Search Result
Results for "
Prostate cancer models
" in MedChemExpress (MCE) Product Catalog:
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-16706
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Remodelin
Maximum Cited Publications
11 Publications Verification
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Histone Acetyltransferase
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Cancer
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Remodelin is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells. Remodelin inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model .
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- HY-145388
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PROTACs
Epigenetic Reader Domain
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Cancer
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AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity .
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- HY-16706A
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Histone Acetyltransferase
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Cancer
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Remodelin hydrobromide is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin hydrobromide inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells. Remodelin hydrobromide inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin hydrobromide enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model .
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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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- 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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- HY-106431
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Olpadronate; OLP
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Others
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Metabolic Disease
Cancer
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Olpadronic acid (Olpadronate) is an orally active amino-bisphosphonate and inhibits bone resorption. Olpadronic acid also prevents bone destruction and tumor growth in the skeletal prostate cancer mouse model. Olpadronic acid can be used for research of osteoporosis, malignancies and rheumatoid arthritis .
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- HY-P4144
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Phor18-LHRH (338613); EP-100
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GnRH Receptor
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Endocrinology
Cancer
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Onvitrelin ucalontide ([Phor18-LHRH (338613)]) is an analogue of luteinizing hormone releasing hormone (LHRH) with antineoplastic activity. Onvitrelin ucalontide is a peptide with sequences of KFAKFAKKFAKFAKKFAKQHWSYGLRPG. Onvitrelin ucalontide effectively inhibits breast cancer, ovarian cancer and prostate cancer xenografts in mouse model .
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- HY-148838
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c-Myc
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Cancer
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c-Myc inhibitor 8 (compound 56) is a c-Myc inhibitor. c-Myc inhibitor 8 effectively inhibits cell viability of a variety of cancer cells. c-Myc inhibitor 8 inhibits human prostate and lung cancer growth in mouse models. c-Myc inhibitor 8 can be used for cancer research .
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- HY-169078
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Histone Methyltransferase
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Cancer
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ML234 is a dual inhibitor against EZH2/LSD1 with IC50 values of 0.09 and 0.12 μM, respectively. ML234 displays an excellent antiproliferative capacity against prostate cancer cell lines LNCAP, PC3 and 22RV1. ML234 suppresses the tumor growth in the 22RV1 xenograft mouse model. ML234 is promising for research of anticancer agents in prostate cancer .
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- HY-125065
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Androgen Receptor
5 alpha Reductase
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Endocrinology
Cancer
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MK-4541 is an orally active and selective androgen receptor (AR) modulator. MK-4541 acts as an antagonist to inhibit 5α-reductase. MK-4541 inhibits proliferation and induces apoptosis in AR positive prostate cancer cells. MK-4541 significantly inhibited the growth of R3327-G prostate tumors in xenograft mouse model .
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- HY-136990
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Others
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Cancer
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GLPG0259 is a ATP-competitive inhibitor of MAPK-activated protein kinase 5 (MK5) with oral activity. GLPG0259 reduces inflammation and bone destruction in a mouse model of collagen-induced arthritis. GLPG0259 also inhibited the metastasis of prostate cancer (PCa) cells .
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- HY-168300
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Reactive Oxygen Species
Apoptosis
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Inflammation/Immunology
Cancer
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Antiangiogenic agent 7 (Compound 1) can induce cell apoptosis, increase Reactive Oxygen Species, and inhibit the intracellular enzyme thioredoxin reductase. Antiangiogenic agent 7 has anti-cancer activity, with an IC50 of 0.08-3.5 μM against cervical cancer cells HeLa, prostate cancer cells PC-3, and non-small cell lung cancer A549. Antiangiogenic agent 7 inhibits tumor growth in mouse xenograft models .
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- HY-16247
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HE3235
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Biochemical Assay Reagents
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Cancer
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Apoptone, synthetic analogue of 3β-androstanediol, is an orally bioavailable anticancer agent. Apoptone is active in rodent models of prostate and breast cancer . Apoptone 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-168201
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PROTACs
Histone Acetyltransferase
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Cancer
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MJP6412 is a potent degrader histone acetyltransferases p300/CBP, with DC50 of 1.6 and 1.2 nM for p300 and CBP, respectively. MJP6412 plays an important role in cancer research .
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- HY-155502
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Aldose Reductase
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Cancer
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AKR1C3-IN-10 (compound 5r) is a selective AKR1C3 inhibitor (IC50=51 nM). AKR1C3-IN-10 shows good activity in a prostate cancer xenograft model .
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- HY-149297
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PSMA
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Cancer
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PSMA-IN-1 (compound 23) is an inhibitor of PSMA with a Ki value of 2.49 nM. PSMA-IN-1 inhibits tumor growth with high selectivity and specificity in PSMA+ xenograft models. PSMA-IN-1 is a NIR probe (λEX: 620 nm; λEM: 670 nm) used for tumor disappearance. PSMA-IN-1 can be used for research on prostate cancer .
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- HY-P10744
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Radionuclide-Drug Conjugates (RDCs)
PSMA
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Cancer
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BQ7859 is a probe targeting PSMA that contains a NOTA chelator and demonstrates excellent imaging performance. BQ7859 can be labeled with various radionuclides, such as 68Ga, 18F, 55Co, and 111In. In a mouse prostate cancer xenograft model, BQ7859 (labeled with 111In) efficiently accumulates in tumor regions in a PSMA-dependent manner and provides high-contrast tumor imaging. BQ7859 shows potential for research in prostate cancer imaging, particularly in positron emission tomography (PET) and single-photon emission computed tomography (SPECT) . BQ7859 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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- HY-155543
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Androgen Receptor
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Cancer
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Anticancer agent 135 (compound 26h) is a potent androgen receptor (AR) antagonist. Anticancer agent 135 can effectively block AR nuclear translocation and inhibit AR/AR-V7 heterodimerization, thereby inhibiting downstream gene transcription. Anticancer agent 135 displays potent robust efficacy in prostate cancer xenograft models .
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- HY-P1416
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Foxy-5
5 Publications Verification
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Wnt
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Cancer
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Foxy-5, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model .
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- HY-155458
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PARP
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Inflammation/Immunology
Cancer
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HYDAMTIQ is a PARP-1/2 inhibitor (IC50: 29-38 nM) with anticancer, anti-inflammatory, and ischemic protective effects. HYDAMTIQ inhibits pulmonary PARP activity, is effective against allergen-induced cough and dyspnea, and inhibits bronchial hyperresponsiveness to methacholine. HYDAMTIQ has broad-spectrum tumor suppressor effects, including ovarian and breast cancers, prostate and pancreatic tumors, and glioblastoma multiforme. HYDAMTIQ has demonstrated in vivo efficacy in animal models of cerebral ischemia, asthma, cancer, and more .
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- HY-P10759
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Peptide-Drug Conjugates (PDCs)
Aminopeptidase
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Cancer
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DTS-201 sodium (CPI-0004Na) is a peptidic prodrug of Doxorubicin (HY-15142A). DTS-201, comprising the tetrapeptide portion, is cleaved by endopeptidases in the tumor environment to produce metabolites that subsequently enter the cell and are converted to active Doxorubicin. DTS-201 shows antitumoral efficacy in tumor xenograft models of prostate, breast, and lung cancer .
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- HY-122611
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Androgen Receptor
Apoptosis
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Cancer
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CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
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- HY-122611A
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Androgen Receptor
Apoptosis
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Cancer
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CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 hydrochloride induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 hydrochloride is well tolerated in the prostate cancer mouse model
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- HY-P1416A
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Wnt
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Cancer
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Foxy-5 TFA, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 TFA triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 TFA effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model .
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- HY-147081
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AGRO-100
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Histone Methyltransferase
Bcl-2 Family
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Cancer
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AS 1411 (AGRO-100) is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. AS 1411 works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. AS 1411-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity .
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- HY-149091
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Histone Demethylase
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Cancer
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KDM5B-IN-4 (compound 11ad) is a lysine demethylase 5B (KDM5B) inhibitor with an IC50 of 0.025 μM KDM5B-IN-4 increases substrate H3K4me1/2/3 level by inhibiting KDM5B in PC-3 cells. KDM5B-IN-4 downregulates PI3K/AKT. KDM5B-IN-4 reduces tumor volume in mice and shows less toxic to organs .
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- HY-142743
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Epigenetic Reader Domain
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Cancer
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Y08175 is a potent CBP bromodomain inhibitor. Y08175 exhibits considerable inhibitory effect with IC50s of 37 and 178.15 nM against CBP bromodomain in AlphaScreen assay and HTRF assay, respectively. Y08175 can be used for the research of prostate cancer .
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- HY-163062
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Microtubule/Tubulin
Apoptosis
Complement System
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Cancer
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Tubulin/NRP1-IN-1 (compound TN-2) is a dual inhibitor of Tubulin and NRP1 with IC50s of 0.71 and 0.85 μM, respectively. Tubulin/NRP1-IN-1 significantly inhibits the viability of prostate tumor cell lines and induces apoptosis .
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- HY-163608
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PSMA
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Cancer
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Ac-macropa is a PSMA-targeted Actinium-225 Conjugate, and can be used for study of prostate cancer .
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-
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- HY-147696
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HSP
AMPK
Reactive Oxygen Species
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Cancer
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SMTIN-T140 (compound 6a) is a potent TRAP1 (tumor-necrosis-factor-receptor associated protein 1) inhibitor, with an IC50 of 1.646 μM. SMTIN-T140 shows anticancer activity. SMTIN-T140 leads to mitochondrial dysfunction, increases mitochondrial ROS production and activates AMPK. SMTIN-T140 potently suppressed tumor growth without any noticeable in vivo toxicity in a mouse model xenografted with PC3 prostate cancer cells .
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- HY-146494
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Androgen Receptor
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Cancer
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Androgen receptor antagonist 5 (compound 42f) is a potent androgen receptor (AR) antagonist with an IC50 value of 6.17 μM. Androgen receptor antagonist 5 can effectively impair AR nuclear translocation, reducing the levels of nuclear AR, and disrupts AR-mediated gene regulation. Androgen receptor antagonist 5 has antiproliferative activity against LNCaP and exhibits antitumor activity in LNCaP xenograft tumor mice model. Androgen receptor antagonist 5 can be used for researching prostate cancer .
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- HY-122611R
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Androgen Receptor
Apoptosis
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Cancer
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CSRM617 (Standard) is the analytical standard of CSRM617. This product is intended for research and analytical applications. CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
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- HY-N1486R
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Apoptosis
Endogenous Metabolite
NF-κB
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Inflammation/Immunology
Cancer
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CSRM617 (Standard) is the analytical standard of CSRM617. This product is intended for research and analytical applications. CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
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- HY-133005
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4-Desacetylvinblastine; Desacetylvincaleukoblastine
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Drug Intermediate
Drug Metabolite
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Cancer
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Desacetylvinblastine (4-Desacetylvinblastine) is the major metabolite of Vinblastine (HY-13780) and a cytotoxic agent. When used alone, desacetylvinblastine has poor anti-tumor effects, but it can exert significant anti-tumor activity when in the presence of specific conjugates .
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- HY-169349
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Androgen Receptor
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Cancer
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Androgen receptor antagonist 12 (Compound EF2) is an orally active Androgen receptor (AR) antagonist (IC50: 0.30 μM). Androgen receptor antagonist 12 inhibits transcriptional activity of variant AR mutants and and the proliferation of AR-positive PCa cell lines. Androgen receptor antagonist 12 blocks AR nuclear translocation. Androgen receptor antagonist 12 inhibits tumor growth in a C4-2B xenograft mouse model. Androgen receptor antagonist 12 can be used for prostate cancer (PCa) research .
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- HY-158101
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CC-94676
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PROTACs
Androgen Receptor
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Cancer
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BMS-986365 (CC-94676) is an orally active and selective targeted androgen receptor (AR) PROTAC degrader, capable of inducing cereblon (CRBN) E3 ligase-dependent ubiquitination and degradation of the androgen receptor (AR), as well as various AR mutants. BMS-986365 shows significant in vivo potency, degrading AR, inhibiting AR signaling, and restricting tumor growth in animal models of advanced prostate cancer. (Blue: HY-W247437; Black: linker (HY-W126831); Pink: HY-168697) .
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- HY-163611
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ROR
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Cancer
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XY039 (compound 13e) is a RORγ inverse agonist with the IC50 of 0.55 μM. XY039 induces cell apoptosis and shows antiproliferative activity in vivoand in vitro .
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- HY-163612
-
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ROR
Apoptosis
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Cancer
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XY077 (compound 14a) is a RORγ inverse agonist with the IC50 of 0.004 μM. XY077 induces cell apoptosis and shows antiproliferative activity in vivoand in vitro .
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- HY-W017540
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ATP Synthase
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Cardiovascular Disease
Neurological Disease
Metabolic Disease
Cancer
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Cyclocreatine, a creatine analogue, acts as a brain-penetrant and potent bioenergetic protective agent by providing high levels of ATP. Cyclocreatine can be phosphorylated and dephosphorylated by creatine kinases. Cyclocreatine suppresses creatine metabolism ameliorating the cognitive, autistic and epileptic phenotype in a mouse model of creatine transporter defciency. Cyclocreatine protects against ischemic injury and enhances cardiac recovery during early reperfusion in dogs and rats. Cyclocreatine decreases plaque-adjacent neuronal dystrophy in TREM2-deficient mice with amyloid-β pathology. Cyclocreatine is proming for research of ischemic heart disease, cardiovascular diseases, Alzheimer’s disease and other neurodegenerative diseases associated with microglial dysfunction, prostate cancer .
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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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-
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- HY-159922
-
|
Androgen Receptor
|
Cancer
|
AR antagonist 9 is an orally bioavailable selective androgen receptor (AR) antagonist that exerts anticancer effects by disrupting the dimerization of AR ligand-binding domains, showing potential for overcoming drug resistance in prostate cancer (PCa). Its AR antagonistic activity has an IC50 value of 0.051 μM, comparable to Enzalutamide (HY-70002) (IC50 = 0.060 μM). AR antagonist 9 demonstrated superior efficacy against ARF876L/T877A and ARW741C mutants compared to Enzalutamide (HY-70002). Furthermore, AR antagonist 9 exhibited favorable pharmacokinetic properties, with an oral bioavailability of F = 66.24% in rats. In the LNCaP xenograft mouse model, oral administration of AR antagonist 9 significantly inhibited tumor growth. AR antagonist 9 holds promise for research into overcoming PCa drug resistance .
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Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1416
-
Foxy-5
5 Publications Verification
|
Wnt
|
Cancer
|
Foxy-5, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model .
|
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- HY-P1416A
-
|
Wnt
|
Cancer
|
Foxy-5 TFA, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 TFA triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 TFA effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model .
|
-
- HY-P4144
-
Phor18-LHRH (338613); EP-100
|
GnRH Receptor
|
Endocrinology
Cancer
|
Onvitrelin ucalontide ([Phor18-LHRH (338613)]) is an analogue of luteinizing hormone releasing hormone (LHRH) with antineoplastic activity. Onvitrelin ucalontide is a peptide with sequences of KFAKFAKKFAKFAKKFAKQHWSYGLRPG. Onvitrelin ucalontide effectively inhibits breast cancer, ovarian cancer and prostate cancer xenografts in mouse model .
|
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- HY-P10744
-
|
Radionuclide-Drug Conjugates (RDCs)
PSMA
|
Cancer
|
BQ7859 is a probe targeting PSMA that contains a NOTA chelator and demonstrates excellent imaging performance. BQ7859 can be labeled with various radionuclides, such as 68Ga, 18F, 55Co, and 111In. In a mouse prostate cancer xenograft model, BQ7859 (labeled with 111In) efficiently accumulates in tumor regions in a PSMA-dependent manner and provides high-contrast tumor imaging. BQ7859 shows potential for research in prostate cancer imaging, particularly in positron emission tomography (PET) and single-photon emission computed tomography (SPECT) . BQ7859 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
|
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- HY-P10759
-
|
Peptide-Drug Conjugates (PDCs)
Aminopeptidase
|
Cancer
|
DTS-201 sodium (CPI-0004Na) is a peptidic prodrug of Doxorubicin (HY-15142A). DTS-201, comprising the tetrapeptide portion, is cleaved by endopeptidases in the tumor environment to produce metabolites that subsequently enter the cell and are converted to active Doxorubicin. DTS-201 shows antitumoral efficacy in tumor xenograft models of prostate, breast, and lung cancer .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
|
Classification |
-
- HY-16247
-
HE3235
|
|
Alkynes
|
Apoptone, synthetic analogue of 3β-androstanediol, is an orally bioavailable anticancer agent. Apoptone is active in rodent models of prostate and breast cancer . Apoptone is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
Cat. No. |
Product Name |
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Classification |
-
- HY-147081
-
AGRO-100
|
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Aptamers
|
AS 1411 (AGRO-100) is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. AS 1411 works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. AS 1411-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity .
|
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