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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 cyclinD1 and c-Myc .
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 CyclinD1 and induces G0/G1 arrest by inhibiting deubiquitinase USP2a .
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/cyclinD1, 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 .
Arctiin is an orally active inhibitor of NF-κB. Arctiin suppresses cyclinD1 protein expression in human tumor cells. Arctiin also reduces malondialdehyde and pro-in ammatory cytokines levels. Arctiin can used in study glomerulonephritis .
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/cyclinD1 pathway and induces apoptosis .
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/cyclinD1, CDK6/cyclinD1 and FLT3, respectively. FN-1501 has anticancer activity.
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 cyclinD1 and induces p53 expression. Anticancer agent 50 has the potential for the research of T-lymphoma .
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 cyclinD1 protein expression in human tumor cells. Arctiin also reduces malondialdehyde and pro-in?ammatory cytokines levels. Arctiin can used in study glomerulonephritis .
DCB-3503 is an allosteric modulator of heat shock cognate protein HSC70 and an inhibitor of CyclinD1. DCB-3503 inhibits CyclinD1 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 cyclinD1 .
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 cyclinD1, 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 .
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), CyclinD1 and increases the expression of cleaved caspase-3 protein. HJC0416 shows anti-tumor activity .
DIF-3 is an orally active anticancer agent. DIF-3 reduces the expression levels of cyclinD1 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 .
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 cyclinD1. 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) .
GP-82996 (CINK4) is a pharmacological inhibitor of CDK4/6. GP-82996 has IC50s of 1.5, 5.6 and 25 μM for CDK4/cyclinD1, CDK6/cyclinD1 and Cdk5/p35, respectively. GP-82996 induces the apoptosis of cancer cells U2OS. GP-82996 can be used in the research of cancer .
PF-06842874 is a CDK4/CyclinD1 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 .
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 CyclinD1 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 .
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/cyclinD1, respectively .
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/cyclinD1, respectively .
CA224 (Compound 1) is a selective and orally active Cdk4–cyclinD1 inhibitor with an IC50 of 6.2 µM. CA224 induces cell apoptosis and shows antitumor activity .
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 cyclinD1 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 .
CDK4 inhibitor is a novel and specific CDK4/CyclinD1 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.
Purvalanol A is a potent CDK inhibitor, which inhibits cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclinD1, and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, resepctively.
CDK4/6-IN-5 is a potent CDK4 and CDK6 inhibitor with Kis of 0.2 and 4.4 nM for CDK4/CyclinD1 and CDK6/Cyclin D3, respectively . (from patent WO2019207463A1 example A93).
NSC 625987 is a specific and high-affinity CDK4 inhibitor with an IC50 of 0.2 μM for CDK4:cyclinD1. NSC 625987 shows >500-fold selectivity for CDK4 over CDK2 .
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 CyclinD1. 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 .
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, cyclinD1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.
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/cyclinD1, 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/CyclinD1), 3 nM (CDK6/Cyclin D3), and 0.63 μM (CDK7/Cyclin H), respectively. Ulecaciclib can cross blood brain barrier and has good pharmacokinetic characteristics .
CDK4/6-IN-9 (compound 10) is a selective CDK4/6 inhibitor with an IC50 of 905 nM for CDK6/cyclinD1. CDK4/6-IN-9 has the potential for multiple myeloma (MM) research .
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-cyclinD1, and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, resepctively.
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, cyclinD1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.
Lenoremycin (Ro 21-6150) is a microbial metabolite. Lenoremycin decreases β-catenin and cyclinD1 proteins levels. Lenoremycin decreases cancer stem cells (CSCs) populations via inducing reactive oxygen species production .
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/cyclinD1, and CDK5/p35, respectively . Indirubin-5-sulfonate also shows inhibitory activity against GSK-3β .
Garcinone D is an activator of the STAT3/CyclinD1 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 CyclinD1 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 .
Riviciclib (P276-00 free base) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclinD1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively .
Riviciclib shows antitumor activity on cisplatin-resistant cells .
Riviciclib hydrochloride (P276-00) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclinD1, 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 .
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, CyclinD1 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 cyclinD1 regulation and G1/S transition. Cdc25A (80-93) (human) can be used in cancer research .
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclinD1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclinD1-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.
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/CyclinD1 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 CyclinD1 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 .
1D228 is a c-Met/TRK inhibitor with antitumor activity. 1D228 inhibits cyclinD1 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 .
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 cyclinD1 for proteasomal degradation. Obatoclax Mesylate has anti-cancer and broad-spectrum antiparasitic activity .
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, CyclinD1, TCF4, and ID2) .
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 cyclinD1 for proteasomal degradation. Obatoclax has anti-cancer and broad-spectrum antiparasitic activity .
(-)-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 cyclinD1, Bax and Bcl-2. (-)-Hinesol has the potential for the research of non–small cell lung cancer .
CPD-10 is a potent CCND1 and CDK4 PROTAC degrader. CPD-10 shows anti-proliferation. CPD-10 induces apoptosis. CPD-10 decreases the protein expression of cyclinD1, cyclin D3, CDK4, P-Rb(5807/811) in a dose-dependent manner. (Pink: ligand for target protein (HY-50767); black: linker (HY-22391); Blue: E3 ligase ligand (HY-168667)) .
Taurolithocholic acid is a bile acid that has the activity of increasing cell viability, inducing the S phase of the cell cycle, and promoting DNA synthesis in a concentration-dependent manner in the intrahepatic cholangiocarcinoma cell line RMCCA-1. It can also increase the phosphorylation of EGFR and ERK 1/2 and the expression of cyclinD1 in RMCCA-1 cells, and its induced RMCCA-1 cell growth can be inhibited by specific antagonists and inhibitors.
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 cyclinD1 degradation and causes cell cycle arrest. ML364 increases the levels of mitochondrial ROS and decreases in the intracellular content of ATP .
OBHSA is a selective estrogen receptor (ERα) degrader. OBHSA blocks the cell cycle by degrading cyclinD1, 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 .
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, cyclinD1 protein at 48 h. Decursin inhibits cell proliferation and migration. Decursin shows anti-tumor, anti-inflammatory and analgesic activities .
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, CyclinD1, 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 .
[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-cyclinD1 kinase activity in vitro (IC50: 1.5 μM). [Ala92]-p16 (84-103) blocks cell cycle progression through the G1 phase .
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 cyclinD1 and survivin .
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 cyclinD1 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) .
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 cyclinD1. 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, cyclinD1 protein at 48 h. Decursin inhibits cell proliferation and migration. Decursin shows anti-tumor, anti-inflammatory and analgesic activities [4].
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-cyclinD1 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 .
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, CyclinD1, 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 .
HVH-2930 is an inhibitor for heat shock protein 90 (HSP90). HVH-2930 inhibits cell viability of BT474 (Trastuzumab (HY-P9907) sensitive) and JIMT-1 (Trastuzumab (HY-P9907) resistant), with IC50 of 6.86 μM and 4.42 μM, through downregulation of HSP90 clients HER2, p-HER2, AKT, p-AKT, cyclinD1 and survivin. HVH-2930 exhibits antitumor efficacy in mouse models. HVH-2930 exhibits good pharmacokinetic characteristics in mice .
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 cyclinD1. 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 .
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-CyclinD1-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 .
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 cyclinD1. 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 .
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-cyclinD1 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 .
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 (cyclinD1 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 cyclinD1. 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 .
P1D-34 is a Pin1PROTAC degrader with a DC50 value of 177 nM. P1D-34 also down-regulates Pin1 client proteins such as CyclinD1, 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 (cyclinD1 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.
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 CyclinD1, Bcl-2, and Bcl-xl. WR-S-462 inhibits TNBC (triple-negative breast cancer) growth and metastasis .
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 CyclinD1 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 .
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, CyclinD1 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 .
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, CyclinD1 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 .
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 .
(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 .
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 .
(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 CyclinD1 protein levels in mice .
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 .
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 .
Cdc25A (80-93) (human) is a polypeptide that controls the cell proliferation and tumorigenesis by a change in expression of proteins involved in cyclinD1 regulation and G1/S transition. Cdc25A (80-93) (human) can be used in cancer research .
[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-cyclinD1 kinase activity in vitro (IC50: 1.5 μM). [Ala92]-p16 (84-103) blocks cell cycle progression through the G1 phase .
Arctiin is an orally active inhibitor of NF-κB. Arctiin suppresses cyclinD1 protein expression in human tumor cells. Arctiin also reduces malondialdehyde and pro-in ammatory cytokines levels. Arctiin can used in study glomerulonephritis .
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 cyclinD1. 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) .
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 CyclinD1 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 .
Garcinone D is an activator of the STAT3/CyclinD1 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 CyclinD1 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 .
(-)-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 cyclinD1, Bax and Bcl-2. (-)-Hinesol has the potential for the research of non–small cell lung cancer .
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, cyclinD1 protein at 48 h. Decursin inhibits cell proliferation and migration. Decursin shows anti-tumor, anti-inflammatory and analgesic activities .
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 .
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 cyclinD1 protein expression in human tumor cells. Arctiin also reduces malondialdehyde and pro-in?ammatory cytokines levels. Arctiin can used in study glomerulonephritis .
Lenoremycin (Ro 21-6150) is a microbial metabolite. Lenoremycin decreases β-catenin and cyclinD1 proteins levels. Lenoremycin decreases cancer stem cells (CSCs) populations via inducing reactive oxygen species production .
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/CyclinD1 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 CyclinD1 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 .
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, cyclinD1 protein at 48 h. Decursin inhibits cell proliferation and migration. Decursin shows anti-tumor, anti-inflammatory and analgesic activities [4].
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-cyclinD1 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 .
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 cyclinD1. 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 .
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 .
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-cyclinD1 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 .
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 (cyclinD1 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 cyclinD1. 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 .
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 (cyclinD1 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.
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 .
The CCND1 protein is a regulatory component of the cyclin D1-CDK4 complex that coordinates phosphorylation and RB family inhibition to regulate the G(1)/S transition. This promotes the dissociation of E2F from the RB/E2F complex and promotes the transcription of E2F target genes critical for G(1) phase progression. CCND1 Protein, Human (His) is the recombinant human-derived CCND1 protein, expressed by E. coli , with N-6*His labeled tag.
The 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.
![[Ala92]-p16 (84-103)](http://file.medchemexpress.eu/product_pic/hy-p1109.gif)
