Search Result
Results for "
resistant tumors
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-156698
-
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PROTACs
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Inflammation/Immunology
Cancer
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HJM-561 is a potent, selective, orally bioavailable EGFR PROTAC. HJM-561 overcomes osimertinib (HY-15772)-resistant EGFR triple mutations and has anti-tumor activity .
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-
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- HY-107271
-
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Others
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Cancer
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Imperialine 3-β-D-glucoside is the glycoside of Imperialine. Imperialine 3-β-D-glucoside may exhibit anti-tumor properties against multi-agent resistant tumor cells .
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-
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- HY-P99217
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AMG 102
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c-Met/HGFR
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Cancer
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Rilotumumab (AMG 102) is an anti-HGF (anti-hepatocyte growth factor) monoclonal antibody, inhibits HGF/MET-driven signaling. Rilotumumab shows anti-tumor activity, and can be used in castration-resistant prostate cancer (CRPC) and solid tumor research .
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- HY-135336A
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(S)-(-)-Verapamil hydrochloride
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Leukotriene Receptor
Calcium Channel
Apoptosis
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Cancer
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(S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells .
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-
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- HY-144070A
-
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Estrogen Receptor/ERR
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Cancer
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(Rac)-ErSO-DFP is a derivative of ErSO-DFP and a selective small molecule Erα biomodulator. (Rac)-ErSO-DFP againsts ERα+ breast cancer (including resistant tumors) by hyperactiving the Erα-dependent a-UPR (extracted from patent WO2022087234A1) .
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-
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- HY-N10765
-
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Bacterial
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Inflammation/Immunology
Cancer
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Salvinolone is active against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus (VRE). Salvinolone shows cytotoxic activity with an IC50 of 47.6 μM against the HL-60 tumor cell line for 72 h .
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-
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- HY-N2104
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Others
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Cancer
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Daurinoline is an alkaloid that can be isolated from the roots of Menispermum dauricum. Daurinoline may be a potential anti-tumor agent or chemosensitizer for chemo-resistant NSCLC research .
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-
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- HY-160020
-
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Androgen Receptor
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Cancer
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ET516 is a potent inhibitor of Androgen Receptor. ET516 significantly inhibits the proliferation and tumor growth of prostate cancer cells expressing AR-resistant mutants .
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-
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- HY-161661
-
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Others
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Cancer
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Anticancer agent 223 (Compound V-d) is an anticancer agent that triggers cell death through caspase-dependent and caspase-independent mechanisms. Anticancer agent 223 inhibits tumor spheroid formation and resensitizes cisplatin (HY-17394)-resistant A2780 cells to cisplatin (HY-17394) treatment .
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-
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- HY-139920A
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SH-1028 mesylate
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EGFR
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Cancer
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Oritinib (SH-1028) mesylate is a selective, orally active, and pyrimidine-based irreversible inhibitor of EGFR with an IC50 of 18 nM. Oritinib (SH-1028) mesylate exhibits potent activity against EGFR sensitive and resistant (T790 M) mutations. Oritinib (SH-1028) mesylate significantly inhibits proliferation of tumor cells with EGFR sensitive and resistant mutation .
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-
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- HY-N6932
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-
-
- HY-W773183
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Betulonic acid methyl ester; Methyl 3-oxolup-20(29)-en-28-oate
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Others
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Cancer
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Methyl betulonate (Betulonic acid methyl ester) is a triterpenoid. Methyl betulonate inhibits cell growth of eight tumor (including resistant) and two normal fibroblast cell lines with the IC50s >50.0 μM .
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-
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- HY-149053
-
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P-glycoprotein
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Cancer
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OY-101 is an orally active, potent and specific P-glycoprotein (P-gp) inhibitor. OY-101 can sensitize drug-resistant tumors and effectively reverse tumor multidrug resistance. OY-101 is improvements in water-solubility, cytotoxicity, and reversal activity compared to Tetrandrine (HY-13764) .
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-
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- HY-147812
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DNA/RNA Synthesis
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Cancer
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POLA1 inhibitor 1 (Compound 12) is an orally active POLA1 inhibitor. POLA1 inhibitor 1 shows antitumor activity against several tumor histotypes and Adarotene-resistant cell line .
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- HY-12965B
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TAM Receptor
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Cancer
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(Z)-S49076 hydrochloride is an orally active inhibitor of MET and AXL that blocks the downstream signaling of these receptors both in vitro and in vivo, inhibiting the proliferation and migration of tumor cells and suppressing tumor growth in xenograft models. (Z)-S49076 hydrochloride is capable of overcoming the resistance to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) due to MET amplification in Erlotinib (HY-50896)-resistant cell lines both in vitro and in vivo. (Z)-S49076 hydrochloride can be used for research in non-small cell lung cancer (NSCLC) .
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-
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- HY-127079
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Microtubule/Tubulin
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Cancer
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Epothilone F is a Microtubule/Tubulin-stabilizing agent with anti-tumor activity. Epothilone F inhibits the proliferation of breast cancer cells, non-small cell lung cancer cells, drug-resistant ovarian cancer cells .
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-
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- HY-19319
-
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Epigenetic Reader Domain
Androgen Receptor
Apoptosis
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Cancer
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MI-136 is an inhibitor of the menin-MLL protein-protein interaction (PPI), with an IC50 of 31 nM and a Kd of 23.6 nM. MI-136 shows to block AR signaling and has the potential for the study in castration-resistant tumors .
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- HY-111145
-
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Androgen Receptor
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Cancer
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RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgen receptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer .
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-
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- HY-P1653
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Antifolate
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Cancer
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EC-1456 is a folate-tubulysin conjugate with significant anti-proliferative activity against FR-positive tumors, including models which were anticancer drug resistant. EC-1456 can be utilized in cancer research .
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-
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- HY-N2360
-
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E1/E2/E3 Enzyme
Apoptosis
MMP
ClpP
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Infection
Inflammation/Immunology
Cancer
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Hinokiflavone is a novel modulator of pre-mRNA splicing activity extracted from plants with anti-inflammatory, anti-tumor and antiviral activities. Hinokiflavone is also a potent inhibitor for matrix metalloproteinases (MMPs). Hinokiflavone attenuates the virulence of Methicillin (HY-121544)-resistant staphylococcus aureus by inhibiting caseinolytic protease P (ClpP) with an IC50 value of 34.36 mg/mL. Hinokiflavone induces apoptosis via the reactive oxygen species-mitochondria-mediated apoptotic pathway and inhibits tumor cell migration and invasion. Hinokiflavone is a SUMO protease inhibitor against sentrin-specific protease 1 (SENP1) activity .
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- HY-110201
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Estrogen Receptor/ERR
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Cancer
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Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors .
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-
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- HY-124628
-
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Fatty Acid Synthase (FASN)
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Cancer
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IPI-9119 is an orally active, selective and irreversible FASN inhibitor with an IC50 of 0.3 nM in vitro biochemical assay. IPI-9119 inhibits tumor growth of castration-resistant prostate cancer (CRPC) xenografts mouse models .
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-
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- HY-162040
-
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P-glycoprotein
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Cancer
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P-gp inhibitor 17 (compound 2g) is a P-gp inhibitor directly interacted with the transmembrane domain of P-gp. P-gp inhibitor 17 can be used for P-gp-mediated multidrug-resistant in tumor cells study .
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-
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- HY-N0944
-
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Others
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Cancer
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(-)-Heraclenol is a derivative of furocoumarin isolated from Ducrosia anethifolia. (-)-Heraclenol shows antiproliferative and cytotoxic activities on cancer cell lines .
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-
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- HY-124325
-
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DNA Alkylator/Crosslinker
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Cancer
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PIP-199 is a selective inhibitor of RMI (RecQ-mediated genome instability protein) core complex/MM2 interaction, with an IC50 of 36 μM. PIP-199 can be used for the research of sensitizing resistant tumors to DNA crosslinking chemotherapeutics .
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-
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- HY-106588
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SKI 2053R
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DNA Alkylator/Crosslinker
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Cancer
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Heptaplatin (SKI 2053R) is a platinum derivative with anticancer activity against various cancer cell lines, including cisplatin-resistant tumor cell lines. SKI-2053R is active in the research of gastric adenocarcinoma and has favorable toxicity profiles .
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- HY-127155
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Bacterial
Antibiotic
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Infection
Cancer
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Kigamicin C is an anti-tumor antibiotic that selectively kills pancreatic cancer PANC-1 cells only in nutrient-poor conditions. Kigamicin C has antimicrobial activity against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA) .
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-
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- HY-135336AS
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(S)-(-)-Verapamil-d7 hydrochloride
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Isotope-Labeled Compounds
Leukotriene Receptor
Calcium Channel
Apoptosis
|
Cancer
|
(S)-Verapamil-d7 (hydrochloride) is a deuterium labeled (S)-Verapamil hydrochloride. (S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells[1][2].
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-
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- HY-117563
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SKI 5C
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SphK
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Cancer
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CAY10621 (SKI 5C; compound 5c) is a specific sphingosine kinase 1 (SPHK1) inhibitor with an IC50 of 3.3 μM. CAY10621 is low toxic toward cells. CAY10621 has the potential for resistant cancer tumors research .
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-
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- HY-161668
-
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Ligands for E3 Ligase
Ferroptosis
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Cancer
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Ru-Poma is a Ru(II)-based photosensitizer, which attenuates Cisplatin (HY-17394)-resistant tumor through photodynamic therapy (PDT). Ru-Poma photodegrades CRBN through a Pomalidomide (HY-10984) moiety. Ru-Poma induces ferroptosis, through an increase in lipid peroxide, downregulation of GPX4 and GAPDH expression. Ru-Poma exhibits cytotoxicity in A549, with IC50 of 18.46 μM and 0.37 μM in dark and upon irradiation, respectively .
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-
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- HY-162822
-
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P-glycoprotein
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Cancer
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P-gp modulator-5 (compound 25) is a modulator of P-gp and can inhibit the proliferation of multidrug resistant (MDR) tumors. P-gp modulator-5 inhibits the activity of drug efflux pumps in MDR cells, leading to a large accumulation of ROS and altered cell cycle profiles .
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-
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- HY-N0790
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Lupeol
3 Publications Verification
Clerodol; Monogynol B; Fagarasterol
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Androgen Receptor
Apoptosis
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Cancer
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Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent androgen receptor (AR) inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC) .
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-
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- HY-159580
-
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STAT
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Cancer
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STAT3-IN-31 (compound K2071) is a STATtic-derived STAT3 and mitotic inhibitor. STAT3-IN-31 blocks mitotic progression and affects the formation of mitotic spindles. STAT3-IN-31 also affects glioblastoma cell migration and inhibits cell proliferation in tumor spheroids. STAT3-IN-31 is also able to induce glioblastoma senescence, inhibit the growth of Temozolomide (HY-17364)-resistant cells and the secretion of the pro-inflammatory cytokine monocyte chemoattractant protein MCP-1 .
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- HY-12458
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DNA/RNA Synthesis
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Infection
Cancer
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Pyrindamycin A is an antibiotic that inhibits DNA synthesis. Pyrindamycin A shows antitumor activities against murine leukemia, exhibits stronger cytotoxic activities towards murine and human tumor cell lines and especially towards doxorubicin-resistant cells, inhibits P388 and P388/ADR cells with the same IC50 of 3.9 μg/ml .
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- HY-169903
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Apoptosis
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Cancer
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SMIP34 is a PELP1 inhibitor. SMIP34 binds to PELP1 with a Kd of 37.4 μM. SMIP34 inhibits cancer cell proliferation and tumor progression. SMIP34 can be used for breast cancer research, and is active against wild-type (WT), mutant (MT) ER + and therapy-resistant (TR)-ER + breast cancer .
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- HY-129236
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Na+/K+ ATPase
Apoptosis
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Cancer
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Hellebrin is a bufadienolide compound extracted from plants that can inhibit tumor cell growth. Hellebrigenin shows potential in overcoming cancer cells' resistance to apoptosis stimuli and has also demonstrated anti-proliferation effects in multidrug-resistant (MDR) cancer cell models. Hellebrin can act on Na+/K+-ATPase to regulate intracellular signaling pathways .
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-
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- HY-128910
-
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Drug-Linker Conjugates for ADC
Microtubule/Tubulin
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Cancer
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MC-VC(S)-PABQ-Tubulysin M is a synthetic ADC drug-linker conjugate composed of the tubulin polymerization inhibitor Tubulysin M (an ADC Cytotoxin) (HY-N7053) and MC-VC(S)- PABQ (an ADC linker) is connected. MC-VC(S)-PABQ-Tubulysin M is effective against multidrug-resistant lymphoma cell lines and tumors .
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-
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- HY-13617
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CGP 30694
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Antifolate
|
Cancer
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Edatrexate (CGP 30694), as known as 10-Ethyl-10-deazaaminopterin, is Methotrexate (HY-14519) analog, exhibits antitumor activity against MTX-resistant tumors. Edatrexate is an antifolate antimetabolite, can be used for reasearch of non-small-cell lung cancer, breast cancer, non-Hodgkin's lymphoma, and cancer of the head and neck .
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-
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- HY-121588
-
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Adrenergic Receptor
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Cancer
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IMTPPE is an inhibitor of the androgen receptor (AR) in C4-2 prostate cancer cells, inhibiting its transcriptional activity and protein levels. IMTPPE inhibited the proliferation of AR-positive prostate cancer cells but had no effect on AR-negative prostate cancer cells. IMTPPE also inhibited the growth of enzalutamide-resistant 22Rv1 xenograft tumors .
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-
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- HY-160053
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PDGFR
|
Cancer
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Gint4.T aptamer sodium is a nuclease-resistant RNA aptamer-based antagonist targeting platelet-derived growth factor receptor beta (PDGFRβ) (Kd: 9.6 nM). Gint4.T aptamer sodium inhibits PDGFRβ heterodimerization and EGFR transactivation. It can significantly inhibit cell migration and proliferation, induce differentiation and prevent tumor growth in vivo. Gint4.T aptamer sodium specifically inhibits PDGFRβ-mediated tropism of mesenchymal stem cells (MSCs) toward the tumor microenvironment .
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-
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- HY-15794
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Methoxymorpholinyl doxorubicin; FCE 23762; PNU 152243
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G-quadruplex
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Cancer
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Nemorubicin (Methoxymorpholinyl doxorubicin) is a Doxorubicin derivative with potent antitumor activity. Nemorubicin is highly cytotoxic to a variety of tumor cell lines presenting a multidrug-resistant phenotype. Nemorubicin not only intercalate into the duplex DNA, but also result in significant ligands for G-quadruplex DNA segments, stabilizing their structure. Nemorubicin requirs an intact nucleotide excision repair (NER) system to exert its activity .
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-
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- HY-153342
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ARV-766
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PROTACs
Androgen Receptor
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Cancer
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Luxdegalutamide (ARV-766) is an orally active protein hydrolysis targeted chimeric (PROTAC) targeting androgen receptor (AR), which can degrade AR resistance related mutants, including T878/H875/L702 mutants. Luxdegalutamide has anti-tumor activity and can be used in the study of castration resistant prostate cancer .
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-
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- HY-143471
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PLK1/BRD4-IN-1
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Polo-like Kinase (PLK)
Epigenetic Reader Domain
Apoptosis
Androgen Receptor
c-Myc
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Cancer
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WNY0824 (PLK1/BRD4-IN-1) is an orally active dual inhibitor of PLK1 and BET protein families, with IC50 values of 22, 402.5, 150.7, 103.9, and 311.9 nmol/L for PLK1, BRD2, BRD3, BRD4, and BRDT, respectively. WNY0824 induces cell cycle arrest and apoptosis by inhibiting AR- and MYC-mediated transcriptional processes. In addition, WNY0824 also inhibits tumor growth in Enzalutamide (HY-70002) resistant CRPC xenograft tumor models .
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-
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- HY-N0790R
-
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Androgen Receptor
Apoptosis
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Cancer
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Lupeol (Standard) is the analytical standard of Lupeol. This product is intended for research and analytical applications. Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic?triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent?androgen receptor (AR)?inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC) .
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-
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- HY-P10743
-
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Radionuclide-Drug Conjugates (RDCs)
PSMA
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Cancer
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BQ7876 is a probe targeting prostate-specific membrane antigen (PSMA) that contains a DOTA chelator. BQ7876, after being radiolabeled with radionuclide (177Lu), functions in both radionuclide imaging and tumor cell destruction by specifically binding to PSMA. BQ7876 shows potential for research in the field of metastatic castration-resistant prostate cancer (mCRPC) . BQ7876 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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-
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- HY-124093
-
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Thymidylate Synthase
Bacterial
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Infection
Cancer
|
8-Deazahomofolic acid is an inhibitor of thymidylate synthase (TS) and other folate-related enzymes. 8-Deazahomofolic acid shows inhibitory activity against folate-dependent S. faecium, L. casei, and MTX (HY-14519) resistant strains. 8-Deazahomofolic acid also inhibits the growth of L1210 leukemia cells, with an IC50 value of 87.5 μM. 8-Deazahomofolic acid can be used in research on bacterial infections and tumors .
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-
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- HY-15794G
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Methoxymorpholinyl doxorubicin; FCE 23762; PNU 152243
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G-quadruplex
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Cancer
|
Nemorubicin (Methoxymorpholinyl doxorubicin) GMP is a GMP-class Nemorubicin (HY-15794). Nemorubicin is a Doxorubicin derivative with potent antitumor activity. Nemorubicin is highly cytotoxic to a variety of tumor cell lines presenting a multidrug-resistant phenotype. Nemorubicin not only intercalate into the duplex DNA, but also result in significant ligands for G-quadruplex DNA segments, stabilizing their structure. Nemorubicin requirs an intact nucleotide excision repair (NER) system to exert its activity .
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-
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- HY-122912
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ALDH1Ai 673A
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Aldehyde Dehydrogenase (ALDH)
Necroptosis
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Cancer
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ALDH1A inhibitor 673A is an ALDH1A inhibitor. ALDH1A inhibitor 673A inhibits all three ALDH1A family members (IC50: 246 nM, 230 nM, 348 nM for ALDH1A1, ALDH1A2, ALDH1A3 respectively. ALDH1A inhibitor 673A induces necroptotic cell death preferentially in CD133+ ovarian CSCs. ALDH1A inhibitor 673A also inhibits chemotherapy-resistant tumor growth .
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-
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- HY-126170
-
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Antibiotic
Bacterial
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Infection
Cancer
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Valanimycin is an antibiotic, which inhibits Escherichia coli (BE1121) through interaction with DNA. Valanimycin exhibits cytotoxicity to mouse leukemia L1210, P388/S (doxorubicin (HY-15142A)-sensitive), and P388/ADR (doxorubicin-resistant), with IC50 of 0.79, 2.65, and 1.44 μg/mL, respectively. Valanimycin exhibits antitumor efficacy against ehrlich ascites tumors or L1210 in mice .
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- HY-19542
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C6-Cer; N-Hexanoylsphingosine
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Apoptosis
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Cancer
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C6 Ceramide (C6-Cer) is a short-chain, cell-permeable ceramide pathway activator with anticancer activity. C6 Ceramide-mediated miR-29b expression participates in the progression of multiple myeloma through suppressing the proliferation, migration and angiogenesis of endothelial cells by targeting Akt signal pathway. C6 Ceramide exhibits multiple anti-cancer properties including cell cycle arrest, Apoptosis, inhibition of tumor growth and enhances the effects of chemotherapy in drug-resistant cancer cells. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects .
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- HY-N10264
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(+)-Avrainvillamide; CJ-17,665
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Antibiotic
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Infection
Cancer
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Avrainvillamide ((+)-Avrainvillamide) is a naturally occurring alkaloid with antiproliferative effects, binds to the nuclear chaperone nucleophosmin, a proposed oncogenic protein that is overexpressed in many different human tumors. Avrainvillamide affects cell biology both by directly binding NPM1 and Crm1 as well as by inhibiting the association of these proteins with certain native cellular partners. Avrainvillamide, an antibiotic, inhibits growth of multi-agent resistant Staphylococcus aureus, Streptococcus pyogenes, and Enterococcus faecalis, with MICs of 12.5, 12.5 and 25 μg/ml, respectively .
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- HY-145102
-
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HSP
Apoptosis
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Cancer
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NCT-58 is a potent inhibitor of C-terminal HSP90. NCT-58 does not induce the heat shock response (HSR) due to its targeting of the C-terminal region and elicits anti-tumor activity via the simultaneous downregulation of HER family members as well as inhibition of Akt phosphorylation. NCT-58 kills Trastuzumab-resistant breast cancer stem-like cells. NCT-58 induces apoptosis in HER2-positive breast cancer cells .
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- HY-168555
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CDK
PROTACs
Apoptosis
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Cancer
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YJ1206 is an orally active, selective CDK12/CDK13 PROTAC degrader with an IC50 of 12.55 nM for in VCaP cells. YJ1206 increases DNA damage, induces apoptosis, and promotes tumor regression in orthotopic WA74 patient-derived xenograft (PDX) mice models of resistant prostate cancer. YJ1206 suppresses tumor growth in vivo in conjunction with AKT pathway inhibitors. YJ1206 is composed of the CDK12/CDK13 degradation agent (HY-168658), a linker (HY-W004328), and a VHL E3 ubiquitin ligase (HY-W453548). (Pink: Navitoclax; Blue: VHL ligand; Black: linker) .
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- HY-N6796
-
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Farnesyl Transferase
Ras
Apoptosis
Phospholipase
TNF Receptor
Atg8/LC3
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Infection
Inflammation/Immunology
Cancer
|
Manumycin A is a polyketide antibiotic and an inhibitor of thioredoxin reductase 1 (TrxR-1). Manumycin A can inhibit the growth of breast cancer cells and exert its anti-tumor activity through LC3. Manumycin A can downregulate the release of pro-inflammatory cytokines in human monocytes stimulated by TNF α, and has potential anti-inflammatory activity. Manumycin A can inhibit the Ras/Raf/ERK1/2 signaling and hnRNP H1 in castration resistant prostate cancer cells to suppress exosome biogenesis and secretion .
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- HY-164477
-
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Androgen Receptor
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Cancer
|
FL442 is an Androgen Receptor (AR) modulator. FL442 exhibits strong inhibitory effects in AR-dependent prostate cancer cells, showing similar inhibitory efficiency to traditional antiandrogen drugs Bicalutamide (HY-14249) and Enzalutamide (HY-70002), while maintaining antiandrogenic activity against the AR mutant F876L, which is highly resistant to Enzalutamide. Pharmacokinetic studies of FL442 in mice reveal a long half-life (8 hours), good targeting (prostate tissue), and metabolic stability, and it effectively inhibits LNCaP tumor growth at low plasma concentrations (30 ng/mL) .
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- HY-149918
-
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Microtubule/Tubulin
Apoptosis
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Cancer
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Antiproliferative agent-23 is a microtubule-destabilizing agent (MDA) and efficiently disturbes the tubulin-microtubule system. Antiproliferative agent-23 induces apoptosis via a mitochondrion-dependent pathway by downregulating the Bcl-2 protein, upregulating Bax and Cyt c proteins, and activating the caspase cascade. Antiproliferative agent-23 initiates reactive oxygen species (ROS)-mediated endoplasmic reticulum stress in A549/CDDP cells (cisplatin resistant cancer cell line) via the PERK/ATF4/CHOP signaling pathway. Antiproliferative agent-23 has anti-tumor activity .
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- HY-155580
-
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Monoamine Oxidase
HSP
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Cancer
|
MAO A/HSP90-IN-2 (compound 4-C) is a dual inhibitor of HSP90and MAO A with the IC50 values of 0.016 and 4.58 μM, respectively. MAO A/HSP90-IN-2 increases HSP70 expression and reduces HER2 and phospho-Akt expression, and decreases IFN-γ induced PD-L1 expression in GL26 cells. MAO A/HSP90-IN-2 inhibits the growth of Temozolomide (HY-17364) -sensitive and -resistant GBM cells, colon cancer, leukemia, non-small cell lung and other cancers, and has potential to inhibit tumor immune escape [1] sup >.
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-
- HY-153321
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BTK-IN-24
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Btk
PROTACs
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Inflammation/Immunology
Cancer
|
NX-5948 (BTK-IN-24) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: ligand for target protein; Blue: CRBN; Black: linker) .
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- HY-147414
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PF-114
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Bcr-Abl
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Cancer
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Vamotinib (PF-114) is a potent, selective and orally active tyrosine kinase inhibitor. Vamotinib inhibits the autophosphorylation of BCR/ABL and BCR/ABL-T315I. Vamotinib induces apoptosis. Vamotinib shows anti-proliferative and anti-tumor activity. Vamotinib has the potential for the research of resistant philadelphia chromosome-positive (Ph+) leukemia. Vamotinib inhibits ABL series kinases with IC50s of 0.49 nM (ABL), 0.78 nM (ABL T315I), 9.5 nM (ABL E255K), 2.0 nM (ABL F317I), 7.4 nM (ABL G250E), 1.0 nM (ABL H396P), 2.8 nM (ABL M351T), 12 nM (ABL Q252H), and 4.1 nM (ABL Y253F), respectively . Vamotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-B0766
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SY801
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Autophagy
Apoptosis
HBV
HCV
HSP
Reactive Oxygen Species
Bcl-2 Family
Glutathione S-transferase
p38 MAPK
NF-κB
Microtubule/Tubulin
ERK
JNK
TNF Receptor
Interleukin Related
CDK
Cyclin G-associated Kinase (GAK)
mTOR
P-glycoprotein
Ferroptosis
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Infection
Inflammation/Immunology
Cancer
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Bicyclol (SY801) is an orally active derivative of the traditional Chinese medicine Schisandra chinensis, which has antiviral, anti-inflammatory, immunomodulatory, antioxidant, anti-steatosis, anti-fibrotic and anti-tumor activities. Bicyclol regulates the expression of heat shock proteins and plays an anti-apoptosis role in hepatocytes. Bicyclol reduces the activation of NF-κB and the levels of inflammatory factors in hepatocytes infected with hepatitis C virus (HCV) by inhibiting the activation of the ROS-MAPK-NF-κB pathway, and prevents ferroptosis in acute liver injury. Bicyclol can change the expression of Mdr-1, GSH/GST and Bcl-2, increase the intracellular concentration of anticancer drugs, and sensitize drug-resistant cells to anticancer drugs. Bicyclol inhibits the proliferation of human malignant hepatoma cells by regulating the PI3K/AKT pathway and the Ras/Raf/MEK/ERK pathway. Bicyclol can be used in the study of chronic hepatitis, acute liver injury, nonalcoholic fatty liver disease, liver fibrosis and hepatocellular carcinoma .
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HY-L169
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446 compounds
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Resistance refers to the decrease in the effectiveness of drugs in treating diseases or symptoms. Due to the increasing global antibiotic resistance, it may threaten our ability to treat common infectious diseases. Drug resistance is also the main cause of chemotherapy failure in malignant tumors. In approximately 50% of cases, drug resistance exists even before chemotherapy begins. There are many mechanisms of anticancer drug resistance, including increased protein expression that leads to drug removal, mutations in drug binding sites, recovery of tumor protein production, and pre-existing genetic heterogeneity in tumor cell populations. In addition, the issue of drug resistance seems to have affected the development of new anticancer drugs. Drug resistance may be caused by various conditions, such as mutations, epigenetic modifications, and upregulation of drug efflux protein expression. Overcoming multidrug resistance in cancer treatment is becoming increasingly important.
MCE designs a unique collection of 446 anti-drug-resistant compounds. It is a good tool to be used for research on cancer and other diseases.
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Cat. No. |
Product Name |
Type |
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- HY-15794G
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Methoxymorpholinyl doxorubicin (GMP); FCE 23762 (GMP); PNU 152243 (GMP)
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Fluorescent Dye
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Nemorubicin (Methoxymorpholinyl doxorubicin) GMP is a GMP-class Nemorubicin (HY-15794). Nemorubicin is a Doxorubicin derivative with potent antitumor activity. Nemorubicin is highly cytotoxic to a variety of tumor cell lines presenting a multidrug-resistant phenotype. Nemorubicin not only intercalate into the duplex DNA, but also result in significant ligands for G-quadruplex DNA segments, stabilizing their structure. Nemorubicin requirs an intact nucleotide excision repair (NER) system to exert its activity .
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Cat. No. |
Product Name |
Type |
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- HY-15794G
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Methoxymorpholinyl doxorubicin (GMP); FCE 23762 (GMP); PNU 152243 (GMP)
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Biochemical Assay Reagents
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Nemorubicin (Methoxymorpholinyl doxorubicin) GMP is a GMP-class Nemorubicin (HY-15794). Nemorubicin is a Doxorubicin derivative with potent antitumor activity. Nemorubicin is highly cytotoxic to a variety of tumor cell lines presenting a multidrug-resistant phenotype. Nemorubicin not only intercalate into the duplex DNA, but also result in significant ligands for G-quadruplex DNA segments, stabilizing their structure. Nemorubicin requirs an intact nucleotide excision repair (NER) system to exert its activity .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P1653
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Antifolate
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Cancer
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EC-1456 is a folate-tubulysin conjugate with significant anti-proliferative activity against FR-positive tumors, including models which were anticancer drug resistant. EC-1456 can be utilized in cancer research .
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- HY-P10743
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Radionuclide-Drug Conjugates (RDCs)
PSMA
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Cancer
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BQ7876 is a probe targeting prostate-specific membrane antigen (PSMA) that contains a DOTA chelator. BQ7876, after being radiolabeled with radionuclide (177Lu), functions in both radionuclide imaging and tumor cell destruction by specifically binding to PSMA. BQ7876 shows potential for research in the field of metastatic castration-resistant prostate cancer (mCRPC) . BQ7876 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P99217
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AMG 102
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c-Met/HGFR
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Cancer
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Rilotumumab (AMG 102) is an anti-HGF (anti-hepatocyte growth factor) monoclonal antibody, inhibits HGF/MET-driven signaling. Rilotumumab shows anti-tumor activity, and can be used in castration-resistant prostate cancer (CRPC) and solid tumor research .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-107271
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- HY-N6932
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- HY-N2360
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- HY-N0944
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- HY-N0790
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- HY-N10765
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- HY-N2104
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- HY-127155
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- HY-N0790R
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Triterpenes
Structural Classification
other families
Terpenoids
Source classification
Plants
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Androgen Receptor
Apoptosis
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Lupeol (Standard) is the analytical standard of Lupeol. This product is intended for research and analytical applications. Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic?triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent?androgen receptor (AR)?inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC) .
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- HY-126170
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- HY-N10264
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(+)-Avrainvillamide; CJ-17,665
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Infection
Alkaloids
Structural Classification
Microorganisms
Pyrrole Alkaloids
Classification of Application Fields
Source classification
Disease Research Fields
Indole Alkaloids
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Antibiotic
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Avrainvillamide ((+)-Avrainvillamide) is a naturally occurring alkaloid with antiproliferative effects, binds to the nuclear chaperone nucleophosmin, a proposed oncogenic protein that is overexpressed in many different human tumors. Avrainvillamide affects cell biology both by directly binding NPM1 and Crm1 as well as by inhibiting the association of these proteins with certain native cellular partners. Avrainvillamide, an antibiotic, inhibits growth of multi-agent resistant Staphylococcus aureus, Streptococcus pyogenes, and Enterococcus faecalis, with MICs of 12.5, 12.5 and 25 μg/ml, respectively .
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- HY-N6796
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Cat. No. |
Product Name |
Chemical Structure |
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- HY-135336AS
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(S)-Verapamil-d7 (hydrochloride) is a deuterium labeled (S)-Verapamil hydrochloride. (S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells[1][2].
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Cat. No. |
Product Name |
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Classification |
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- HY-160053
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Aptamers
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Gint4.T aptamer sodium is a nuclease-resistant RNA aptamer-based antagonist targeting platelet-derived growth factor receptor beta (PDGFRβ) (Kd: 9.6 nM). Gint4.T aptamer sodium inhibits PDGFRβ heterodimerization and EGFR transactivation. It can significantly inhibit cell migration and proliferation, induce differentiation and prevent tumor growth in vivo. Gint4.T aptamer sodium specifically inhibits PDGFRβ-mediated tropism of mesenchymal stem cells (MSCs) toward the tumor microenvironment .
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