Search Result
Results for "
22Rv1
" in MedChemExpress (MCE) Product Catalog:
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-B0568
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Deferiprone
Maximum Cited Publications
47 Publications Verification
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Ferroptosis
HCV
Apoptosis
COX
Histone Demethylase
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Cardiovascular Disease
Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
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Deferiprone is a potent, orally active, brain-penetrant, cell-penetrant, skin-permeable, free iron chelating agent. Deferiprone inhibits the proliferation and migration, and stimulates apoptosis in tumor cell. Deferiprone can inhibit KDM. Deferiprone has antianemic, neuroprotective, anti-inflammatory, antioxidant, and antidotal activity. Deferiprone can be used in cancer, cardiovascular disease, infection, inflammation, and neurological disease study .
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- HY-158113
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Histone Acetyltransferase
PROTACs
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Cancer
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CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC50 of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC50s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker) .
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- HY-P99762
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MGD009
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CD3
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Cancer
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Obrindatamab is a humanized anti-B7-H3/CD3 bispecific antibody. Obrindatamab binds to B7-H3 and CD3, thereby mediating redirected cytotoxic T-lymphocyte (CTL) activity against B7-H3-expressing cancer cells. Obrindatamab can be used in research of cancer .
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- HY-153918
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Androgen Receptor
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Cancer
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(R)-SKBG-1 is a covalent inhibitor targeting the RNA binding protein NONO. (R)-SKBG-1 can reduce the expression of androgen receptor (AR) and its splice variants, inhibiting cancer cell proliferation. (R)-SKBG-1 inhibits androgen receptor expression with IC50 of 3.1 μM and 5.5 μM for AR-FL mRNA and AR-V7 mRNA, respectively. (R)-SKBG-1 interferes with the gene regulatory network of cancer cells and inhibits cancer cell growth by stabilizing the interaction between NONO and mRNA. (R)-SKBG-1 can be used in the study of cancers related to NONO dysfunction, such as prostate cancer .
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- HY-145479
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PROTACs
Androgen Receptor
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Cancer
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PROTAC AR-V7 degrader-1 is an orally active and selective AR-V7 PROTAC degrader with a DC50 of 0.32 μM (in 22Rv1 cells). PROTAC AR-V7 degrader-1 can inhibit the proliferation of tumor cells and exhibit anti-tumor activity. PROTAC AR-V7 degrader-1 can be used for the research of cancers such as prostate cancer .(Pink: VPC-14228 (HY-117669); Black: linker (HY-W041652); Blue: VHL Ligand (HY-112078))
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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-168534
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SF3B1
Apoptosis
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Cancer
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WX-02-23 is a small-molecule probe that stereoselectively and site-specifically binds to C258 of FOXA1 and C1111 of SF3B1. WX-02-23 remodels FOXA1's chromatin binding and pioneer activity in a DNA-dependent manner, disrupts spliceosome assembly, and enhances the thermal stability of SF3B1. WX-02-23 inhibits tumor cell proliferation and induces apoptosis. WX-02-23 can be used for research on cancers such as prostate 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-126076A
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DNA/RNA Synthesis
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Cancer
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VPC-80051 is an inhibitor of hnRNP A1 splicing activity. VPC-80051 directly interacts with hnRNP A1 RBD and reduces AR-V7 messenger levels in 22Rv1 CRPC cell line. VPC-80051 can be used in prostate cancer research .
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- HY-133045
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Ligands for E3 Ligase
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Cancer
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VHL Ligand 8 is a VHL ligand. VHL Ligand 8 can be used to synthesize ARD-266 (HY-133020), a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM .
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- HY-N7045
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Androgen Receptor
Apoptosis
CDK
Caspase
PSMA
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Cancer
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Isosilybin B is a flavonolignan. Isosilybin B can be isolated from Silybum marianum. Isosilybin B can regulate cell cycle-related proteins (e.g., reduce cyclins (D3, D1, A, E), Cdk4, Cdk2, Cdc25A), and activate Caspases (Caspase-9 and Caspase-3). Isosilybin B can promote Apoptosis, reduce androgen receptor (AR) and PSA. Isosilybin B has anticancer activity against prostate cancer .
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- HY-112659
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MicroRNA
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Neurological Disease
Cancer
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Lin28-let-7 antagonist 1 (compound 1632) is a potent antagonist of Lin28/pre-let-7 interaction. Lin28-let-7 antagonist 1 inhibits Lin28A binding to pre-let-7a-2, with an IC50 of 8 μM. Lin28-let-7 antagonist 1 inhibits proliferation in human cancer cells .
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- HY-162706
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PROTACs
CDK
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Cancer
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BSJ-5-63 is a potent CDK12, CDK7, CDK9 PROTAC degrader. BSJ-5-63 BSJ-5-63 decreases the protein expression of CDK12, CDK7, CDK9, RNAPII, Cyclin K. BSJ-5-63 decreases the mRNA expression of BRCA1, BRCA2. BSJ-5-63 shows anticancer activity and has the potential for the research of prostate cancer (Pink: ligand for target protein (HY-150948); black: linker (HY-W140827); Blue: E3 ligase ligand (HY-112078)) .
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- HY-158432
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Histone Demethylase
PROTACs
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Cancer
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GT-653 is a PROTAC degrader for lysine-specific demethylase 5B (KDM5B). GT-653 degrades 68.35% KDM5B at 10 μM in a ubiquitin proteasome-dependent manner, upregulates H3K4me3 levels, and activates the type-I interferon signaling pathway in prostate cancer cells 22RV1. (Pink: KDM5B ligand (HY-158433); Black: Linker (HY-W004896); Blue: E3 ligase ligand (HY-103596))
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- HY-173177
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Apoptosis
MDM-2/p53
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Cancer
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PSF-IN-2 (Compound (C)-30) is a PSF inhibitor with an IC50 value of 0.005 pM. PSF-IN-2 exhibits anti-cancer activity, and its IC50 value for inhibiting the proliferation of 22Rv1 cells is 0.5 μM. PSF-IN-2 activates the p53 signaling pathway by inhibiting the binding of PSF to RNA, inducing the expression of related genes, promoting apoptosis, and inhibiting the cell cycle. PSF-IN-2 can be used in cancer research .
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- HY-160777
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Galeterone 3β-imidazole
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Molecular Glues
Androgen Receptor
MNK
Apoptosis
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Cancer
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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) .
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- HY-133020
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PROTACs
Androgen Receptor
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Cancer
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ARD-266 is a highly potent and von Hippel-Lindau E3 ligase-based Androgen Receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM . ARD-266 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-162412
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PROTACs
Adrenergic Receptor
Apoptosis
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Cancer
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PROTAC AR/AR-V7 degrader-1 (27c) is a PROTAC-based and dual AR, AR-V7 degrader, with DC50 values of 2.67 and 2.64 μM for AR and AR-V7, respectively. PROTAC AR/AR-V7 degrader-1 (27c) induces apoptosis (Red: AR antagonist; Blue: E3 ligase ligand; Black: linker) .
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- HY-161369
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PROTACs
Histone Acetyltransferase
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Cancer
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CBPD-268 is a potent and orally active CBP/p300 PROTAC degrader with an DC50 value of ≤ 0.03 nM. CBPD-268 induces CBP/p300 degradation and inhibits cell growth. CBPD-268 shows antitumor activity. CBPD-268 has the potential for the research of AR-positive prostate cancer (Structure Note: Red, Androgen receptor degrader (HY-W248665A); Blue, CBP/p300 ligand (HY-161483); Black, Linker) .
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- HY-176835
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Endonuclease
Autophagy
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Cancer
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PNR-3-80 is an endonuclease G (ENDOG) inhibitor with an IC50 of 0.67 μM. As a non-competitive binder to the ENDOG-substrate complex, PNR-3-80 specifically inhibits the endonuclease activity of ENDOG. PNR-3-80 reduces cell death induced by Cisplatin (HY-17394) and Docetaxel (HY-B0011), and inhibits DNA damage and autophagy (autophagy) induced by Etoposide (HY-13629). PNR-3-80 can be used in studies related to cell injury .
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- HY-151385
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JAK
STAT
IFNAR
Interleukin Related
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Cancer
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VVD-118313 (compound 5a) is a potent, selective JAK1 inhibitor. VVD-118313 targets an isoform-restricted allosteric cysteine to block JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer . VVD-118313 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-141860
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PSMA
Microtubule/Tubulin
Reactive Oxygen Species (ROS)
Cytochrome P450
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Cancer
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PSMA-Val-Cit-PAB-MMAE is a small-molecule conjugate targeting PSMA, with Monomethyl auristatin E (MMAE) (HY-15162) as its cytotoxic payload. PSMA-Val-Cit-PAB-MMAE binds to PSMA, thereby being delivered into PSMA-expressing prostate cancer cells. Subsequently, the Val-Cit linker is cleaved under the mediation of cathepsin B, releasing active MMAE. PSMA-Val-Cit-PAB-MMAE inhibits CYP3A4 activity (IC50 = 11.2 μM), induces intracellular ROS production and oxidative stress, disrupts the cytoskeleton through microtubule destabilization, and induces prostate cancer cell death. PSMA-Val-Cit-PAB-MMAE can be used in research related to prostate cancer .
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- HY-164373
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Androgen Receptor
Apoptosis
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Cancer
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SC428 is an androgen receptor (AR) inhibitor that targets the N-terminal domain. SC428 potently decrease the transactivation of (AR)-V7, (AR)v567es, as well as full-length ( AR ) (AR-FL) and its LBD mutants, substantially. SC428 inhibits androgen-stimulated (AR)-FL nuclear translocation, chromatin binding, and (AR) -regulated gene transcription. SC428 inhibits the proliferation of tumor cells in vitro. SC428 inhibits tumor cell growth by inducing apoptosis in mice transplanted with 22RV1 .
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- HY-16187
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HIF/HIF Prolyl-Hydroxylase
Apoptosis
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Cancer
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EL-102 is a hypoxia-induced factor 1 (Hif1α) inhibitor. EL-102 induces apoptosis, inhibits tubulin polymerisation and shows activities against prostate cancer. EL-102 can be used for the research of cancer .
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- HY-108986
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Sirtuin
SARS-CoV
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Cancer
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JFD00244 is a sirtuin 2 (SIRT2) inhibitor, with anti-tumor effect. JFD00244 is also a Nsp-16 inhibitor against SARS-CoV-2 .
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- HY-B0568R
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Reference Standards
Ferroptosis
HCV
Apoptosis
COX
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Infection
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Endocrinology
Cancer
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Deferiprone (Standard) is the analytical standard of Deferiprone. This product is intended for research and analytical applications. Deferiprone is a potent, orally active, brain-penetrant, cell-penetrant, skin-permeable, free iron chelating agent. Deferiprone inhibits the proliferation and migration, and stimulates apoptosis in tumor cell. Deferiprone has antianemic, neuroprotective, anti-inflammatory, antioxidant, and antidotal activity. Deferiprone can be used in cancer, cardiovascular disease, infection, inflammation, and neurological disease study .
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- HY-150268
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BET-IN-16
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Epigenetic Reader Domain
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Cancer
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Zavabresib (BET-IN-16) (Compound I) is a BET inhibitor. BET-IN-16 shows anticancer activity. Zavabresib inhibits prostate cancer cell growth, with IC50 values of 0.043 and 0.034 μM against LNCaP and 22Rv1 cells, respectively .
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- HY-P10781
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Radionuclide-Drug Conjugates (RDCs)
PSMA
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Cancer
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PSMA-D5 has a binding affinity for PSMA with a Ki of 0.21 nM and can be used for PSMA tracing after radiolabeling. PSMA-D5 ([68Ga]-labeled) contains a DOTA chelator, allowing convenient labeling with therapeutic radionuclides such as 177Lu and 225Ac. PSMA-D5 ([68Ga]-labeled) shows excellent pharmacokinetic properties, exhibiting remarkable tumor uptake in 22Rv1 tumors . PSMA-D5 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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- HY-121522
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Histone Demethylase
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Cancer
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SD-70 is an inhibitor for histone demethylase JMJD2C and exhibits antitumor efficacy. SD-70 inhibits viability of cancer cells CWR22Rv1 (9% cell survival at 10 μM), PC3 (14% cell survival at 2 μM) and DU145 (26% cell survival at 2 μM) .
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- HY-149495
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PROTACs
CDK
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Cancer
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CP-07 is a potent and selective PROTACCDK9 degrader (DC50: 43 nM). CP-07 inhibits 22RV1 cell proliferation (IC50: 62 nM) and colony formation by down-regulating Mcl-1 and c-Myc. CP-07 inhibits 22RV1 xenograft tumor growth. CP-07 can be used for research of prostate cancer .
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- HY-103245
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Androgen Receptor
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Cancer
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Cl-4AS-1, a potent steroidal androgen receptor (AR) agonist (IC50 = 12 nM), is also an inhibitor of 5α-reductase types I and II (IC50 = 6 and 10 nM, respectively) .
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- HY-176128
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PROTACs
Androgen Receptor
Apoptosis
PARP
Caspase
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Cancer
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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 .
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- HY-130713
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Thalidomide-C2-amido-C2-COOH contains a CRBN ligand and a linker for recruiting E3 ubiquitin ligases. Thalidomide-C2-amido-C2-COOH can be used to design and synthesize PROTAC CDK2/9 Degrader-1 (HY-130709). PROTAC CDK2/9 Degrader-1 is applicable to prostate cancer-related research .
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- HY-163340
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Glucocorticoid Receptor
Androgen Receptor
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Cancer
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GA32 (compound 58r) is potent androgen receptor (AR)/glucocorticoid receptor (GR) dual inhibitor with IC50 values of 0.13 μM and 0.83 μM for AR and GR, respectively. GA32 inhibits the proliferation of Enzalutamide (HY-70002) resistance castration-resistant prostate cancer both in vitro and in vivo .
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- HY-163281
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Fluorescent Dye
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Cancer
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FSY-OSO2F shows an uptake in MCF-7 cells through the regulation of L-Tyr, ASC, and ASC2 transporters. FSY-OSO2F can be used as a PET tracer, when labeled with 18F, and exhibits good uptake and good contrast in MCF-7 and 22Rv1 subcutaneous tumors .
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- HY-N16066
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CHNQD-0803
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AMPK
Apoptosis
NF-κB
TNF Receptor
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Inflammation/Immunology
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Candidusin A (CHNQD-0803) (Compound 4) is a AMPK activator with a KD of 47.28 nM. Candidusin A can be isolated from marine fungus Aspergillus candidus. Candidusin A has cytotoxic activity and induces apoptosis in human prostate cancer cells (22Rv1, PC-3 and LNCaP cells). Candidusin A reduces adipogenesis genes expression and fat deposition, negatively regulates the NF-κB-TNFα inflammatory axis to suppress inflammation, and ameliorates liver injury and fibrosis. Candidusin A can be used for non-alcoholic steatohepatitis (NASH) research .
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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-163938
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PROTACs
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Cancer
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PROTAC erf3a Degrader-1 (Compound C63) is an orally active PROTAC erf3a Degrader. PROTAC erf3a Degrader-1 inhibits cancer cell proliferation (eg: 22Rv1). PROTAC erf3a Degrader-1 can be used for research of prostate cancer, ovarian cancer, liver cancer, cervical cancer, leukemia, breast cancer. (Red: erf3a ligand (HY-13778); Black: linker (HY-163960); Blue: CRBN ligand (HY-41547)) .
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- HY-163510
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Androgen Receptor
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Cancer
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AR/AR-V7-IN-1 (Compound 20i) is an AR/ARV7 inhibitor (IC50 = 172.85 nM). AR/AR-V7-IN-1 potently inhibits cell growth with IC50 values of 4.87 and 2.07 μM in the LNCaP and 22RV1 cell lines, respectively. AR/AR-V7-IN-1 exhibits effective tumor growth inhibition in the 22RV1 xenograft study. AR/AR-V7-IN-1 can be used for the research of prostate cancer .
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- HY-175454
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DNA/RNA Synthesis
PDGFR
Oxidative Phosphorylation
Mitochondrial Metabolism
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Cancer
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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 .
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- HY-143235
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Epigenetic Reader Domain
Apoptosis
Bcl-2 Family
Caspase
c-Myc
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Cancer
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BRD4 Inhibitor-15 (compound 13) is a potent BRD4 inhibitor, with an IC50 of 18 nM. BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells by regulating Bcl-2/Bax proteins and activating caspase-3 signaling pathway. BRD4 Inhibitor-15 down-regulates the c-Myc level in 22RV1 cells. BRD4 Inhibitor-15 can be used for prostate cancer research .
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- HY-149914
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Androgen Receptor
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Cancer
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WCA-814 is an androgen receptor (AR) antagonist-Hsp90 inhibitor conjugate. WCA-814 induces the degradation of full-length and AR-V7. WCA-814 has cytotoxic effect in prostatic cancer cells (IC50: 171.2 nM, 26.5 nM for LNCaP, 22Rv1 cell) .
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- HY-161769
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PROTACs
Epigenetic Reader Domain
Apoptosis
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Cancer
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HL435 is a heterobifunctional molecule that degrades BRD4 by linking to JQ1, with DC50 of 11.9 nM and 21.9 nM, in MDA-MB-231 and MCF-7 cells, respectively. HL435 inhibits the proliferation of MDA-MB-231, MCF-7, 22Rv1 and A549, arrests the cell cycle and induces apoptosis. HL435 exhibits antitumor activity in mouse model. (Pink: ligand for target protein JQ-1 (HY-78695); Black: linker (HY-W004640); blue: ligand for E3 ligase HL389 (HY-161770))
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- HY-P10622
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Apoptosis
Reactive Oxygen Species (ROS)
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Metabolic Disease
Cancer
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SHLP-3 is a mitochondrial derived peptide encoded by the 16S ribosomal RNA (MT-RNR2) gene. SHLP-3 increases cell viability and reduces apoptosis in insulinoma NIT-1β cells and human prostate cancer 22Rv1 cells. SHLP-3 increases mitochondrial function and exerts cytoprotective effects by increasing mitochondrial oxygen consumption rate (OCR), cellular ATP and reducing the ability to produce ROS. SHLP-3 can be used in the study of diabetes and cancer .
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- HY-133044
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PROTAC Linkers
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Cancer
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Boc-Pip-alkyne-Ph-COOH is a PROTAC linker, which refers to the alkyl/ether composition. Boc-Pip-alkyne-Ph-COOH can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 effectively induces degradation of androgen receptor (AR) protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM . Boc-Pip-alkyne-Ph-COOH is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-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-124056
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CXCR
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Cancer
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AZ10397767 is an orally active, selective CXCR2 receptor antagonist with an IC50 of 1 nM. AZ10397767 attenuates the Oxaliplatin (HY-17371)-induced NF-κB transcriptional activity and potentiates Oxaliplatin-induced apoptosis in androgen-independent prostate cancer (AIPC) cells. AZ10397767 significantly inhibits neutrophil recruitment into tumors which then adversely affects tumor growth in vitro and in vivo .
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- HY-169078
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Histone Methyltransferase
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Cancer
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ML234 is a dual inhibitor against EZH2/LSD1 with IC50 values of 0.09 and 0.12 μM, respectively. ML234 displays an excellent antiproliferative capacity against prostate cancer cell lines LNCAP, PC3 and 22RV1. ML234 suppresses the tumor growth in the 22RV1 xenograft mouse model. ML234 is promising for research of anticancer agents in prostate cancer .
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- HY-P10625
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Apoptosis
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Metabolic Disease
Cancer
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SHLP-6 is a mitochondrial-derived peptide, a biologically active microprotein encoded by the 16S ribosomal RNA (MT-RNR2) gene. SHLP6 increases apoptosis in insulinoma cells NIT1 and human prostate cancer cell 22Rv1. SHLP6 can be used in the study of diabetes and cancer .
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- HY-142772
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Epigenetic Reader Domain
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Cancer
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Y08284 is a potent, selective, oral active CBP bromodomain inhibitor with an IC50 of 4.21 nM. Y08284 suppresses the proliferation of prostate cancer cell lines LNCaP, C4-2B, and 22Rv1. Antitumor activity .
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- HY-121588
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Adrenergic Receptor
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Cancer
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IMTPPE is an inhibitor of the androgen receptor (AR) in C4-2 prostate cancer cells, inhibiting its transcriptional activity and protein levels. IMTPPE inhibited the proliferation of AR-positive prostate cancer cells but had no effect on AR-negative prostate cancer cells. IMTPPE also inhibited the growth of enzalutamide-resistant 22Rv1 xenograft tumors .
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-
- HY-176068
-
|
|
Androgen Receptor
|
Cancer
|
|
3-Cl-Pyridine-amide-acrylaldehyde-piperazine is a synthetic intermediate of LO-4-25 (HY-176067). LO-4-25 is an androgen receptor (AR) DNA binding domain ligand linked via a linker to the truncated fumaramide handle. LO-4-25 shows robust degradation of both AR and AR-V7 in 22Rv1 cells .
|
-
- HY-117136
-
|
|
HDAC
Caspase
Bcl-2 Family
|
Cancer
|
|
AN-7 is an orally active histone deacetylase (HDAC) inhibitor that induces histone hyperacetylation and differentiation in vitro and in vivo, and inhibits the proliferation of human prostate 22Rv1 cancer cells. AN-7 can increase the expression of the pro-apoptotic protein Bax, reduce the expression of the anti-apoptotic protein Bcl-2, and promote apoptosis by activating caspase-3, and can be used in the study of prostate cancer .
|
-
- HY-160260
-
|
|
Epigenetic Reader Domain
Histone Acetyltransferase
|
Cancer
|
|
EP300/CBP-IN-1 (compound 172) is a potent EP300/CBP inhibitor with IC50s of 2.3 nM and 2.1 nM for CBP BRD and EP300 BRD, respectively. EP300/CBP-IN-1 has the inhibitory effect on the proliferation of prostate cancer CWR22RV1 cells .
|
-
- HY-177694
-
|
|
PROTACs
Androgen Receptor
|
Cancer
|
|
PROTAC AR Degrader-11 is a potent androgen receptor and androgen receptor splice variant-7 PROTAC degrader. PROTAC AR Degrader-11 shows potent cytotoxicity against both CWR22RV1 cells and VCaP cells. PROTAC AR Degrader-11 can be used in prostate cancer research . (Structure Note: Pink: Androgen Receptor ligand (HY-171809); Blue: CRBN ligand (HY-A0003); Black: linker (HY-169966))
|
-
- HY-173640
-
|
|
Androgen Receptor
Phosphodiesterase (PDE)
|
Cancer
|
|
ID11916 is an orally active androgen receptor (AR) antagonist and a phosphodiesterase 5 (PDE5) inhibitor. ID11916 blocks androgen binding to AR, nuclear translocation, and androgen-dependent transcriptional activity of AR, while increasing intracellular cGMP levels and activating PKG via inhibition. ID11916 shows potent anti-cancer effect in prostate cancer cell lines VCaP and 22Rv1 and in AR-positive breast cancer cell lines SK-BR-3 .
|
-
- 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-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-146573
-
|
|
Aldose Reductase
17β-HSD
|
Cancer
|
|
AKR1C3-IN-6 (Compound 1) is a potent, selective AKR1C3 inhibitor with IC50 values of 0.31 μM and 73.23 μM against AKR1C3 and AKR1C2, respectively. AKR1C3-IN-6 shows antitumor activity .
|
-
- 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-174908
-
|
|
Histone Methyltransferase
11β-HSD
Androgen Receptor
|
Cancer
|
|
SJL2-1 is a PRMT5 inhibitor, with an IC50 of 1.56 μM. SJL2-1 suppresses proliferation, migration, and invasion in prostate cancer cells. SJL2-1 promotes apoptosis and blocks the cell cycle at the G0/G1 phase. SJL2-1 can target the binding of PRMT5 in cells and inhibit the methylation and expression of the androgen receptor. SJL2-1 can be used for the study of early androgen-sensitive prostate cancer and advanced castration-resistant prostate cancer (CRPC) .
|
-
- HY-170330
-
-
- HY-163609
-
|
|
PROTACs
Aldose Reductase
|
Cancer
|
|
PROTAC AKR1C3 degrader-1 (compound 5) is a potent AKR1C3 PROTAC degrader. PROTAC AKR1C3 degrader-1 decreases the protein expression of AKR1C3, AKR1C1/2, and ARv7. PROTAC AKR1C3 degrader-1 has the potential for the research of prostate cancer. (Blue:ubiquitin E3 ligase cereblon ligand (HY-A0003), Black: linker (HY-163647); Pink: AKR1C3 inhibitor (HY-163610)) .
|
-
- HY-175248
-
|
|
PSMA
|
Cancer
|
|
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) .
|
-
- HY-179123
-
|
|
Androgen Receptor
Apoptosis
|
Cancer
|
|
ZC9 is a novel androgen receptor (AR) degrader. ZC9 directly binds to AR and inhibits Dihydrotestosterone-induced nuclear translocation of AR. ZC9 promotes AR degradation via the ubiquitin-proteasome system and suppresses AR transcriptional activity. ZC9 significantly decreases the mRNA levels of other AR downstream genes, including PSA, TMPRSS2, and PMEPA1. ZC9 promotes Apoptosis. ZC9 exhibits anticancer activity against prostate cancer .
|
-
- HY-149298
-
|
|
PSMA
|
Cancer
|
|
PSMA-IN-2 is an inhibitor of PSMA with a Ki value of 1.07 nM. PSMA-IN-2 displays favorable in vivo NIR imaging (λEM = 1088 nm, λex = 808 nm), and can be used for NIRII image-guided tumor resection surgery in PSMA-positive tumor-bearing mice .
|
-
- HY-146445
-
|
|
Epigenetic Reader Domain
Histone Acetyltransferase
|
Cancer
|
|
P300 bromodomain-IN-1 (Compoun 1u) is a potent p300 (EP300) bromodomain inhibitor with an IC50 of 49 nM. P300 bromodomain-IN-1 suppresses the expression of c-Myc and induces G1/G0 phase arrest and apoptosis in OPM-2 cells .
|
-
- HY-170820
-
|
|
Molecular Glues
Bcl-2 Family
CDK
EGFR
HSP
Androgen Receptor
c-Myc
|
Cancer
|
|
XYD049 is a CRBN-based molecular glue degrader targeting GSPT1, with a DC50 of 19 nM. XYD049 mediates the formation of a ternary complex between CRBN and GSPT1, thereby triggering CRBN- and proteasome-dependent degradation of GSPT1. By degrading GSPT1, XYD049 downregulates castration-resistant prostate cancer (CRPC)-related oncogenes, including BCL2, CDK2, E2F3, EGFR, HSP90B1, TMPRSS2, AR, AR-V7, PSA and c-Myc. XYD049 inhibits cancer cell growth and suppresses tumor growth in mice. XYD049 can be used for research on castration-resistant prostate cancer. XYD049 consists of a linker (black part) NH2-C5-NH-Boc (HY-W004710), a CRBN-based E3 ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547), and a target protein ligand (red part) GSPT1 ligand-1 (HY-170821), among which the E3 ligase ligand plus linker forms the conjugate E3 Ligase Ligand-linker Conjugate 158 (HY-170822) .
|
-
- HY-153718
-
|
|
Ligands for Target Protein for PROTAC
CDK
c-Myc
|
Cancer
|
|
KI-ARv-03 is a potent and selective ATP-competitive CDK9 inhibitor with an IC₅₀ of 0.15 μM (at 45 μM ATP), exhibiting over 130-fold selectivity against other CDKs (including CDK1-7). KI-ARv-03 reduces androgen receptor (AR)-driven transcription and proliferation in prostate cancer cells. KI-ARv-03 can be used for leukemia, pancreatic cancer, alveolar rhabdomyosarcoma (ARMS) and castration-resistant prostate cancer (CRPC) research. KI-ARv-03 is a ligand for target protein for PROTAC. KI-ARv-03 can be used to synthesize PROTAC KI-CDK9d-32 (HY-173523) [1][2].
|
-
- HY-176836
-
|
|
Endonuclease
|
Cancer
|
|
PNR-3-82 is a selective Apoptotic endonuclease G (EndoG) inhibitor with an IC50 of 0.61 μM for EndoG over DNase I. PNR-3-82 does not inhibit five cell death-related enzymes including DNase II, RNase A, proteinase, lactate dehydrogenase and superoxide dismutase 1. PNR-3-82 has a cytoprotective activity and blocks Cisplatin (HY-17394) and Docetaxel (HY-B0011)-induced cell death. PNR-3-82 can be used for cell injuries research .
|
-
- HY-174377
-
|
|
Androgen Receptor
p38 MAPK
Caspase
Cytochrome P450
Calcium Channel
Reactive Oxygen Species (ROS)
Apoptosis
Mitochondrial Metabolism
GLUT
|
Cancer
|
|
PeS-9 is an Androgen Receptor (AR) degrader that induces androgen receptor degradation PeS-9 induces mitochondrial and ER stress by promoting cytotoxic ROS production, leading to the release of mitochondrial cytochrome C and AIF. PeS-9 subsequently activates caspases-9 and -3, causing DNA fragmentation and apoptotic cell death. PeS-9 has anticancer activity against prostate cancer and exerts in vivo antitumor and antimetastatic activity with minor side effects. PeS-9 can be used for the study of targeting monotherapy against GLUT-1-overexpressing tumors .
|
-
- HY-163938A
-
|
|
PROTACs
|
Cancer
|
|
PROTAC erf3a Degrader-2 (Compound C59) is an orally active PROTAC erf3a Degrader. PROTAC erf3a Degrader-2 inhibits protein expression of SRD5A3 and GSPT1(eRF3a). PROTAC erf3a Degrader-2 inhibits cancer cell proliferation (eg: 22Rv1). PROTAC erf3a Degrader-2 can be used for research of prostate cancer, ovarian cancer, liver cancer, cervical cancer, leukemia, breast cancer. (Red: erf3a ligand (HY-13778); Black: linker (HY-163960); Blue: E3 ligase ligand (HY-W763812)) .
|
-
- HY-172886
-
|
|
PI3K
Bcl-2 Family
Apoptosis
|
Cancer
|
|
PI3K-IN-58 (Compound 17f) is a PI3Kα inhibitor (IC50: 0.039 μM). PI3K-IN-58 exhibits significant antiproliferative effects on PC-3, 22RV1, MDA-MB-231 and MDA-MB-453 cell lines with IC50s of 3.48 μM, 1.06 μM, 2.21 μM and 0.93 μM, respectively. PI3K-IN-58 induces apoptosis by downregulating the expression levels of anti-apoptotic proteins Bcl-XL and Bcl-2 and upregulating the expression of anti-apoptosis protein BAX. PI3K-IN-58 can be used in PI3K-targeted cancer research .
|
-
- 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-156059
-
|
|
Androgen Receptor
Neprilysin
|
Neurological Disease
Metabolic Disease
|
|
NEP28 is a selective androgen receptor modulator with an EC50 of 2.90 nM in 22RV1 cells. NEP28 increases the activity of Aβ-degrading enzyme neprilysin. NEP28 is efficacious in muscle and brain without serious side effects on prostate in rats. NEP28 can be used for osteoporosis, sarcopenia, and Alzheimer's disease 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-146574
-
|
|
Aldose Reductase
17β-HSD
|
Cancer
|
|
AKR1C3-IN-7 (Compound 13) is a potent, selective AKR1C3 inhibitor with an IC50 of 0.19 μM. AKR1C3-IN-7 shows antitumor activity .
|
-
- HY-164005
-
-
- HY-146575
-
|
|
Aldose Reductase
17β-HSD
|
Cancer
|
|
AKR1C3-IN-8 (Compound 5) is a potent, selective AKR1C3 inhibitor with an IC50 of 0.069 μM. AKR1C3-IN-8 shows antitumor activity .
|
-
- HY-158433
-
-
- HY-163192
-
|
|
ROR
Apoptosis
|
Cancer
|
|
W6134 is highly potent and selective RORγ covalent inhibitor with an IC50 of 0.21 μM. W6134 exhibits excellent selectivity for RORγ over RORα, RXRγ, and ERRγ. W6134 significantly inhibits RORγ transcriptional activity W6134 inhibits the proliferation and colony formation and induces apoptosis in castration-resistant prostate cancer cells (CRPC). W6134 can be used for the research of castration-resistant prostate cancers (CRPC) .
|
-
- HY-173559
-
|
|
Androgen Receptor
|
Cancer
|
|
AR antagonist 12 (compound 20i) is an orally active androgen receptor antagonist wiith IC50 values of 119.3 μM and 98.2 μM for wt-AR and AR-F877L,respectively. AR antagonist 12 induces a dose-dependent and time-dependent reduction in AR, AR-V7, and PSA protein levels. AR antagonist 1 shows anticancer activuty and can be used for the study of Enzalutamide (HY-70002)-resistant Prostate cancer .
|
-
- HY-162764
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor degrader-5 (compound 14k) exhibits promising properties, including superior androgen receptor degradation activity and antiproliferative activity .
|
-
- HY-149927
-
|
|
Drug Derivative
|
Cancer
|
|
Antitumor agent-91 is a cyclic phosphate ester derivative with anticancer and anti-proliferative activities. Antitumor agent-91 has potential application in human castration resistant prostate cancer and pancreatic cancer .
|
-
- HY-122108
-
|
LL-Z 1272-alpha
|
Apoptosis
|
Cancer
|
|
Ilicicolin A is a potent anticancer agent. Ilicicolin A induces apoptosis. Ilicicolin A inhibits cell growth and colony formation. Ilicicolin A shows antitumor activity. Ilicicolin A has the potential for the research of 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-161770
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
HL389 inhibits proliferation of cancer cells MDA-MB-231 and MCF-7, with IC50 of 11.39 μM and 9.66 μM. HL389 can be utilized as the ligand for E3 ligase for the synthesis of PROTAC degrader HL435 (HY-161769) .
|
-
- HY-143317
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
XY153 (compound 8l) is a BD2-selective BET inhibitor and selectively binds to BRD4 BD2. XY153 binds to BRD4 BD2, BRD3 BD2 and BRD2 BD2 with IC50s of 0.79, 5.31 and 5.09 nM, respectively. XY153 shows potent antiproliferative activity against multiple tumor cell lines. XY153 can be used for the research of acute myeloid leukemia (AML) and cancer .
|
-
- HY-162568
-
|
|
DNA Stain
|
Cancer
|
|
7-tert-Butylfascaplysin (7-TB) is a derivative of Fascaplysin (HY-112328), that can be isolated from Fascaplysinopsis sp.. 7-tert-Butylfascaplysin induces replication stress, leads to toxic DNA double-strand breaks and apoptosis-like cell death, and thus exhibits cytotoxicity in cancer cells in nanomolar levels. 7-tert-Butylfascaplysin exhibits DNA intercalating activity with EC50 of 3.2 μM .
|
-
- HY-151266
-
|
|
Androgen Receptor
|
Cancer
|
|
AR antagonist 4 (Compound 67-b) is an orally active androgen receptor (AR) antagonist with an IC50 of 246.6 nM against wt-AR, and is also an AR degrader with a DC50 of 2.84 μM .
|
-
- HY-179016
-
|
|
Ferroptosis
Apoptosis
Mitochondrial Metabolism
Calcium Channel
|
Cancer
|
|
Ferroptosis/apoptosis inducer-3 (Compound 34) is a Ferroptosis and Apoptosis inducer. Ferroptosis/apoptosis inducer-3 induces both Ferroptosis and Apoptosis by causing G2/M phase cell cycle arrest, disrupting mitochondrial membrane potentials, promoting lipid peroxidation, and increasing the levels of Ca 2+ and Fe 2+ through the activation of calcium/calmodulin signaling. Ferraplasm/apoptosis inducer-3 shows anticancer effects against cervical cancer, adenocarcinoma, breast cancer, colon cancer, and colorectal carcinoma .
|
-
- 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-182534
-
|
|
Succinate Dehydrogenase
|
Cancer
|
|
Succinate dehydrogenase-IN-12 is a selective inhibitor of mitochondrial complex II (succinate dehydrogenase), with an IC50 value of 3.3 nM. Succinate dehydrogenase-IN-12 can be used for tumor research .
|
-
- HY-103245R
-
|
|
Reference Standards
Androgen Receptor
|
Cancer
|
|
Cl-4AS-1 (Standard) is the analytical standard of Cl-4AS-1 (HY-103245). This product is intended for research and analytical applications. Cl-4AS-1, a potent steroidal androgen receptor (AR) agonist (IC50 = 12 nM), is also an inhibitor of 5α-reductase types I and II (IC50 = 6 and 10 nM, respectively) .
|
-
- HY-161773
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
HL389-NHC2-PEG3-C2NH inhibits proliferation of cancer cells MDA-MB-231 and MCF-7, with IC50 of 11.39 μM and 9.66 μM. HL389-NHC2-PEG3-C2NH can be utilized as a conjugate of an E3 ligase ligand and a linker, for the synthesis of PROTAC degrader HL435 (HY-161769) .
|
-
- HY-108986R
-
|
|
Reference Standards
Sirtuin
SARS-CoV
|
Cancer
|
|
JFD00244 (Standard) is the analytical standard of JFD00244 (HY-108986). This product is intended for research and analytical applications. JFD00244 is a sirtuin 2 (SIRT2) inhibitor, with anti-tumor effect. JFD00244 is also a Nsp-16 inhibitor against SARS-CoV-2 .
|
-
- 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-181727
-
|
|
Androgen Receptor
HSP
CDK
|
Cancer
|
|
AR/AR-V7 degrader-1 is an orally active AR and AR-V7 degrader. AR/AR-V7 degrader-1 disrupts the interaction between AR/AR-V7 and HSP90, leading to their ubiquitination and degradation in castration-resistant prostate cancer cells. AR/AR-V7 degrader-1 regulates the expression of cell cycle-related proteins in prostate cancer cells (downregulates CDK4, CDK6, Cyclin D1, Cyclin E1; upregulates P21) and induces G0/G1 phase arrest. AR/AR-V7 degrader-1 inhibits the proliferation and migration of prostate cancer cells. AR/AR-V7 degrader-1 suppresses the growth of castration-resistant prostate cancer tumors in nude mice and induces the degradation of AR and AR-V7 in tumor tissues. AR/AR-V7 degrader-1 is applicable to the research of castration-resistant prostate cancer .
|
-
- HY-N16404
-
|
|
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
Asperindole A is an indole-diterpene alkaloid. Asperindole A can be isolated from fungus Aspergillus sp. KMM 4676. Asperindole A induces Apoptosis. Asperindole A exerts cytotoxic activity against hormone-resistant and hormone-sensitive prostate cancer cells .
|
-
- 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-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-143332
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
TRIM24/BRPF1-IN-2 (compound 20l) is a potent TRIM24/BRPF1 dual inhibitor, with IC50 values of 0.98 and 1.16 μM, respectively. TRIM24/BRPF1-IN-2 shows TRIM24/BRPF1 bromodomain binding affinity. TRIM24/BRPF1-IN-2 can be used for prostate 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-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-182331
-
|
|
PROTACs
RAR/RXR
Androgen Receptor
Apoptosis
Caspase
MDM-2/p53
|
Cancer
|
|
WCF-598 is a RXRγ (Kd: 234.2 nM) PROTAC degrader. WCF-598 induces RXRγ degradation via the ubiquitin-proteasome pathway and binds directly to RXRγ. WCF-598 indirectly induces AR-V7 degradation, impairs the stability of the RXRγ-AR-V7 complex, downregulates AR-V7 levels, and inhibits the transcription of downstream target genes of AR-V7. WCF-598 induces tumor cell apoptosis, inhibits cell proliferation, activates the p53 signaling pathway, and suppresses cell cycle progression. WCF-598 can be used for the research of prostate cancer .
|
-
- HY-182288
-
|
|
STAT
Apoptosis
|
Cancer
|
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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 .
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- HY-183602
-
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DNA/RNA Synthesis
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Cancer
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FRC-303 is a CHD1 inhibitor with a Kd of 0.14 μM and an IC50 of 0.18 μM. FRC-303 binds to the H3K4me3 binding site of CHD1 tandem chromodomain, forms aromatic cage interactions and extended ligand contacts, acts as a methyl-lysine mimic, and occupies natural peptide ligand-binding regions. FRC-303 can be used for the research of prostate cancer .
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- HY-181427
-
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Androgen Receptor
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Cancer
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UT-143 is an orally active, selective irreversible covalent antagonist of androgen receptor (AR). UT-143 inhibits the proliferation of AR-positive prostate cancer cells, reduces the weight of androgen target tissues in rats, and suppresses the growth of AR-positive xenograft tumors. UT-143 can be used for the research of prostate cancer .
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- HY-181790
-
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Ligands for Target Protein for PROTAC
Histone Methyltransferase
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Cancer
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DOT1L ligand-2 (Compound 52) is a DOT1L ligand. DOT1L ligand-2 acts as a Ligand for Target Protein for PROTAC, which is used to develop and design degraders of PROTAC DOT1L, such as DOT1L808 (HY-181789). DOT1L ligand-2 is applicable to research related to MLL-rearranged leukemia .
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-
- HY-172247
-
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ATM/ATR
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Cancer
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ATR-IN-31 is a selective ATR kinase inhibitor with an IC50 of 7 nM. ATR-IN-31 does not significantly inhibit ATM kinase activity. ATR-IN-31 inhibits viability of prostate cancer cells.ATR-IN-31 can be used for the research of prostate cancer .
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- HY-183603
-
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DNA/RNA Synthesis
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Cancer
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FRC-222 is a CHD1 tandem chromodomain inhibitor with a Kd of 0.15 μM and an IC50 of 0.18 μM. FRC-222 binds to the H3K4me3 binding site of CHD1 tandem chromodomain via aromatic cage interactions and extended ligand contacts. FRC-222 can be used for the research of prostate cancer[1].
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- HY-184126
-
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Androgen Receptor
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Cancer
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JZY3221 is an androgen receptor (AR) inhibitor. JZY3221 binds to the AR ligand-binding domain to inhibit AR function. JZY3221 constitutes the AR inhibitory moiety of DALTAC JZY3032 (HY-184124). JZY3221 is applicable to research related to prostate cancer .
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- HY-168555
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PROTACs
CDK
Apoptosis
Akt
mTOR
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Cancer
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YJ1206 is an orally active selective CDK12/CDK13 PROTAC degrader. YJ1206 induces DNA damage and genomic instability, activates the AKT pathway, and triggers apoptosis. YJ1206 reduces tumor cell viability, inhibits tumor growth, and attenuates tumor cell dissemination. YJ1206 is applicable to research related to prostate cancer and high-grade serous tubo-ovarian cancer .
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- HY-159805
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|
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CDK
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Cancer
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CDK2-IN-31 is a CCNE1:CDK2 complex inhibitor with an IC50 of 0.13 μM. CDK2-IN-31 binds to a cryptic allosteric pocket at the CCNE1:CDK2 interface, inducing structural rearrangements of the CDK2 A-loop that disrupt the kinase's active conformation and interfere with substrate binding. CDK2-IN-31 inhibits phosphorylation of retinoblastoma protein 1 (RB1) in CCNE1-dependent ovarian cancer cells. CDK2-IN-31 impairs coenrichment of protein PRC1 with CCNE1-N112C:CDK2 complexes. CDK2-IN-31 can be used for the research of ovarian cancer .
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- HY-181853
-
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Radionuclide-Drug Conjugates (RDCs)
PSMA
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Cancer
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NOTA-SP₂A-PSMAL is a ligand targeting prostate-specific membrane antigen (PSMA), which competitively binds to PSMA with high binding affinity and an IC50 value of 0.26 nM. 18F-labeled NOTA-SP2A-PSMAL can be used as a PET tracer for positron emission tomography imaging of prostate cancer. NOTA-SP2A-PSMAL can be used for the synthesis and research of radionuclide conjugates (RDCs) .
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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-N17406
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-
| Cat. No. |
Product Name |
Type |
-
- HY-D3353
-
|
|
Fluorescent Dye
|
|
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 .
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| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P10781
-
|
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Radionuclide-Drug Conjugates (RDCs)
PSMA
|
Cancer
|
|
PSMA-D5 has a binding affinity for PSMA with a Ki of 0.21 nM and can be used for PSMA tracing after radiolabeling. PSMA-D5 ([68Ga]-labeled) contains a DOTA chelator, allowing convenient labeling with therapeutic radionuclides such as 177Lu and 225Ac. PSMA-D5 ([68Ga]-labeled) shows excellent pharmacokinetic properties, exhibiting remarkable tumor uptake in 22Rv1 tumors . PSMA-D5 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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-
- HY-P10622
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|
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Apoptosis
Reactive Oxygen Species (ROS)
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Metabolic Disease
Cancer
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SHLP-3 is a mitochondrial derived peptide encoded by the 16S ribosomal RNA (MT-RNR2) gene. SHLP-3 increases cell viability and reduces apoptosis in insulinoma NIT-1β cells and human prostate cancer 22Rv1 cells. SHLP-3 increases mitochondrial function and exerts cytoprotective effects by increasing mitochondrial oxygen consumption rate (OCR), cellular ATP and reducing the ability to produce ROS. SHLP-3 can be used in the study of diabetes and cancer .
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- HY-P10625
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Apoptosis
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Metabolic Disease
Cancer
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SHLP-6 is a mitochondrial-derived peptide, a biologically active microprotein encoded by the 16S ribosomal RNA (MT-RNR2) gene. SHLP6 increases apoptosis in insulinoma cells NIT1 and human prostate cancer cell 22Rv1. SHLP6 can be used in the study of diabetes and cancer .
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| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P99762
-
|
MGD009
|
CD3
|
Cancer
|
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Obrindatamab is a humanized anti-B7-H3/CD3 bispecific antibody. Obrindatamab binds to B7-H3 and CD3, thereby mediating redirected cytotoxic T-lymphocyte (CTL) activity against B7-H3-expressing cancer cells. Obrindatamab can be used in research of cancer .
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-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N7045
-
-
-
- HY-N16066
-
|
CHNQD-0803
|
Monophenols
Microorganisms
Phenols
Source Classification
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AMPK
Apoptosis
NF-κB
TNF Receptor
|
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Candidusin A (CHNQD-0803) (Compound 4) is a AMPK activator with a KD of 47.28 nM. Candidusin A can be isolated from marine fungus Aspergillus candidus. Candidusin A has cytotoxic activity and induces apoptosis in human prostate cancer cells (22Rv1, PC-3 and LNCaP cells). Candidusin A reduces adipogenesis genes expression and fat deposition, negatively regulates the NF-κB-TNFα inflammatory axis to suppress inflammation, and ameliorates liver injury and fibrosis. Candidusin A can be used for non-alcoholic steatohepatitis (NASH) research .
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-
-
- HY-122108
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|
LL-Z 1272-alpha
|
Microorganisms
Phenols
Polyphenols
Source Classification
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Apoptosis
|
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Ilicicolin A is a potent anticancer agent. Ilicicolin A induces apoptosis. Ilicicolin A inhibits cell growth and colony formation. Ilicicolin A shows antitumor activity. Ilicicolin A has the potential for the research of prostate cancer .
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-
-
- HY-N16404
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-
-
- HY-N17406
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-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-133020
-
|
|
|
PROTAC Synthesis
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ARD-266 is a highly potent and von Hippel-Lindau E3 ligase-based Androgen Receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM . ARD-266 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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