Search Result
Results for "
Prostate cancer model
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
4
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-145388
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PROTACs
SWI/SNF Complex
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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-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 (DC50 of 10-40 nM). BMS-986365 is 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 no degradation of the close AR family members estrogen receptor (ER), progesterone receptor (PR), and glucocorticoid receptor (GR). BMS-986365 shows significant in vivo potency, degrading AR, inhibiting AR signaling, and restricting tumor growth in animal models of advanced prostate cancer. BMS-986365 can be used for the study of metastatic castration-resistant prostate cancer (mCRPC) .
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- HY-16706
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Remodelin
Maximum Cited Publications
17 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-P990673
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DSTP-3086S Antibody; RG-7450 Antibody
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ADC Antibody
Transmembrane Glycoprotein
Mitosis
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Cancer
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Vandortuzumab (DSTP-3086S Antibody; RG-7450 Antibody) is a humanized anti-STEAP1 IgG1 antibody and antimitotic agent that can be conjugated with MMAE (HY-15162) to form the antibody-drug conjugate (ADC) Vandortuzumab vedotin. Vandortuzumab vedotin specifically binds to STEAP1 and drives internalization of the complex, releasing the MMAE (HY-15162) payload intracellularly. After binding to tubulin, MMAE inhibits cell division and induces cell death. Vandortuzumab exhibits antitumor activity in preclinical xenograft models of prostate cancer and can be used for research related to metastatic castration-resistant prostate cancer (mCRPC) .
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- HY-157941
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ATM/ATR
Checkpoint Kinase (Chk)
DNA/RNA Synthesis
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Cancer
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ART0380 is a potent, selective and orally active ATR kinase inhibitor. ART0380 potently inhibits human ATR-ATRIP complex with an IC50 of 51.7 nM. ART0380 binds the ATP pocket of the ATR-ATRIP complex, blocks ATR-dependent Chk1 serine 345 phosphorylation, and induces cell cycle disorder and DNA damage. ART0380 demonstrates potent and selective antitumor activity in preclinical models with varying types of ataxia-telangiectasia mutated (ATM) gene aberrancy. ART0380 can be used for the research of cancer, such as colorectal cancer and prostate cancer .
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- HY-173158
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PROTACs
Histone Acetyltransferase
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Cancer
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AUR1545 is a selective KAT2A/KAT2B ((GCN5/PCAF)) PROTAC degrader that induces monocyte differentiation and inhibits the growth of acute myeloid leukemia cells. AUR1545 inhibits cell growth, induces epithelial differentiation and suppresses tumor growth in small cell lung cancer models. AUR1545 inhibits cell growth and induces differentiation in neuroendocrine prostate cancer cells and primary patient-derived organoids. AUR1545 is applicable to research related to acute myeloid leukemia, small cell lung cancer and neuroendocrine prostate cancer .
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- HY-163410
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PROTACs
Epigenetic Reader Domain
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Cancer
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AU-24118 is a selective and orally bioavailable PROTAC degrader of mSWI-SNF ATPases (SMARCA2 and SMARCA4) and PBRM1. AU-24118 integrates a bait moiety binding to the bromodomains of SMARCA2 and SMARCA4, along with a ligand moiety for CRBN ligase. AU-24118 demonstrates tumor regression in prostate cancer model. AU-24118 can be studied to combat prostate cancer. (Pink: PBRM1/SMARCA2,4 ligand (HY-171774); Blue: CRBN ligand (HY-171775)) .
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- HY-142870
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Pyruvate Carboxylase (PC)
Apoptosis
β-catenin
ERK
Wnt
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Cancer
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ZY-444 is an anti-cancer agent, targeting pyruvate carboxylase (PC). ZY-444 suppresses the Wnt/β-catenin/Snail signaling pathway by blocking nuclear translocation of β-catenin. ZY-444 selectively inhibits proliferation, migration, and invasion and induces apoptosis in cancer cells. ZY-444 exhibits potent anti-tumor in cancer mouse models. ZY-444 can be used for the study of breast cancer, lung cancer (NSCLC), prostate cancer and iodine-refractory thyroid cancer .
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- HY-147081
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AS 1411
2 Publications Verification
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-70006
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TOK-001; VN-124-1
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Molecular Glues
Androgen Receptor
MNK
Cytochrome P450
Apoptosis
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Cancer
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Galeterone (TOK-001) is a potent, orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. Galeterone also functions as a CYP17 inhibitor (IC50 = 47 nM). Galeterone induces cell apoptosis. Galeterone inhibits tumor growth in human prostate cancer xenograft mouse models. Galeterone can be used for castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) research [1][2].
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- HY-P1416
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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-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-P9992
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BAY-2315497; PSMA-TTC
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PSMA
Apoptosis
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Cancer
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Peligifatamab is a PSMA-targeted α-radioimmunoconjugate with an EC50 of 1.2 nM against human targets. Peligifatamab induces DNA damage, DNA double-strand breaks, cell cycle arrest and apoptosis (Apoptosis) in PSMA-positive prostate cancer cells. Peligifatamab reduces cell viability in a manner dependent on cellular PSMA expression levels. Peligifatamab inhibits tumor growth and tumor-induced abnormal bone growth in prostate cancer bone metastasis models. Peligifatamab exhibits antitumor efficacy in subcutaneous prostate cancer models and xenograft models. Peligifatamab can be used for the research of metastatic castration-resistant 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-176763
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Sec61
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Cancer
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KZR-261 is a Sec61 translocase inhibitor. KZR-261 binds directly to the Sec61 channel, thereby inhibiting the biosynthesis of certain Sec61 substrate proteins, including oncogenic factors. KZR-261 activates the endoplasmic reticulum stress response. KZR-261 exhibits broad in vitro anticancer activity. KZR-261 shows antitumor efficacy in mouse models of cancer. KZR-261 can be used for the research of multiple myeloma, colorectal cancer, small cell lung cancer, pancreatic cancer, prostate cancer, non-Hodgkin's lymphoma, and mantle cell lymphoma .
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- HY-45661
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NUV-422
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CDK
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Neurological Disease
Cancer
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Inixaciclib (NUV-422) is a blood-brain barrier-penetrant inhibitor of CDK2, CDK4 and CDK6. Inixaciclib inhibits cancer cell growth. Inixaciclib induces anti-tumor activity in xenograft models of glioblastoma, CDK4/CDK6 inhibitor-resistant HR + HER2 - metastatic breast cancer, and anti-androgen-resistant prostate cancer. Inixaciclib can be used for the research of relapsed or metastatic castration-resistant prostate cancer .
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- HY-19337
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BAY 1896953; ORM-15341
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Androgen Receptor
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Cancer
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Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a Ki value of 8 nM for rat wild-type AR and an IC50 value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .
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- HY-12842
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IAP
Survivin
Apoptosis
Caspase
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Inflammation/Immunology
Cancer
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UC-112 is a XIAP inhibitor with anticancer activity. UC-112 selectively downregulates and degrades survivin via the ubiquitin-mediated proteasomal degradation pathway. UC-112 reduces XIAP levels in in vivo tumor models. UC-112 activates caspase-3/7 and caspase-9, and induces cancer cell apoptosis. UC-112 is applicable to studies on melanoma, prostate cancer and cancer-related research .
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- HY-12929
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SU093
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Pim
Apoptosis
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Cancer
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NSC756093 (SU093) is a GBP1:PIM1 interaction inhibitor. NSC756093 binds to GBP1-PIM1 with a Kd of 38 nM. NSC756093 suppresses proliferation, reduces migration, induces G1 phase cell-cycle arrest, and increases apoptotic cell death in ovarian cancer cells. NSC756093 reduces cellular proteasomal activity, induces accumulation of ubiquitinated proteins, and restrains tumor progression and lung metastasis in murine ovarian cancer xenograft models. NSC756093 increases sensitivity of prostate cancer cells to Docetaxel (HY-B0011) and sensitizes GBP1-overexpressing ovarian cancer cells to Paclitaxel (HY-B0015). NSC756093 can be used for the research of prostate cancer and ovarian cancer .
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- HY-170329
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PROTACs
Androgen Receptor
Apoptosis
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Cancer
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PROTAC AR Degrader-8 is the PROTAC degrader for androgen receptor (AR) that degrades AR-FL with DC50s of 0.018 μM and 0.14 μM in 22Rv1 cell and LNCaP cell, degrades AR-V7 with DC50 of 0.026 μM in 22Rv1 cell. PROTAC AR Degrader-8 inhibits the proliferation of cancer cell 22Rv1 and LNCaP with IC50 values of 0.038 μM and 1.11 μM. PROTAC AR Degrader-8 arrests cell cycle at G2/M phase, induces apoptosis in 22Rv1 cell. PROTAC AR Degrader-8 exhibits anticancer efficacy in mouse and zebrafish model. PROTAC AR Degrader-8 can be used for the research of prostate cancer, castration-resistant prostate cancer .
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- HY-149433
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PROTACs
Androgen Receptor
Apoptosis
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Cancer
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BWA-522 is an orally active PROTAC degrader targeting full-length androgen receptor (AR-FL) and androgen receptor splice variant 7 (AR-V7). BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor, suppresses AR downstream signaling proteins and induces cancer cells apoptosis. BWA-522 inhibits tumor growth in LNCaP xenograft mouse model. BWA-522 can be used for the research of prostate cancer .
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- HY-N7043
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Apoptosis
PPAR
NF-κB
p38 MAPK
ERK
Androgen Receptor
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Inflammation/Immunology
Cancer
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Isosilybin A is a PPARγ agonist that can be isolated from silymarin. Isosilybin A activates extrinsic and intrinsic pathways of apoptosis through targeting of the Akt-NF-kB-AR axis. Isosilybin A can relieve the inflammatory response in the rosacea model via inhibiting Erk and p38 signaling pathways and M1 macrophage polarization, with its targets related to RELA and VEGFA. Isosilybin A has anti-prostate cancer (PCA) activity [1][2][3].
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- HY-149862
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PROTACs
Androgen Receptor
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Cancer
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ARD-2051 is a selective and orally active androgen receptor (AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC50 values of 0.6 nM for AR protein degradation in both the LNCaP and VCaP prostate cancer cell lines. ARD-2051 exhibits effective anti-tumor activity in VCaP xenograft mice model. ARD-2051 can be used for the research of prostate cancer (Pink: AR ligand (HY-400666), Blue: CRBN Ligand (HY-14658), Black: Linker) .
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- HY-136990
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p38 MAPK
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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-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-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-147081A
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AGRO-100 sodium
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Histone Methyltransferase
Bcl-2 Family
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Cancer
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AS 1411 (AGRO-100) sodium is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 sodium 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 sodium reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. S 1411 sodium works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. S 1411 sodium-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-175652
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PROTACs
Adenosine Receptor
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Cancer
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AZD9750 is an orally active, Cereblon (CRBN)-recruiting, androgen receptor (AR)-targeted PROTAC degrader. AZD9750 induces the proteasome-dependent degradation of both wild-type AR and the drug-resistant mutant AR L702H, thereby inhibiting the AR signaling pathway. AZD9750 suppresses tumor growth in mouse prostate cancer xenograft models and has been utilized in prostate cancer research .
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- HY-16232
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D 19575; Glucosylifosfamide mustard
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Apoptosis
Caspase
Bcl-2 Family
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Cancer
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Glufosfamide is a glucose-conjugated alkylating cytotoxic agent and a derivative of Ifosfamide (HY-17419). Glufosfamide induces apoptosis frequency and increase the expression of caspase-9 and caspase-3 in cancer cells. Glufosfamide shows great anti-tumor activity in MiaPaCa-2-RFP mouse model. Glufosfamide can be used for the study of hepatocellular carcinoma, prostate cancer and pancreatic carcinoma .
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- HY-A0287
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Clomifene; (Z/E)-Enclomiphene; (Z/E)-Enclomifene
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Estrogen Receptor/ERR
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Metabolic Disease
Cancer
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Clomiphene (Clomifene; (Z/E)-Enclomiphene; (Z/E)-Enclomifene) is an orally active ovulation-inducing agent. Clomiphene binds to hypothalamic estrogen receptors to elevate FSH levels, and exhibits antiestrogenic or estrogenic properties. Clomiphene can induce erturbations during meiotic maturation and cytogenetic abnormalities in mouse oocytes. Clomiphene ameliorates memory impairment in PCOS models. Clomiphene mobilizes cytosolic calcium and reduces viability in prostate cancer cells. Clomiphene can be used for the research of polycystic ovary syndrome (PCOS) and prostate cancer .
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- HY-170933
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SGK
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Cancer
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SGK1-IN-6 is a selective SGK1 inhibitor with an IC50 of 0.39 μM, showing selectivity over SGK2/3. SGK1-IN-6 inhibits cancer cell migration and invasion, improves SGK1 protein thermal stability. SGK1-IN-6 decreases SGK1 protein levels in tumor tissues, suppresses tumor growth in mouse xenograft models. SGK1-IN-6 can be used for the research of prostate cancer .
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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-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-147696
-
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HSP
AMPK
Reactive Oxygen Species (ROS)
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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-70006A
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TOK-001 hydrochloride; VN-124-1 hydrochloride
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Molecular Glues
Androgen Receptor
MNK
Cytochrome P450
Apoptosis
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Cancer
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Galeterone (TOK-001) hydrochloride is a potent, orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. Galeterone hydrochloride also functions as a CYP17 inhibitor (IC50 = 47 nM). Galeterone hydrochloride induces cell apoptosis. Galeterone hydrochloride inhibits tumor growth in human prostate cancer xenograft mouse models. Galeterone hydrochloride can be used for castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) research [1][2].
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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-124067
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IKK
JAK
STAT
NF-κB
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Cancer
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EC-70124 is an orally active multikinase inhibitor targeting IKKβ and JAK2. EC-70124 blocks IkB phosphorylation and STAT3 (Tyr705) activation, suppressing NF-κB nuclear translocation and STAT3 transcriptional activity. EC-70124 reduces tumor growth and cancer stem cell (CSC) populations in prostate cancer cells and xenograft models. EC-70124 is promising for research of 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-A0287S
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Clomifene-d5 hydrochloride; (Z/E)-Enclomiphene-d5 hydrochloride; (Z/E)-Enclomifene-d5 hydrochloride
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Isotope-Labeled Compounds
Estrogen Receptor/ERR
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Metabolic Disease
Cancer
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Clomifene (Clomifene; (Z/E)-Enclomiphene; (Z/E)-Enclomifene)-d5 hydrochloride is a deuterium labeled Clomifene hydrochloride (HY-A0287A). Clomiphene hydrochloride is an orally active ovulation-inducing agent. Clomiphene hydrochloride binds to hypothalamic estrogen receptors to elevate FSH levels, and exhibits antiestrogenic or estrogenic properties. Clomiphene hydrochloride can induce erturbations during meiotic maturation and cytogenetic abnormalities in mouse oocytes. Clomiphene hydrochloride ameliorates memory impairment in PCOS models. Clomiphene hydrochloride mobilizes cytosolic calcium and reduces viability in prostate cancer cells. Clomiphene hydrochloride can be used for the research of polycystic ovary syndrome (PCOS) and prostate cancer .
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- HY-106219
-
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Microtubule/Tubulin
P-glycoprotein
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Cancer
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BMS 275183 is a potent, orally active analogue of Paclitaxel (HY-B0015). BMS 275183 can stabilize microtubules and exhibits antitumor activity in in vivo tumor models. BMS 275183 is active in vitro against Paclitaxel-resistant tumors including those harboring tubulin mutations or overexpressing P-glycoprotein. BMS 275183 can be used for cancer research, such as non-small cell lung cancer (NSCLC) and prostate carcinoma .
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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-179056
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PROTACs
PSMA
Androgen Receptor
HSP
Apoptosis
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Cancer
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Psa-AR is a PROTAC degrader targeting PSMA, with a Kd of 7.2 nM. Psa-AR exhibits strong degradation capabilities for AR, AR-V7, and HSP90, and induces cell apoptosis. Psa-AR demonstrates potent tumor suppressive activity in the 22Rv1 xenograft tumor model. Psa-AR can be used in the research of castration-resistant prostate cancer .
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- HY-175243
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Adenosine Deaminase
Apoptosis
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Cancer
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ADAR1-IN-1 is a potent ADAR1 inhibitor. ADAR1-IN-1 significantly suppressed DU-145 cell proliferation (IC50 = 1.11 μM), clonogenicity, migration, and invasion, arrests cell cycle, and induces apoptosis. ADAR1-IN-1 safely and effectively inhibits tumor growth. ADAR1-IN-1 can be used for the study of prostate cancer (PCa) .
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- HY-175248
-
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PSMA
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Cancer
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PSMA-DIM is a dimeric PSMA ligand with a Kd of 37.09 nM for LNCaP cells. PSMA-DIM can be radiolabeled with [ 68Ga]Ga to form [ 68Ga]Ga-PSMA-DIM. [ 68Ga]Ga-PSMA-DIM can effectively distinguish between cells and animal models with different expression levels of PSMA. [ 68Ga]Ga-PSMA-DIM exhibits high LNCaP cells uptake and tumor uptake peak values. PSMA-DIM can be used for the study of prostate cancer (PCa) .
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- HY-P10992
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PI3K
Akt
mTOR
Caspase
Apoptosis
Bcl-2 Family
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Cancer
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YVPGP is an oligopeptide exacted from Anthopleura anjunae. YVPGP has a significant antitumor activity by mediating PI3K/AKT/mTOR signaling pathway. YVPGP arrests DU-145 cells in the S phase and induces apoptosis via mitochondrial and death receptor pathways (caspase3, 7, 8, 9). YVPGP effectively inhibits tumor growth in DU-145 xenografts mice model, promising for prostate cancer research .
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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-P99881
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ABBV 176
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Antibody-Drug Conjugates (ADCs)
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Cancer
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Rolinsatamab talirine (ABBV 176) is a prolactin receptor (PRLR)-targeting antibody-drug conjugate (ADC), compoused of Rolinsatamab (HY-P99238) and SGD-1882 (HY-101127). Rolinsatamab talirine binds to PRLR to deliver a cytotoxin to tumor cells. Rolinsatamab talirine induces DNA damage, and exhibits cytotoxicity against multiple breast tumor models, including triple negative and low PRLR-expressing models. Rolinsatamab talirine demonstrates enhanced anti-tumor activity in several breast cancer models. Rolinsatamab talirine can be used for the research of breast cancer, hepatocellular carcinoma, ovarian cancer, endometrial cancer, prostate cancer, colorectal cancer, adrenocortical carcinoma, and solid tumors .
|
-
-
- HY-A0287A
-
|
Clomifene hydrochloride; (Z/E)-Enclomiphene hydrochloride; (Z/E)-Enclomifene hydrochloride
|
Estrogen Receptor/ERR
|
Metabolic Disease
Cancer
|
|
Clomiphene (Clomifene; (Z/E)-Enclomiphene; (Z/E)-Enclomifene) hydrochloride is an orally active ovulation-inducing agent. Clomiphene hydrochloride binds to hypothalamic estrogen receptors to elevate FSH levels, and exhibits antiestrogenic or estrogenic properties. Clomiphene hydrochloride can induce erturbations during meiotic maturation and cytogenetic abnormalities in mouse oocytes. Clomiphene hydrochloride ameliorates memory impairment in PCOS models. Clomiphene hydrochloride mobilizes cytosolic calcium and reduces viability in prostate cancer cells. Clomiphene hydrochloride can be used for the research of polycystic ovary syndrome (PCOS) and prostate cancer .
|
-
-
- HY-111170
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
STA-9584 is a potent vascular disrupting agent (VDA) that targets tubulin. STA-9584 exhibits potent antitumor activity in mouse xenograft model by selectively targeting microvasculature at both the center and periphery of tumors. STA-9584 can be used for research in prostate and breast cancer .
|
-
- HY-175454
-
|
|
DNA/RNA Synthesis
PDGFR
Oxidative Phosphorylation
Mitochondrial Metabolism
|
Cancer
|
|
YH-0623 is an orally active mitochondrial RNA polymerase (POLRMT) inhibitor (IC50 = 50.48 nM, Nanoluciferase Bioluminescence Resonance Energy Transfer (NanoBRET) assay). YH-0623 exhibits antiproliferative effects on 22Rv1 cells by reducing the expression of mitochondrial-related genes. YH-0623 inhibits 22Rv1 cell growth, colony formation, and the expression of OXPHOS-related proteins. YH-0623 significantly inhibits tumor growth in a prostate cancer xenograft mouse model. YH-0623 is indicated for prostate cancer research .
|
-
- HY-168201
-
|
|
PROTACs
Histone Acetyltransferase
|
Cancer
|
|
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 .
|
-
- HY-155502
-
|
|
Aldose Reductase
|
Cancer
|
|
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 .
|
-
- HY-149297
-
|
|
PSMA
|
Cancer
|
|
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 .
|
-
- HY-P11261
-
|
|
PSMA
|
Cancer
|
AAZTA-NI-PSMA-093 is a bispecific agent targeting prostate-specific membrane antigen (PSMA) with an IC50 value for PSMA of 87.48 nM. AAZTA-NI-PSMA-093 has a PSMA targeting module and an oxygen-sensitivity module (hypoxia-sensitive NI-moiety). AAZTA-NI-PSMA-093 can utilize the PSMA targeting property as a "navigation system" to efficiently concentrate the entire molecule within prostate cancer cells, and once the cells are in an oxygen-deficient state, the molecule will irreversibly capture and remain in the oxygen-deficient cells, achieving "secondary enrichment". AAZTA-NI-PSMA-093 can be labeled with ⁶⁸Ga and ¹⁷⁷Lu, and has high accumulation and rapid clearance characteristics in mouse models. AAZTA-NI-PSMA-093 can be used for the study of prostate cancer .
|
-
- HY-177345
-
|
|
Sigma Receptor
Apoptosis
Caspase
|
Cancer
|
|
SV119 is a selective sigma-2 (σ₂) receptor ligand (Ki ≈ 5-10 nM). SV119 induces apoptosis in various human cancer cell lines by activating caspase-3 and promoting mitochondrial depolarization. SV119 can enhance the effects of chemotherapeutic agents such as Paclitaxel (HY-B0015), increasing their cytotoxicity against tumor cells. SV119 significantly inhibits tumor growth in mouse xenograft models, both alone and in combination. SV119 is useful in the research of cancers such as breast, prostate, and pancreatic cancer .
|
-
- HY-178941
-
|
|
Dihydroorotate Dehydrogenase
Apoptosis
Caspase
Reactive Oxygen Species (ROS)
|
Cancer
|
|
DHODH-IN-32 (Compound A1) is a DHODH inhibitor. DHODH-IN-32 shows significant cytotoxicity against NCI-60 cell lines, especially being sensitive to breast cancer, prostate cancer and leukemia cell lines. DHODH-IN-32 can induce cell apoptosis by activating the Caspase pathway. DHODH-IN-32 causes G0/G1 phase cell cycle arrest and inhibits cellular metabolism by ROS. DHODH-IN-32 exhibits significant anti-tumor properties in mouse breast cancer models. DHODH-IN-32 can be used for the study of breast cancer .
|
-
- HY-W877997
-
|
|
E3 Ligase Ligand-Linker Conjugates
Drug Derivative
|
Cancer
|
|
Pomalidomide 5'-pip-acid is an E3 ligase ligand-linker conjugate derived from the molecular glue Pomalidomide (HY-10984), which can be used to synthesize the dual-target PROTAC degrader PROTAC CBP/p300/BRD4 Degrader-1 (HY-181758) targeting CBP/p300 and BRD4. Pomalidomide 5'-pip-acid shows anti-proliferative activity against cancer cells with an IC50 of 2.73 nM. Pomalidomide 5'-pip-acid induces anti-proliferative effects in cancer cells. Pomalidomide 5'-pip-acid is applicable to research related to prostate cancer and colorectal cancer .
|
-
- HY-113701
-
|
|
Androgen Receptor
|
Cancer
|
|
CH5137291 is an orally active pure antagonist of the androgen receptor (AR), without generating agonist metabolites. CCH5137291 directly blocks the transfer of AR from the cytoplasm to the nucleus. H5137291 can completely inhibit tumor growth in cells and mouse models of castration-resistant prostate cancer models. CH5137291 can be used for the study of castration-resistant prostate cancer (CRPC) .
|
-
- HY-169078
-
|
|
Histone Methyltransferase
|
Cancer
|
|
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 .
|
-
- HY-106431
-
|
Olpadronate; OLP
|
Farnesyl Transferase
|
Metabolic Disease
Cancer
|
|
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 .
|
-
- HY-178148
-
|
|
Androgen Receptor
|
Endocrinology
Cancer
|
|
AR antagonist 17 is a selective, orally active, low brain-penetrant Androgen Receptor (AR) antagonist (IC50 = 0.010 μM), effectively blocking AR dimerization and nuclear translocation, and demonstrating potent efficacy in several castration-resistant prostate cancer (CRPC) cells. AR antagonist 17 showed superior efficacy against variant drug-resistant AR mutants. AR antagonist 17 can inhibit tumor growth in an LNCaP xenograft model without apparent toxicity. AR antagonist 17 can be used for the study of castration-resistant prostate cancer (CRPC) .
|
-
- HY-168300
-
|
|
Reactive Oxygen Species (ROS)
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
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 .
|
-
- HY-106431R
-
|
Olpadronate (Standard); OLP (Standard)
|
Reference Standards
Others
|
Metabolic Disease
Cancer
|
|
Olpadronic acid (Standard) is the analytical standard of Olpadronic acid. This product is intended for research and analytical applications. 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 .
|
-
- 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).
|
-
- HY-106154
-
|
|
Peptide-Drug Conjugates (PDCs)
Aminopeptidase
|
Cancer
|
|
DTS-201 (CPI-0004) 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 .
|
-
- HY-155543
-
|
|
Androgen Receptor
|
Cancer
|
|
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 .
|
-
- HY-155458
-
|
|
PARP
|
Inflammation/Immunology
Cancer
|
|
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 .
|
-
- HY-173474
-
|
|
Estrogen Receptor/ERR
Androgen Receptor
|
Cancer
|
|
ERβ agonist-1 (Compound 8) is a dual-active selective ERβ agonist (EC50: 46.8 nM) and AR antagonist (IC50: 1555 nM). ERβ agonist-1 activates ERβ signaling by binding to ERβ and inhibits AR activity. ERβ agonist-1 retains selective ERβ agonist activity in mouse models and can be used to study prostate cancer .
|
-
- HY-142743
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
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 .
|
-
- HY-163062
-
|
|
Microtubule/Tubulin
Apoptosis
Complement System
|
Cancer
|
|
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 .
|
-
- HY-122611R
-
|
|
Reference Standards
Androgen Receptor
Apoptosis
|
Cancer
|
|
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
|
-
- HY-N7043R
-
|
|
Reference Standards
Apoptosis
PPAR
NF-κB
p38 MAPK
ERK
Androgen Receptor
|
Inflammation/Immunology
Cancer
|
|
Isosilybin A (Standard) is the analytical standard of Isosilybin A (HY-N7043). Isosilybin A is a PPARγ agonist that can be isolated from silymarin. Isosilybin A activates extrinsic and intrinsic pathways of apoptosis through targeting of the Akt-NF-kB-AR axis. Isosilybin A can relieve the inflammatory response in the rosacea model via inhibiting Erk and p38 signaling pathways and M1 macrophage polarization, with its targets related to RELA and VEGFA. Isosilybin A has anti-prostate cancer (PCA) activity [1][2][3].
|
-
- HY-N1486R
-
|
3-Ketoursolic acid (Standard)
|
Reference Standards
Apoptosis
Endogenous Metabolite
NF-κB
|
Inflammation/Immunology
Cancer
|
|
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
|
-
- HY-146494
-
|
|
Androgen Receptor
|
Cancer
|
|
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 .
|
-
- HY-169349
-
|
|
Androgen Receptor
|
Cancer
|
|
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 .
|
-
- HY-163612
-
|
|
ROR
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-163611
-
|
|
ROR
|
Cancer
|
|
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 .
|
-
- HY-181970
-
|
|
Orphan Nuclear Receptor
Androgen Receptor
c-Myc
|
Cancer
|
|
XY25026 is an orally active LRH-1 inhibitor with an IC50 of 0.28 μM. XY25026 inhibits the proliferation of androgen receptor (AR)-positive prostate cancer cells, suppresses the expression of AR target genes KLK2 and KLK3, and inhibits tumor growth in xenograft models. XY25026 is applicable to the research of castration-resistant prostate cancer .
|
-
- HY-182288
-
|
|
STAT
Apoptosis
|
Cancer
|
|
YN11 is a STAT3 inhibitor (Kd=11.9 μM). YN11 directly binds to the SH2 domain of STAT3, inhibits the phosphorylation of STAT3, and reduces the expression of downstream target proteins. YN11 induces cell cycle arrest, promotes apoptosis, and inhibits cell invasion and migration in prostate cancer cells. YN11 suppresses tumor growth in a prostate cancer xenograft mouse model. YN11 does not cause significant body weight loss or obvious histopathological changes in major organs in xenograft mice. YN11 is applicable to relevant research on prostate cancer .
|
-
- HY-P992209
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
Anti-CD318/CDCP1 Antibody (25A11) is an anti-CDCP1 antibody. Anti-CD318/CDCP1 Antibody (25A11) drives the internalization of antibody-CDCP1 complexes, inhibits cancer cell migration and invasion, and blocks downstream migration/invasion signaling pathways. When conjugated with saponin, Anti-CD318/CDCP1 Antibody (25A11) mediates the killing of prostate cancer cells. When conjugated with saponin, this antibody acts as an immunotoxin to inhibit the growth and metastasis of primary prostate tumors in mouse xenograft models. Anti-CD318/CDCP1 Antibody (25A11) is applicable to prostate cancer-related research .
|
-
- HY-181758
-
|
|
PROTACs
Epigenetic Reader Domain
Histone Acetyltransferase
c-Myc
Apoptosis
|
Cancer
|
|
PROTAC CBP/p300/BRD4 Degrader-1 is a dual-target PROTAC degrader with DC50 values of 8.8 pM (BRD4), 6.55 nM (CBP), and 1.05 nM (p300). PROTAC CBP/p300/BRD4 Degrader-1 induces CRBN- and proteasome-dependent degradation of BRD4 and CBP/p300, downregulates c-Myc and acetyl-H3K27, induces apoptosis. PROTAC CBP/p300/BRD4 Degrader-1 acts as an antiproliferative and antitumor agent, induces tumor growth inhibition in xenograft models. PROTAC CBP/p300/BRD4 Degrader-1 can be used for the research of prostate cancer and colorectal cancer .
|
-
- HY-180804
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
CZL-077 is a potent, selective, and orally active p300/CBP bromodomain (BRD) inhibitor (p300 IC50 = 0.034 μM, CBP IC50 = 0.052 μM) exhibiting high selectivity over the BRDs of BET proteins (BRD2/3/4). CZL-077 inhibits cell growth with IC50 values of 0.024 μM and 5.6 μM in OPM-2 and 22RV1 cells, respectively. CZL-077 shows antitumor efficacy in OPM-2 and 22RV1 xenograft mouse models. CZL-077 can be used for multiple myeloma and prostate cancer research .
|
-
- HY-P11624
-
|
|
Apoptosis
|
Cancer
|
|
PP-60 is an apoptosis inducer. PP-60 inhibits the proliferation of cancer cells and induces cancer cell apoptosis. PP-60 exerts anti-tumor effects in nude mouse liver tumor models. PP-60 is applicable to research related to cancers such as liver cancer, lung cancer, and prostate cancer .
|
-
- HY-159739
-
|
|
Androgen Receptor
|
Cancer
|
|
M17-B15 is an androgen receptor dimerization inhibitor with an IC50 of 30 nM. M17-B15 effectively disrupts AR self-association, thereby suppressing AR signaling. M17-B15 exhibits extraordinary anti- prostate cancer (PCa) efficacy in vitro and in mouse xenograft tumor models.M17-B15 can be used for the study of prostate cancer .
|
-
- HY-19337S1
-
|
BAY 1896953-d6; ORM-15341-d6
|
Isotope-Labeled Compounds
Androgen Receptor
|
Cancer
|
|
Ketodarolutamide-d6 (BAY 1896953-d6) is the deuterium labeled Ketodarolutamide (HY-19337). Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a Ki value of 8 nM for rat wild-type AR and an IC50 value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .
|
-
- HY-19337S
-
|
BAY 1896953-d3; ORM-15341-d3
|
Isotope-Labeled Compounds
Androgen Receptor
|
Cancer
|
|
Ketodarolutamide-d3 (BAY 1896953-d3) is the deuterium labeled Ketodarolutamide (HY-19337). Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a Ki value of 8 nM for rat wild-type AR and an IC50 value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .
|
-
- HY-180995
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
VARS1-IN-1 is a valyl-tRNA synthetase (VARS1) inhibitor with a Kd of 0.213 μM. VARS1-IN-1 suppresses VARS1’s tRNA aminoacylation activity, reduces charged levels of valine tRNAs and redues total protein synthesis rate. VARS1-IN-1 suppresses aggressive tumor growth and cell proliferation in PC3 prostate cancer xenograft models. VARS1-IN-1 can be used for the research of prostate cancer .
|
-
- HY-184124
-
|
|
Androgen Receptor
Histone Acetyltransferase
|
Cancer
|
|
JYZ3032 is an orally active super inhibitor of androgen receptor (AR) and p300/CBP. JYZ3032 redirects the catalytic activity of p300 and locks the complex in a transcriptionally inactive state, thereby inhibiting AR-driven transcription and proliferation. JYZ3032 induces deep and durable tumor regression in castration-resistant and patient-derived xenograft models, and exhibits good tolerability. JYZ3032 can be used in research related to metastatic castration-resistant prostate cancer and prostate cancer .
|
-
- HY-P991748
-
|
|
EGFR
|
Cancer
|
|
Anti-Human/Mouse Amphiregulin Antibody (AR37) reacts with human and mouse amphiregulin (AREG) that can block AREG-induced activation of EGFR. Anti-Human/Mouse Amphiregulin Antibody (AR37) can prolong the survival and inhibit the growth of ovarian, breast, and prostate cancer models expressing AREG .
|
-
- HY-183632
-
|
|
Microtubule/Tubulin
Apoptosis
|
Neurological Disease
Cancer
|
|
QW-5-70 is a potent colchicine‑site tubulin inhibitor that blocks tubulin polymerization. QW-5-70 induces mitotic and G2/M cell cycle arrest, triggers mitochondrial apoptosis, and suppresses cancer cell colony formation and migration. QW-5-70 overcomes P‑glycoprotein‑mediated multidrug resistance and inhibits drug‑resistant tumor growth. QW-5-70 demonstrates strong in vitro and in vivo antitumor efficacy in neuroblastoma and prostate cancer models. QW-5-70 can be used for the research of high-risk neuroblastoma and castration-resistant prostate cancer .
|
-
- HY-16232R
-
|
D 19575 (Standard); Glucosylifosfamide mustard (Standard)
|
Reference Standards
Apoptosis
Bcl-2 Family
Caspase
|
Cancer
|
|
Glufosfamide (Standard) is the analytical standard of Glufosfamide. This product is intended for research and analytical applications. Glufosfamide is a glucose-conjugated alkylating cytotoxic agent and a derivative of Ifosfamide (HY-17419). Glufosfamide induces apoptosis frequency and increase the expression of caspase-9 and caspase-3 in cancer cells. Glufosfamide shows great anti-tumor activity in MiaPaCa-2-RFP mouse model. Glufosfamide can be used for the study of hepatocellular carcinoma, prostate cancer and pancreatic carcinoma .
|
-
- HY-183630
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
AZD4956 is a potent and selective DNA polymerase theta (POLQ) inhibitor. AZD4956 exhibits an IC50 value of less than 3 μmol/L against POLQ and 3.4 μmol/L against MMEJ. AZD4956 suppresses the MMEJ pathway and enhances the activity of DNA-damaging agents in HRR-deficient cellular contexts. AZD4956 shows antitumor activity in BRCA1/2-mutated triple-negative breast cancer and prostate cancer models. AZD4956 can be used for the study of homologous recombination-deficient tumors .
|
-
- HY-183710
-
|
|
CDK
Androgen Receptor
c-Myc
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
CDK9-IN-50 is a selective and orally active CDK9 inhibitor with an IC50 of 2.2 nM. CDK9-IN-50 targets a distinct CDK9-specific subpocket to disrupt RNA polymerase II Ser2 phosphorylation and downregulate short-lived oncoproteins, including AR-V7 and Myc. CDK9-IN-50 exhibits antiproliferative activity against cancer cells, induces apoptosis and induces tumor growth inhibition in CRPC orthotopic mice models. CDK9-IN-50 can be used for the research of cancer, such as prostate cancer .
|
-
- HY-D3353
-
|
|
PSMA
|
Cancer
|
|
PSMA-SulfoCy7 is a high-affinity imaging agent targeting PSMA/GCPII (with a Ki of 18.1 nM for human PSMA). PSMA-SulfoCy7 regulates PSMA-dependent NAAG hydrolysis. PSMA-SulfoCy7 exhibits excellent in vivo imaging capability, enabling clear visualization of PSMA-expressing tumors in xenograft models, with no obvious toxicity even at a dose of 87.9 mg/kg. PSMA-SulfoCy7 is widely used in prostate cancer-related studies .
|
-
- HY-181759
-
|
|
Ligands for Target Protein for PROTAC
Epigenetic Reader Domain
Histone Acetyltransferase
|
Cancer
|
|
CBP/p300/BRD4 ligand-1 is a small-molecule inhibitor targeting CBP, p300, and BRD4. CBP/p300/BRD4 ligand-1 competitively binds to the functional domains of target proteins without disrupting key interactions. CBP/p300/BRD4 ligand-1 can be used for the construction of dual-target PROTAC degraders (HY-181758) in studies related to prostate cancer and other cancers .
|
-
- HY-123303
-
|
NZ-28
|
HSP
|
Cancer
|
|
NSC-134754 is a dehydroemetine derivative and heat shock protein induction inhibitor. NSC-134754 acts at the post-transcriptional level, targets Hsp72 and Hsp27, and does not alter general protein synthesis, HSF-1 transcriptional activity, or Hsp mRNA levels. NSC-134754 shows no significant toxicity in preclinical models and sensitizes cancer cells to proteasome and Hsp90 inhibitors. NSC-134754 can be used for the research of multiple myeloma, prostate carcinoma, colon carcinoma .
|
-
- HY-181687
-
|
|
HSP
CDK
|
Cancer
|
|
Hsp90-IN-46 is a Hsp90 inhibitor. Hsp90-IN-46 exhibits broad-spectrum antiproliferative activity against tumor cell lines. Hsp90-IN-46 inhibits breast cancer cell proliferation by reducing colony formation and downregulating the proliferation marker Ki-67. Hsp90-IN-46 inhibits Hsp90 and its ATPase activity, downregulates the downstream substrate oncoproteins HER2 and CDK4, and moderately induces the heat shock response. Hsp90-IN-46 shows significant antitumor activity in a mouse model of triple-negative breast cancer tumor xenografts. Hsp90-IN-46 can be used for research on various cancers including triple-negative breast cancer, leukemia, non-small cell lung cancer, colon cancer, ovarian cancer, renal cancer, prostate cancer .
|
-
- HY-133005
-
|
4-Desacetylvinblastine; Desacetylvincaleukoblastine
|
Drug Metabolite
|
Cancer
|
|
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 .
|
-
- HY-P992449
-
|
PRLR ADC antibody
|
ADC Antibody
|
Cancer
|
|
REGN2878 (PRLR ADC antibody) is a monoclonal antibody targeting the prolactin receptor (PRLR) and can block prolactin‑mediated activation of PRLR. REGN2878 exhibits an equilibrium dissociation constant (KD) of 1.05 nM and an IC50 of 0.344 nM for human PRLR. REGN2878 can be rapidly internalized and degraded in lysosomes by PRLR‑positive tumor cells, showing antigen‑specific binding and targeted enrichment properties. REGN2878 derivatives can be used as an immunoPET agent for antigen‑specific imaging of PRLR‑related tumors, and can also serve as a component of ADCs to exert anti‑tumor activity in breast cancer xenograft models. REGN2878 can be used in the research of breast cancer and prostate cancer. Isotype Comparison HY-P99001 .
|
-
- HY-178343
-
|
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
Aurora A-IN-5 is a potent and highly selective Aurora A inhibitor (IC50 = 0.02 μM), showing 362-fold selectivity for over Aurora B. Aurora A-IN-5 shows its selectivity through unique C−H/π interactions, enhanced hydrophobic contacts, an open binding pocket, and tighter protein packing. Aurora A-IN-5 suppresses Aurora A autophosphorylation, thereby inhibiting cancer cell proliferation by inducing G2/M phase arrest, triggering apoptosis, and suppressing colony formation. Aurora A-IN-5 inhibits tumor growth in MDA-MB-231 xenograft mouse models. Aurora A-IN-5 can be used for breast, cervical, prostate, and lymphoma cancer research .
|
-
- HY-176128
-
|
|
PROTACs
Androgen Receptor
Apoptosis
PARP
Caspase
|
Cancer
|
|
BWA-6047 is an oral active PROTAC degrader targeting AR/AR-V7 and GSPT1 with DC50 values of 3.7, 3.0 and 1.2 nM in 22Rv1 cells. BWA-6047 suppresses the expression of AR downstream target genes and and transcriptional activity. BWA-6047 inhibits cancer cells proliferation, causes G1 phase cell cycle arrest and induces apoptosis. BWA-6047 increases cleaved-PARP-1 and cleaved-caspase-3 levels. BWA-6047 reduces growth of LNCaP xenograft tumors in mice models without obvious toxicity. BWA-6047 can be used for the research of prostate cancer .
|
-
- HY-181971
-
|
|
Orphan Nuclear Receptor
Androgen Receptor
c-Myc
|
Cancer
|
|
XY25028 is an orally active LRH-1 inhibitor with an IC50 of 0.30 μM. XY25028 inhibits the proliferation of androgen receptor (AR)-positive prostate cancer cells and suppresses the expression of AR target genes KLK2 and KLK3. XY25028 can be used in the research of castration-resistant prostate cancer .
|
-
- HY-P991243
-
|
|
EGFR
Akt
|
Cancer
|
|
MP-RM-1 is an antibody-based, non-competitive ErbB-3 inhibitor with a Kd value of 32.7 nM. MP-RM-1 inhibits both ligand-dependent and ligand-independent ErbB-3 activation, blocks ErbB-2/ErbB-3 heterodimerization, induces ErbB-3 internalization and degradation, and suppresses the phosphorylation of downstream Akt. MP-RM-1 exerts its antagonistic effect through a non-competitive mechanism. MP-RM-1 inhibits tumor growth in melanoma and prostate cancer xenograft models in nude mice and reduces the proliferative activity of tumor cells .
|
-
- HY-160777A
-
|
Galeterone 3β-imidazole dihydrochloride
|
Molecular Glues
Androgen Receptor
MNK
Apoptosis
|
Cancer
|
|
VNPP433-3β (Galeterone 3β-imidazole) dihydrochloride is an orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. VNPP433-3β dihydrochloride induces cell apoptosis. VNPP433-3β dihydrochloride inhibits tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β dihydrochloride can be used for the study of castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) .
|
-
- HY-160777
-
|
Galeterone 3β-imidazole
|
Molecular Glues
Androgen Receptor
MNK
Apoptosis
|
Cancer
|
|
VNPP433-3β (Galeterone 3β-imidazole) is an orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. VNPP433-3β induces cell apoptosis. VNPP433-3β inhibits tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β can be used for the study of castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) .
|
-
- HY-160777B
-
|
Galeterone 3β-imidazole hydrochloride
|
Molecular Glues
Androgen Receptor
MNK
Apoptosis
|
Cancer
|
|
VNPP433-3β (Galeterone 3β-imidazole) hydrochloride is an orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. VNPP433-3β hydrochloride induces cell apoptosis. VNPP433-3β hydrochloride inhibits tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β hydrochloride can be used for the study of castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) .
|
-
- HY-109747
-
|
|
MMP
|
Cancer
|
|
RO-28-2653 is an orally active matrix metalloproteinase (MMP) inhibitor. RO-28-2653 exhibits highly selective inhibitory effects on MMP2, MMP9 and membrane-type 1-MMP, and may reduce side effects (such as musculoskeletal pain) compared to broad-spectrum MMP inhibitors. RO-28-2653 shows significant tumor growth inhibition in a rat prostate model. RO-28-2653 can be used in studies of hormone-sensitive tumors .
|
-
- HY-173145
-
|
|
Aminopeptidase
|
Cancer
|
|
CD13-IN-1 (Compound 5f) is a CD13 inhibitor with an IC50 of 1.71 μM. CD13-IN-1 can inhibit the proliferation of multiple tumor cells and has anti-tumor activity .
|
-
- HY-W017540
-
|
|
ATP Synthase
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Cancer
|
|
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 .
|
-
- HY-W017540R
-
|
|
Reference Standards
ATP Synthase
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Cancer
|
|
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 .
|
-
- HY-175455
-
|
|
PROTACs
Androgen Receptor
Akt
|
Cancer
|
|
LYA914 is an orally active AR/AR-V7 PROTAC degrader. LYA914 targets the proteolytic degradation of the conserved DNA binding domain (DBD) of the androgen receptor (AR). LYA914 exhibits potent antiproliferative effects in Enzalutamide (HY-70002)-insensitive/resistant cells. LYA914 inhibits tumor growth in VCaP/LNCaP tumor mouse models. LYA914 can be used to study castration-resistant prostate cancer (CRPC). (Pink: AR-DBD ligand-1: HY-175456, Blue: Thalidomide: HY-14658, Pink + Black: AR-DBD ligand-Linker Conjugate 1: HY-175457, Black: Boc-piperidine-oxopiperidin: HY-175458) .
|
-
- HY-P992094
-
|
|
PSMA
|
Cancer
|
|
Capromab is an anti-human PSMA-targeting monoclonal antibody. Capromab binds specifically to the intracellular domain of PSMA, does not undergo internalization after binding, and targets necrotic cells with disrupted membranes. Capromab can be used for the research of prostate cancer .
|
-
- HY-148152A
-
|
|
PSMA
|
Cancer
|
|
PSMA I&S TFA is a PSMA-targeted imaging agent. PSMA I&S TFA undergoes PSMA-mediated internalization into PSMA-expressing cells, with uptake into PSMA-positive tissues competitively inhibited by a potent PSMA inhibitor. PSMA I&S TFA can be used for the research of prostate cancer .
|
-
- HY-182567
-
|
|
NAMPT
|
Cancer
|
|
Nampt-IN-19 is an orally active and non-substrate nicotinamide phosphoribosyltransferase (NAMPT) inhibitor with a human Ki of 5.6 nM. Nampt-IN-19 blocks NAD + biosynthesis from Nicotinamide (HY-B0150). Nampt-IN-19 acts as an antiproliferative agent in cancer cells. Nampt-IN-19 has preclinical pharmacokinetic properties supporting oral antitumor activity in mouse xenograft models. Nampt-IN-19 can be used for the research of colorectal cancer .
|
-
- HY-W017540S
-
|
|
Isotope-Labeled Compounds
ATP Synthase
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Cancer
|
|
Cyclocreatine- 13C3 is the 13C-labeled Cyclocreatine (HY-W017540). 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 .
|
-
- HY-P991577
-
|
DS-8895A
|
Ephrin Receptor
|
Cancer
|
|
DS-8895(DS-8895A) is an anti-EphA2 monoclonal antibody with specific binding to EphA2 receptors and EphA2-expressing cells. DS-8895, when conjugated with 89Zr, 111In, or 125I, supports molecular imaging of EphA2 expression in xenograft models. DS-8895 allows noninvasive measurement of EphA2 expresssion in tumors in vivo. .
|
-
- 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 .
|
-
- HY-179476
-
|
|
Androgen Receptor
Endogenous Metabolite
|
Inflammation/Immunology
Cancer
|
|
3-Oxochol-5-en-24-oic acid is a rare bile acid produced by the intestinal microbiota. 3-Oxochol-5-en-24-oic acid is a potent antagonist of the human androgen receptor (hAR), with an IC50 of 119.4 nM. 3-Oxochol-5-en-24-oic acid has no significant agonistic or antagonistic effects on estrogen receptors (ER) or glucocorticoid receptors (GR). 3-Oxochol-5-en-24-oic acid effectively inhibits the growth of prostate cancer cells. In animal models, it enhances the efficacy of anti-PD-1 therapy by regulating the differentiation of CD8 + T cells. 3-Oxochol-5-en-24-oic acid can be used for research on regulating host immunity and anti-tumor studies .
|
-
- HY-183912
-
|
|
Topoisomerase
ADC Payload
|
Cancer
|
|
PY-4Car2 is a Camptothecin (HY-16560) derivative and a topoisomerase I inhibitor. PY-4Car2 functions as a warhead conjugated via a cleavable linker to the bispecific ADC TJ101. PY-4Car2 can be used as an ADC payload for the research of cancers .
|
-
- HY-185269
-
|
|
Microtubule/Tubulin
Drug Derivative
|
Cancer
|
|
2'-Deoxy-PTX is a Paclitaxel (HY-B0015) derivative and microtubule assembly inducer. 2'-Deoxy-PTX binds to GMPcPP-stabilized microtubules, with a Kaapp of 0.50 × 10 6 M -1. 2′-Deoxy-PTX induces Tubulin to assemble into normal microtubules. 2'-Deoxy-PTX can be used for the research of prostate cancer .
|
-
- HY-183273
-
|
|
Epigenetic Reader Domain
Akt
CDK
Autophagy
Apoptosis
|
Cancer
|
|
BRD4/AKT-IN-1 is a BRD4/AKT inhibitor with BRD4 IC50 66.12 nM and AKT1 IC50 143.81 nM. BRD4/AKT-IN-1 blocks BRD4-mediated c-Myc transcriptional regulation, modulates AKT1 signaling, decouples AKT phosphorylation from pro-survival effectors. BRD4/AKT-IN-1 induces G0/G1 cell cycle arrest via downregulated phosphorylated RB, cyclin E1, CDK2. BRD4/AKT-IN-1 elevates LC3B levels to promote autophagy. BRD4/AKT-IN-1 promotes apoptosis in cancer cells. BRD4/AKT-IN-1 can be used for the research of metastatic castration-resistant prostate cancer .
|
-
- HY-W224634
-
|
|
HSP
|
Cancer
|
|
HSF1-IN-2 (Compound 0048) is a HSF1 inhibitor. HSF1-IN-2 is applicable to cancer research .
|
-
- HY-181669
-
|
|
Histone Acetyltransferase
c-Myc
|
Cancer
|
|
P300-IN-6 is an orally active histone acetyltransferase p300 HAT domain inhibitor with human IC50 values of 7 nM. P300-IN-6 suppresses c-Myc expression, decreases H3K18ac and H3K27ac levels, and inhibits cancer cell proliferation.P300-IN-6 suppresses tumor growth in xenograft mouse models.P300-IN-6 can be used for the research of multiple myeloma .
|
-
- HY-N17406
-
-
- HY-P3371
-
|
DS-7300a; MABX-9001a; I-DXd
|
Antibody-Drug Conjugates (ADCs)
Topoisomerase
Apoptosis
|
Cancer
|
|
Ifinatamab deruxtecan (DS-7300a) is a B7-H3-targeting Antibody-drug conjugate (ADC), which is composed of a humanized anti-B7-H3 monoclonal antibody, an enzymatically cleavable peptide-based linker, and Exatecan derivative (DXd) (HY-13631D). Ifinatamab deruxtecan is a DNA Topoisomerase I inhibitor. Ifinatamab deruxtecan induces Apoptosis. DS-7300a exerts potent antitumor activities against B7-H3-expressing tumors. against rhabdomyosarcoma, endometrial adenocarcinoma and lung adenocarcinoma. Ifinatamab deruxtecan does not exert direct immunomodulatory effects
|
-
- HY-155887
-
|
DSPE-PEG-NH2, MW 3400 ammonium
|
Liposome
|
Cancer
|
|
DSPE-PEG-Amine (DSPE-PEG-NH2), MW 3400 ammonium is an amino-functionalized PEGylated phospholipid. It serves not only as a key component for preparing σ receptor-targeted liposomes (such as anisamide-modified lipids) but also as a starting material for synthesizing click chemistry- and tumor-targeted lipids including DSPE-PEG-DBCO (HY-155788) and DSPE-PEG2000-TCO (HY-170704). DSPE-PEG-Amine, MW 3400 ammonium effectively modulates the ζ potential of nanoparticles, enables complexation with nucleic acids or proteins to protect DNA from nuclease degradation, and supports ligand conjugation on the nanoparticle surface. It is used in studies related to DU-145 tumors, breast cancer, and other relevant research .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-P3371
-
|
DS-7300a; MABX-9001a; I-DXd
|
Fluorescent Dyes
|
|
Ifinatamab deruxtecan (DS-7300a) is a B7-H3-targeting Antibody-drug conjugate (ADC), which is composed of a humanized anti-B7-H3 monoclonal antibody, an enzymatically cleavable peptide-based linker, and Exatecan derivative (DXd) (HY-13631D). Ifinatamab deruxtecan is a DNA Topoisomerase I inhibitor. Ifinatamab deruxtecan induces Apoptosis. DS-7300a exerts potent antitumor activities against B7-H3-expressing tumors. against rhabdomyosarcoma, endometrial adenocarcinoma and lung adenocarcinoma. Ifinatamab deruxtecan does not exert direct immunomodulatory effects
|
-
- HY-D3353
-
|
|
Fluorescent Dyes
|
|
PSMA-SulfoCy7 is a high-affinity imaging agent targeting PSMA/GCPII (with a Ki of 18.1 nM for human PSMA). PSMA-SulfoCy7 regulates PSMA-dependent NAAG hydrolysis. PSMA-SulfoCy7 exhibits excellent in vivo imaging capability, enabling clear visualization of PSMA-expressing tumors in xenograft models, with no obvious toxicity even at a dose of 87.9 mg/kg. PSMA-SulfoCy7 is widely used in prostate cancer-related studies .
|
| Cat. No. |
Product Name |
Type |
-
- HY-155887
-
|
DSPE-PEG-NH2, MW 3400 ammonium
|
Biochemical Assay Reagents
|
|
DSPE-PEG-Amine (DSPE-PEG-NH2), MW 3400 ammonium is an amino-functionalized PEGylated phospholipid. It serves not only as a key component for preparing σ receptor-targeted liposomes (such as anisamide-modified lipids) but also as a starting material for synthesizing click chemistry- and tumor-targeted lipids including DSPE-PEG-DBCO (HY-155788) and DSPE-PEG2000-TCO (HY-170704). DSPE-PEG-Amine, MW 3400 ammonium effectively modulates the ζ potential of nanoparticles, enables complexation with nucleic acids or proteins to protect DNA from nuclease degradation, and supports ligand conjugation on the nanoparticle surface. It is used in studies related to DU-145 tumors, breast cancer, and other relevant research .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1416
-
|
|
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 .
|
-
- 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 .
|
-
- 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 .
|
-
- HY-P10992
-
|
|
PI3K
Akt
mTOR
Caspase
Apoptosis
Bcl-2 Family
|
Cancer
|
|
YVPGP is an oligopeptide exacted from Anthopleura anjunae. YVPGP has a significant antitumor activity by mediating PI3K/AKT/mTOR signaling pathway. YVPGP arrests DU-145 cells in the S phase and induces apoptosis via mitochondrial and death receptor pathways (caspase3, 7, 8, 9). YVPGP effectively inhibits tumor growth in DU-145 xenografts mice model, promising for prostate cancer research .
|
-
- HY-P11261
-
|
|
PSMA
|
Cancer
|
AAZTA-NI-PSMA-093 is a bispecific agent targeting prostate-specific membrane antigen (PSMA) with an IC50 value for PSMA of 87.48 nM. AAZTA-NI-PSMA-093 has a PSMA targeting module and an oxygen-sensitivity module (hypoxia-sensitive NI-moiety). AAZTA-NI-PSMA-093 can utilize the PSMA targeting property as a "navigation system" to efficiently concentrate the entire molecule within prostate cancer cells, and once the cells are in an oxygen-deficient state, the molecule will irreversibly capture and remain in the oxygen-deficient cells, achieving "secondary enrichment". AAZTA-NI-PSMA-093 can be labeled with ⁶⁸Ga and ¹⁷⁷Lu, and has high accumulation and rapid clearance characteristics in mouse models. AAZTA-NI-PSMA-093 can be used for the study of prostate cancer .
|
-
- 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).
|
-
- HY-P11624
-
|
|
Apoptosis
|
Cancer
|
|
PP-60 is an apoptosis inducer. PP-60 inhibits the proliferation of cancer cells and induces cancer cell apoptosis. PP-60 exerts anti-tumor effects in nude mouse liver tumor models. PP-60 is applicable to research related to cancers such as liver cancer, lung cancer, and prostate cancer .
|
-
- HY-P11658
-
|
Peptoid 1
|
Peptides
|
Cancer
|
|
Anticancer peptoid 1 (Peptoid 1) is a peptoid with antitumor activity. Anticancer peptoid 1 exerts cytotoxicity primarily via plasma membrane damage. Anticancer peptoid 1 exerts cytotoxicity against a broad range of cancer cell lines, including those with multidrug resistance. Anticancer peptoid 1 inhibits tumor growth in a human breast cancer xenotransplantation mouse model without noticeable acute adverse effects. Anticancer peptoid 1 can be used for the research of cancer, such as breast cancer, and prostate cancer .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P3371
-
|
DS-7300a; MABX-9001a; I-DXd
|
Antibody-Drug Conjugates (ADCs)
Topoisomerase
Apoptosis
|
Cancer
|
|
Ifinatamab deruxtecan (DS-7300a) is a B7-H3-targeting Antibody-drug conjugate (ADC), which is composed of a humanized anti-B7-H3 monoclonal antibody, an enzymatically cleavable peptide-based linker, and Exatecan derivative (DXd) (HY-13631D). Ifinatamab deruxtecan is a DNA Topoisomerase I inhibitor. Ifinatamab deruxtecan induces Apoptosis. DS-7300a exerts potent antitumor activities against B7-H3-expressing tumors. against rhabdomyosarcoma, endometrial adenocarcinoma and lung adenocarcinoma. Ifinatamab deruxtecan does not exert direct immunomodulatory effects
|
-
(5)
-
- HY-P990673
-
|
DSTP-3086S Antibody; RG-7450 Antibody
|
ADC Antibody
Transmembrane Glycoprotein
Mitosis
|
Cancer
|
|
Vandortuzumab (DSTP-3086S Antibody; RG-7450 Antibody) is a humanized anti-STEAP1 IgG1 antibody and antimitotic agent that can be conjugated with MMAE (HY-15162) to form the antibody-drug conjugate (ADC) Vandortuzumab vedotin. Vandortuzumab vedotin specifically binds to STEAP1 and drives internalization of the complex, releasing the MMAE (HY-15162) payload intracellularly. After binding to tubulin, MMAE inhibits cell division and induces cell death. Vandortuzumab exhibits antitumor activity in preclinical xenograft models of prostate cancer and can be used for research related to metastatic castration-resistant prostate cancer (mCRPC) .
|
-
(5)
-
- HY-P9992
-
|
BAY-2315497; PSMA-TTC
|
PSMA
Apoptosis
|
Cancer
|
|
Peligifatamab is a PSMA-targeted α-radioimmunoconjugate with an EC50 of 1.2 nM against human targets. Peligifatamab induces DNA damage, DNA double-strand breaks, cell cycle arrest and apoptosis (Apoptosis) in PSMA-positive prostate cancer cells. Peligifatamab reduces cell viability in a manner dependent on cellular PSMA expression levels. Peligifatamab inhibits tumor growth and tumor-induced abnormal bone growth in prostate cancer bone metastasis models. Peligifatamab exhibits antitumor efficacy in subcutaneous prostate cancer models and xenograft models. Peligifatamab can be used for the research of metastatic castration-resistant prostate cancer .
|
-
(5)
-
- HY-P991577
-
|
DS-8895A
|
Ephrin Receptor
|
Cancer
|
|
DS-8895(DS-8895A) is an anti-EphA2 monoclonal antibody with specific binding to EphA2 receptors and EphA2-expressing cells. DS-8895, when conjugated with 89Zr, 111In, or 125I, supports molecular imaging of EphA2 expression in xenograft models. DS-8895 allows noninvasive measurement of EphA2 expresssion in tumors in vivo. .
|
-
(5)
-
- HY-P99881
-
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ABBV 176
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Antibody-Drug Conjugates (ADCs)
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Cancer
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Rolinsatamab talirine (ABBV 176) is a prolactin receptor (PRLR)-targeting antibody-drug conjugate (ADC), compoused of Rolinsatamab (HY-P99238) and SGD-1882 (HY-101127). Rolinsatamab talirine binds to PRLR to deliver a cytotoxin to tumor cells. Rolinsatamab talirine induces DNA damage, and exhibits cytotoxicity against multiple breast tumor models, including triple negative and low PRLR-expressing models. Rolinsatamab talirine demonstrates enhanced anti-tumor activity in several breast cancer models. Rolinsatamab talirine can be used for the research of breast cancer, hepatocellular carcinoma, ovarian cancer, endometrial cancer, prostate cancer, colorectal cancer, adrenocortical carcinoma, and solid tumors .
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(5)
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- HY-P991243
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EGFR
Akt
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Cancer
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MP-RM-1 is an antibody-based, non-competitive ErbB-3 inhibitor with a Kd value of 32.7 nM. MP-RM-1 inhibits both ligand-dependent and ligand-independent ErbB-3 activation, blocks ErbB-2/ErbB-3 heterodimerization, induces ErbB-3 internalization and degradation, and suppresses the phosphorylation of downstream Akt. MP-RM-1 exerts its antagonistic effect through a non-competitive mechanism. MP-RM-1 inhibits tumor growth in melanoma and prostate cancer xenograft models in nude mice and reduces the proliferative activity of tumor cells .
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(5)
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- HY-P992209
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Transmembrane Glycoprotein
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Cancer
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Anti-CD318/CDCP1 Antibody (25A11) is an anti-CDCP1 antibody. Anti-CD318/CDCP1 Antibody (25A11) drives the internalization of antibody-CDCP1 complexes, inhibits cancer cell migration and invasion, and blocks downstream migration/invasion signaling pathways. When conjugated with saponin, Anti-CD318/CDCP1 Antibody (25A11) mediates the killing of prostate cancer cells. When conjugated with saponin, this antibody acts as an immunotoxin to inhibit the growth and metastasis of primary prostate tumors in mouse xenograft models. Anti-CD318/CDCP1 Antibody (25A11) is applicable to prostate cancer-related research .
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(5)
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- HY-P991748
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EGFR
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Cancer
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Anti-Human/Mouse Amphiregulin Antibody (AR37) reacts with human and mouse amphiregulin (AREG) that can block AREG-induced activation of EGFR. Anti-Human/Mouse Amphiregulin Antibody (AR37) can prolong the survival and inhibit the growth of ovarian, breast, and prostate cancer models expressing AREG .
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(5)
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- HY-P992449
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PRLR ADC antibody
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ADC Antibody
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Cancer
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REGN2878 (PRLR ADC antibody) is a monoclonal antibody targeting the prolactin receptor (PRLR) and can block prolactin‑mediated activation of PRLR. REGN2878 exhibits an equilibrium dissociation constant (KD) of 1.05 nM and an IC50 of 0.344 nM for human PRLR. REGN2878 can be rapidly internalized and degraded in lysosomes by PRLR‑positive tumor cells, showing antigen‑specific binding and targeted enrichment properties. REGN2878 derivatives can be used as an immunoPET agent for antigen‑specific imaging of PRLR‑related tumors, and can also serve as a component of ADCs to exert anti‑tumor activity in breast cancer xenograft models. REGN2878 can be used in the research of breast cancer and prostate cancer. Isotype Comparison HY-P99001 .
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(5)
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- HY-P992094
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PSMA
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Cancer
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Capromab is an anti-human PSMA-targeting monoclonal antibody. Capromab binds specifically to the intracellular domain of PSMA, does not undergo internalization after binding, and targets necrotic cells with disrupted membranes. Capromab can be used for the research of prostate cancer .
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(5)
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Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-A0287S
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Clomifene (Clomifene; (Z/E)-Enclomiphene; (Z/E)-Enclomifene)-d5 hydrochloride is a deuterium labeled Clomifene hydrochloride (HY-A0287A). Clomiphene hydrochloride is an orally active ovulation-inducing agent. Clomiphene hydrochloride binds to hypothalamic estrogen receptors to elevate FSH levels, and exhibits antiestrogenic or estrogenic properties. Clomiphene hydrochloride can induce erturbations during meiotic maturation and cytogenetic abnormalities in mouse oocytes. Clomiphene hydrochloride ameliorates memory impairment in PCOS models. Clomiphene hydrochloride mobilizes cytosolic calcium and reduces viability in prostate cancer cells. Clomiphene hydrochloride can be used for the research of polycystic ovary syndrome (PCOS) and prostate cancer .
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- HY-W017540S
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Cyclocreatine- 13C3 is the 13C-labeled Cyclocreatine (HY-W017540). 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-19337S1
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Ketodarolutamide-d6 (BAY 1896953-d6) is the deuterium labeled Ketodarolutamide (HY-19337). Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a Ki value of 8 nM for rat wild-type AR and an IC50 value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .
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- HY-19337S
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Ketodarolutamide-d3 (BAY 1896953-d3) is the deuterium labeled Ketodarolutamide (HY-19337). Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a Ki value of 8 nM for rat wild-type AR and an IC50 value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .
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| Cat. No. |
Product Name |
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Classification |
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- HY-147081
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AS 1411
2 Publications Verification
AGRO-100
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Aptamers
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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-147081A
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AGRO-100 sodium
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Aptamers
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AS 1411 (AGRO-100) sodium is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 sodium 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 sodium reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. S 1411 sodium works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. S 1411 sodium-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-155887
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DSPE-PEG-NH2, MW 3400 ammonium
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Pegylated Lipids
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DSPE-PEG-Amine (DSPE-PEG-NH2), MW 3400 ammonium is an amino-functionalized PEGylated phospholipid. It serves not only as a key component for preparing σ receptor-targeted liposomes (such as anisamide-modified lipids) but also as a starting material for synthesizing click chemistry- and tumor-targeted lipids including DSPE-PEG-DBCO (HY-155788) and DSPE-PEG2000-TCO (HY-170704). DSPE-PEG-Amine, MW 3400 ammonium effectively modulates the ζ potential of nanoparticles, enables complexation with nucleic acids or proteins to protect DNA from nuclease degradation, and supports ligand conjugation on the nanoparticle surface. It is used in studies related to DU-145 tumors, breast cancer, and other relevant research .
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