeled tag.
CDK5 is a proline-directed serine/threonine protein kinase that critically regulates neuronal cell cycle, differentiation and potential apoptosis in neuronal diseases by preventing cell cycle re-entry. It interacts with numerous proteins involved in neuronal development and coordinates processes such as survival, migration, differentiation, axonal growth, synaptogenesis, and neurotransmission. CDK5-p25 Protein, Human (sf9, GST, His, Flag) is the recombinant human-derived CDK5-p25, expressed by Sf9 insect cells, with N-GST, N-His, N-Flag labeled tag.
CDK2 is an important serine/threonine protein kinase that plays a critical regulatory role in the cell cycle, especially during meiosis. It phosphorylates various substrates (CTNNB1, USP37, p53/TP53, NPM1, CDK7, RB1, BRCA2, MYC, NPAT, EZH2) and coordinates centrosome duplication and initiation of DNA synthesis at the G1-S transition. CDK2-CCNE2 Protein, Human (sf9, GST, Flag, His) is the recombinant human-derived CDK2-CCNE2, expressed by Sf9 insect cells, with N-His, N-GST, N-Flag labeled tag.
CDK5 is a proline-directed serine/threonine protein kinase that critically regulates neuronal cell cycle, differentiation and potential apoptosis in neuronal diseases by preventing cell cycle re-entry. It interacts with numerous proteins involved in neuronal development and coordinates processes such as survival, migration, differentiation, axonal growth, synaptogenesis, and neurotransmission. CDK5-p35 Protein, Human (sf9, GST, His, Flag) is the recombinant human-derived CDK5-p35, expressed by Sf9 insect cells, with N-His, N-GST, N-Flag labeled tag.
The CDK2AP2 protein is an important component of the NuRD complex and actively participates in chromatin remodeling. It inhibits the G1/S phase transition by inhibiting CDK2 and preventing the interaction of CDK2 with cyclin E or A. CDK2AP2 Protein, Human (HEK293, His) is the recombinant human-derived CDK2AP2 protein, expressed by HEK293 , with C-6*His labeled tag.
The CDK8-CCNC-MED12 protein is an important component of the mediator complex, acting as a bridge for gene transcription regulation, transmitting information from gene-specific regulatory factors to RNA polymerase II. It is recruited to the promoter, assembles a preinitiation complex, and promotes transcription. CDK8-CCNC-MED12 Protein, Human (sf9, GST, FLAG, His) is the recombinant human-derived CDK8-CCNC-MED12 protein, expressed by sf9 insect cells , with N-6*His, N-Flag, N-GST labeled tag.
The CDK8-CCNC-MED12 protein is an important component of the mediator complex, acting as a bridge for gene transcription regulation, transmitting information from gene-specific regulatory factors to RNA polymerase II. It is recruited to the promoter, assembles a preinitiation complex, and promotes transcription. CDK8 Protein, Human (Sf9) is the recombinant human-derived CDK8, expressed by Sf9 insect cells, with tag-free. The total length of CDK8 Protein, Human (Sf9) is 464 a.a..
PCTAIRE1 protein is a multifunctional kinase that plays a key role in vesicle-mediated transport and regulation of GH1 release, emphasizing neuroendocrine function. Its involvement includes NSF phosphorylation, influencing vesicle dynamics, and important contributions to spermatogenesis and reproductive processes. CDK16-CCNY Protein, Human (sf9, GST, Flag) is the recombinant human-derived CDK16-CCNY, expressed by Sf9 insect cells, with N-GST, N-Flag labeled tag.
CDK18-CCNY Protein, Human (Active, sf9, GST, Flag) is the recombinant human-derived CDK18-CCNY, expressed by Sf9 insect cells , with GST, Flag labeled tag.
Cdk1; cyclin-dependent kinase 1; CDC2, cell division cycle 2, G1 to S and G2 to M; CDC28A; p34 protein kinase; cell cycle controller CDC2; cell division protein kinase 1; cell division control protein 2 homolog; cell division cycle 2, G1 to S and G2 to M; CDC2; P34CDC2; MGC111195; dkFZp686L20222
The CDK1/CDC2-cyclin-B complex is a key regulator in the cell cycle. It plays an important role in cell division and development and regulates a variety of cellular activities, including chromosome segregation, nuclear membrane rupture, cytokinesis, etc. The activity of CDK1 is regulated by a variety of phosphorylation and dephosphorylation, thereby controlling the progression of the cell cycle and the DNA repair process. CDK1-CCNB1 Protein, Human (sf9, GST, Flag, His) is the recombinant human-derived CDK1-CCNB1, expressed by Sf9 insect cells, with N-GST, N-Flag, N-His labeled tag.
CDK13-CCNK Protein, Human (sf9, GST, Flag) is the recombinant human-derived CDK13-CCNK, expressed by Sf9 insect cells , with N-GST, N-Flag labeled tag. ,
Cdk1; cyclin-dependent kinase 1; CDC2, cell division cycle 2, G1 to S and G2 to M; CDC28A; p34 protein kinase; cell cycle controller CDC2; cell division protein kinase 1; cell division control protein 2 homolog; cell division cycle 2, G1 to S and G2 to M; CDC2; P34CDC2; MGC111195; dkFZp686L20222
The CDK1/CDC2-cyclin-B complex is a key regulator in the cell cycle. It plays an important role in cell division and development and regulates a variety of cellular activities, including chromosome segregation, nuclear membrane rupture, cytokinesis, etc. The activity of CDK1 is regulated by a variety of phosphorylation and dephosphorylation, thereby controlling the progression of the cell cycle and the DNA repair process. CDK1-CCNA2 Protein, Human (sf9, GST, His) is the recombinant human-derived CDK1-CCNA2, expressed by Sf9 insect cells, with N-His, N-GST labeled tag.
Cdk1; cyclin-dependent kinase 1; CDC2, cell division cycle 2, G1 to S and G2 to M; CDC28A; p34 protein kinase; cell cycle controller CDC2; cell division protein kinase 1; cell division control protein 2 homolog; cell division cycle 2, G1 to S and G2 to M; CDC2; P34CDC2; MGC111195; dkFZp686L20222
The CDK1/CDC2-cyclin-B complex is a key regulator in the cell cycle. It plays an important role in cell division and development and regulates a variety of cellular activities, including chromosome segregation, nuclear membrane rupture, cytokinesis, etc. The activity of CDK1 is regulated by a variety of phosphorylation and dephosphorylation, thereby controlling the progression of the cell cycle and the DNA repair process. CDK1-CCNE2 Protein, Human (sf9, GST, His, Flag) is the recombinant human-derived CDK1-CCNE2, expressed by Sf9 insect cells, with N-His, N-GST, N-Flag labeled tag.
Cdk1; cyclin-dependent kinase 1; CDC2, cell division cycle 2, G1 to S and G2 to M; CDC28A; p34 protein kinase; cell cycle controller CDC2; cell division protein kinase 1; cell division control protein 2 homolog; cell division cycle 2, G1 to S and G2 to M; CDC2; P34CDC2; MGC111195; dkFZp686L20222
The CDK1/CDC2-cyclin-B complex is a key regulator in the cell cycle. It plays an important role in cell division and development and regulates a variety of cellular activities, including chromosome segregation, nuclear membrane rupture, cytokinesis, etc. The activity of CDK1 is regulated by a variety of phosphorylation and dephosphorylation, thereby controlling the progression of the cell cycle and the DNA repair process. CDK1-CCNE1 Heterodimer Protein, Human (sf9, GST, His, Flag) is the recombinant human-derived CDK1-CCNE1, expressed by Sf9 insect cells, with N-GST, N-Flag, N-His labeled tag.
CDK13-CCNT1 Protein, Human (sf9, GST, Flag, His) is the recombinant human-derived CDK13-CCNT1, expressed by Sf9 insect cells , with N-His, N-Flag, N-GST labeled tag. ,
The CDK15ic protein, functioning as an antiapoptotic kinase, counteracts TRAIL/TNFSF10-induced apoptosis by phosphorylating BIRC5 at 'Thr-34'. This regulatory role crucially inhibits programmed cell death triggered by TRAIL/TNFSF10, highlighting the heterodimer's active contribution to antiapoptotic signaling. CDK15-CCNY Heterodimer Protein, Human (sf9, GST, Flag) is the recombinant human-derived CDK15-CCNY, expressed by Sf9 insect cells, with GST, Flag labeled tag.
Ribociclib-d6 (LEE011-d6) is a deuterium labeled Ribociclib (HY-15777). 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 .
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 .
Ribociclib-d8 is the deuterium labeled Ribociclib . 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 cyclin B/CDK1 complex .
TAT-p16 (p16INK4a peptide) is a peptide mimic of p16INK4a that can induce an early G phase cell cycle arrest in the absence of active cyclin E:Cdk2 complex .
Decursin-d6 ((+)-Decursin-d6) is the deuterium labeled Decursin (HY-18981). Decursin ((+)-Decursin) is a potent anti-tumor agent. Decursin also is a cytotoxic agent and a potent protein kinase C activator. Decursin induces apoptosis and cell cycle arrest at G1 phase. Decursin decreases the expression of CDK2, CDK4, CDK6, cyclin D1 protein at 48 h. Decursin inhibits cell proliferation and migration. Decursin shows anti-tumor, anti-inflammatory and analgesic activities .
cyclin-dependent kinase 5; Cell division protein kinase 5; Serine/threonine-protein kinase PSSALRE; Tau protein kinase II catalytic subunit; TPKII catalytic subunit;
IHC-P, WB
Human, Mouse, Rat
CDK5 Antibody (YA5385) is a Mouse-derived and non-conjugated monoclonal antibody, targeting to CDK5.
Cdk1; CDC2; CDC28A; CdkN1; P34CDC2; cyclin-dependent kinase 1; Cdk1; Cell division control protein 2 homolog; Cell division protein kinase 1; p34 protein kinase
WB, ICC/IF, IHC-P, FC
Human, Mouse, Rat
Phospho-CDK1 (Thr161) Antibody (YA9905) is a Rabbit-derived and non-conjugated IgG Recombinant, Monoclonal antibody, targeting to Phospho-CDK1 (Thr161).
Cdk1; CDC2; CDC28A; CdkN1; P34CDC2; cyclin-dependent kinase 1; Cdk1; Cell division control protein 2 homolog; Cell division protein kinase 1; p34 protein kinase
WB, IHC-P
Human, Mouse, Rat
Phospho-CDK/2/3 (Thr14) Antibody (YA9906) is a Rabbit-derived and non-conjugated IgG Recombinant, Monoclonal antibody, targeting to Phospho-Cdk1/2/3 (Thr14).
SKP1; EMC19; OCP2; SKP1A; TCEB1L; S-phase kinase-associated protein 1; cyclin-A/Cdk2-associated protein p19; Organ of Corti protein 2; OCP-2; Organ of Corti protein II; OCP-II; RNA polymerase II elongation factor-like protein; SIII; Transcr
WB, ICC/IF
Human, Mouse, Rat
SKP1 Antibody (YA1974) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to SKP1.
SKP1; EMC19; OCP2; SKP1A; TCEB1L; S-phase kinase-associated protein 1; cyclin-A/Cdk2-associated protein p19; Organ of Corti protein 2; OCP-2; Organ of Corti protein II; OCP-II; RNA polymerase II elongation factor-like protein; SIII; Transcr
WB, ICC/IF
Human, Mouse, Rat
SKP1 Antibody (YA1974) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to SKP1.
UNC-CA359 is a potent epidermal growth factor receptor (EGFR) inhibitor, with an IC50 value of 18 nM. UNC-CA359 exhibits strong anti-tumor activity, can be used to Chordoma research . UNC-CA359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC (PC(18:0/22:4)) is an inhibitor of cyclin-dependent kinases (CDKs). 1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC induces apoptosis and inhibits the growth of various cancer cell lines .
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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