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Results for "

prostate cancer

" in MCE Product Catalog:

287

Inhibitors & Agonists

2

Screening Libraries

17

Peptides

5

Inhibitory Antibodies

33

Natural
Products

1

Recombinant Proteins

11

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas
  • HY-N10491
    Spongionellol A

    P-glycoprotein Cancer
    Spongionellol A is a MDR1 (p-glycoprotein) inhibitor. Spongionellol A has high cytotoxic activity and selectivity in prostate cancer cells by inducing caspase‑dependent apoptosis. Spongionellol A can be used in the research of cancers, such as prostate cancer.
  • HY-P99188
    Carlumab

    CNTO 888

    CCR Cancer
    Carlumab (CNTO 888) is a humanised anti-CCL2 (chemokine ligand 2) antibody with high affinity. Carlumab can be used in cancer research, particularly in prostate cancer.
  • HY-14249
    Bicalutamide

    Androgen Receptor Autophagy Cancer
    Bicalutamide is an orally active non-steroidal androgen receptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer.
  • HY-N10492
    Spongionellol A analog 1

    P-glycoprotein Cancer
    Spongionellol A analog 1, an analog of Spongionellol A (HY-10491), is a MDR1 (p-glycoprotein) inhibitor. Spongionellol A analog 1 has high cytotoxic activity and selectivity in prostate cancer cells by inducing caspase‑dependent apoptosis. Spongionellol A analog 1 can be used in the research of cancers, such as prostate cancer.
  • HY-118091A
    Bexlosteride

    LY300502

    Others Cancer
    Bexlosteride (LY300502) is a benzoquinolinone human type I 5α-reductase inhibitor. Bexlosteride shows metabolic inhibitory, antiproliferative, and antisecretory effects in LNCaP human prostatic adenocarcinoma cell cultures. Bexlosteride can be used for the research of prostatic cancer.
  • HY-W013272
    Hydroxyflutamide

    HFT

    Androgen Receptor Cancer
    Hydroxyflutamide (HF), an active metabolite of Flutamide, is a potent androgen receptor antagonist (IC50=700 nM). Hydroxyflutamide can be used for the research of prostate cancer.
  • HY-110154
    NSC636819

    Histone Demethylase Cancer
    NSC636819 is a competitive and selective inhibitor of KDM4A/KDM4B. KDM4A/KDM4B are potential progression factors for prostate cancer. NSC636819 has the potential for the research of cancer diseases, especially prostate cancer.
  • HY-138641
    Bavdegalutamide

    ARV-110

    Androgen Receptor Cancer
    Bavdegalutamide (ARV-110) is an orally active, specific androgen receptor (AR) PROTAC degrader. Bavdegalutamide promotes ubiquitination and degradation of AR. Bavdegalutamide can be used for the research of prostate cancer.
  • HY-136383
    AZA1

    Rac1/Cdc42-IN-1

    Ras Apoptosis Cancer
    AZA1 is a potent dual inhibitor of Rac1 and Cdc42. AZA1 induces prostate cancer cells apoptosis and inhibits prostate cancer cells proliferation, migration and invasion.
  • HY-N7924
    Astragenol

    Others Cancer Inflammation/Immunology
    Astragenol is an intermediate used for Astragenol derivative synthesis. Astragenol derivatives are promising anti-inflammatory agents for prostate cancer research.
  • HY-16247
    Apoptone

    HE3235

    Others Cancer
    Apoptone, synthetic analogue of 3β-androstanediol, is an orally bioavailable anticancer agent. Apoptone is active in rodent models of prostate and breast cancer.
  • HY-130574
    MnTE-2-PyP chloride

    BMX-010 chloride

    Reactive Oxygen Species Cancer
    MnTE-2-PyP (BMX-010) chloride is a ROS scavenger and potent radioprotector. MnTE-2-PyP also is a manganese porphyrin, protects normal prostate tissue from radiation damage. MnTE-2-PyP can be used for the research of diabetic prostate cancer.
  • HY-16375
    Ozarelix

    D-63153

    GnRH Receptor Apoptosis Cancer
    Ozarelix (D-63153) is a GnRH antagonist. Ozarelix induces cell apoptosis and arrests cell in G2/M phase. Ozarelix can be used in the research of prostate cancer.
  • HY-105173
    Teverelix

    EP 24332

    GnRH Receptor Histamine Receptor Cancer Endocrinology
    Teverelix (EP 24332) is a GnRH antagonist. Teverelix binds competitively and reversibly to GnRH receptors, thereby suppressing the release of LH and FSH. Teverelix can be used in the research of prostatic hyperplasia, endometriosis, and prostate cancer.
  • HY-125399
    PSMA-11

    HBED-CC-PSMA

    Others Cancer
    PSMA-11 is a positron emission tomography (PET) tracer. PSMA-11 detects prostate cancer relapses and metastases by binding to the extracellular domain of prostate-specific membrane antigen (PSMA).
  • HY-128172
    TRPM4-IN-2

    NBA

    TRP Channel Cancer
    TRPM4-IN-2 (NBA) is a potent transient receptor potential melastatin 4 (TRPM4) inhibitor with an IC50 value of 0.16 μM. TRPM4-IN-2 can be used for researching prostate cancer and colorectal cancer.
  • HY-P2450
    Leucinostatin A

    Antibiotic P168

    Fungal Antibiotic Cancer Infection
    Leucinostatin A (Antibiotic P168) is a nonapeptide exerting a remarkable activity especially against Candida albicans and Cryptococcus neoformans. Leucinostatin A is a hydrophobic nonapeptide antibiotic. Leucinostatin A inhibits prostate cancer growth through reduction of insulin-like growth factor-I expression in prostate stromal cells. Antiprotozoal activies.
  • HY-124292
    Honokiol DCA

    Honokiol dichloroacetate

    Androgen Receptor Cancer
    Honokiol DCA (Honokiol dichloroacetate) is a dichloroacetate analog of Honokiol. Honokiol DCA can inhibit the growth of human prostate cancer cells in vitro and suppress the androgen receptor (AR) protein level.
  • HY-W017186
    ALDH1A3-IN-3

    Aldehyde Dehydrogenase (ALDH) Cancer
    ALDH1A3-IN-3 (compound 16) is a potent inhibitor of ALDH1A3, with an IC50 of 0.26 μM. ALDH1A3-IN-3 is also a good ALDH3A1 substrate. ALDH1A3-IN-3 can be used for the research of prostate cancer.
  • HY-16168A
    Degarelix

    GnRH Receptor Apoptosis Cancer Endocrinology
    Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist. Degarelix can be used for prostate cancer research.
  • HY-16168B
    Degarelix acetate hydrate

    GnRH Receptor Apoptosis Cancer Endocrinology
    Degarelix acetate hydrate is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist. Degarelix acetate hydrate can be used for prostate cancer research.
  • HY-N2059
    Santalol

    Others Cancer
    Santalol is a mixture of α and β-isomer santalol. α-santalol is isolated from sandalwood oil. α-santalol is a promising anti-cancer agent against cancers such as oral, breast, prostate and skin cancer.
  • HY-16498
    Tigapotide

    PCK-3145

    Apoptosis Cancer
    Tigapotide (PCK-3145) is an anti-tumour peptide that reduces the development of skeletal metastases associated with prostate cancer. Tigapotide induces apoptosis and reduces tumour parathyroid hormone-related peptide (PTHrP) levels.
  • HY-118134
    Hepln-13

    Others Cancer
    Hepln-13 is a potent and orally active Hepsin inhibitor with an IC50 of 0.33 µM. Hepln-13 can be used for the research of metastatic prostate cancer.
  • HY-122197
    ML339

    CXCR Cancer
    ML339 is a potent and selective CXCR6 (IC50 of 140 nM) antagonist that is selective (IC50 >79 μM) against CXCR5, CXCR4, CCR6 and Apelin receptor (APJ). ML339 holds potential to advance the field of prostate cancer research.
  • HY-13673
    Goserelin

    ICI 118630

    GnRH Receptor Apoptosis Cancer Endocrinology
    Goserelin (ICI 118630), a decapeptide analogue of gonadotropin-releasing hormone (GnRH/LHRH), functions as a GnRH agonist. Goserelin can be used for the research of breast cancer, epithelial ovarian cancer and prostate cancer.
  • HY-13673A
    Goserelin acetate

    ICI-118630 acetate

    GnRH Receptor Apoptosis Endocrinology Cancer
    Goserelin acetate (ICI-118630 acetate), a decapeptide analogue of gonadotropin-releasing hormone (GnRH/LHRH), functions as a GnRH agonist. Goserelin acetate can be used for the research of breast cancer, epithelial ovarian cancer and prostate cancer.
  • HY-136582
    Androgen receptor-IN-2

    Androgen Receptor Cancer
    Androgen receptor-IN-2 is a potent and orally active androgen receptor inhibitor. Androgen receptor-IN-2 has antitumor activity against prostate cancer.
  • HY-100199
    HUHS015

    Others Cancer
    HUHS015 is a potent prostate cancer antigen-1 (PCA-1/ALKBH3) inhibitor with an IC50 of 0.67μM for PCA-1.
  • HY-146396
    Anticancer agent 51

    Others Cancer
    Anticancer agent 51 (compound 3d) is a potent anticancer agent with an Ki of 731.62 nM. Anticancer agent 51 shows anticancer activity. Anticancer agent 51 has the potential for the research of prostate cancer.
  • HY-144669
    ALDH1A3-IN-2

    Aldehyde Dehydrogenase (ALDH) Cancer
    ALDH1A3-IN-2 (Compound 15) is a potent inhibitor of ALDH1A3 with an IC50 of 1.29 μM. Aldehyde dehydrogenases (ALDHs) are overexpressed in various tumor types including prostate cancer. ALDH1A3-IN-2 has the potential for the research of cancer diseases.
  • HY-144671
    ALDH3A1-IN-2

    Aldehyde Dehydrogenase (ALDH) Cancer
    ALDH3A1-IN-2 (Compound 19) is a potent inhibitor of ALDH3A1 with an IC50 of 1.29 μM. Aldehyde dehydrogenases (ALDHs) are overexpressed in various tumor types including prostate cancer. ALDH3A1-IN-2 has the potential for the research of cancer diseases.
  • HY-148377
    Abiraterone sulfate N-oxide

    Others Cancer
    Abiraterone sulfate N-oxide is a carboxylic acid. Abiraterone sulfate N-oxide also is a major metabolite of Abiraterone (HY-70013). Abiraterone sulfate N-oxide can be used for the research of prostate cancer.
  • HY-P99183
    Abituzumab

    EMD 525797; DI17E6

    Integrin Cancer
    Abituzumab (DI17E6) is a humanised anti-integrin αV monoclonal antibody (IgG2 type). Abituzumab effectively reduces the phosphorylation of FAK, Akt and ERK. Abituzumab can be used in cancer research, particularly in prostate cancer.
  • HY-N10265
    Stephacidin B

    Endogenous Metabolite Cancer
    Stephacidin B is a fungal metabolite. Stephacidin B shows in vitro cytotoxicity against a panel of human tumor cell lines. Stephacidin B shows the strongest cytotoxicity against testosterone-dependent prostate LNCaP cancer cells.
  • HY-119694
    Rotenolone

    Others Cancer
    Rotenolone is an antiproliferative agent. Rotenolone shows antiproliferative activity against the ovarian cancer A2780, breast cancer BT-549, prostate cancer DU 145, NSCLC NCI-H460, and colon cancer HCC-2998 cell lines, with IC50s of 0.95, 1.6, 2.7, 2.0, and 2.9 μM, respectively.
  • HY-145451
    Androgen receptor antagonist 2

    Androgen Receptor Cancer Metabolic Disease
    Androgen receptor antagonist 2 (example 12) is an androgen receptor antagonist. Androgen receptor antagonist 2 can be used for prostate cancer and male hair loss research.
  • HY-103184
    Proxalutamide

    GT0918; Pruxelutamide

    Androgen Receptor SARS-CoV Cancer
    Proxalutamide (GT0918) is an orally active potent androgen receptor (AR) antagonist. Proxalutamide (GT0918) can be used in the study for prostate cancer and COVID-19.
  • HY-108250
    (R)-Bicalutamide

    Androgen Receptor Cancer
    (R)-Bicalutamide is the (R)-enantiomer of Bicalutamide (HY-14249). (R)-Bicalutamide is an androgen receptor (AR) antagonist, with antineoplastic activity. (R)-Bicalutamide is widely used for the research of prostate cancer.
  • HY-145312
    ATR-IN-4

    ATM/ATR Cancer
    ATR-IN-4 is a potent ATR (Ataxia telangiectasia mutated gene Rad 3-associated kinase) inhibitor. ATR-IN-4 inhibits growth of human prostate cancer cells DU145 and human lung cancer cells NCI-H460 with IC50s of 130.9 nM and 41 .33 nM, respectively. (Patent CN112142744A, compound 13).
  • HY-137193
    5,6-Dihydroabiraterone

    Drug Metabolite Cancer
    5,6-Dihydroabiraterone is the metabolism of Abiraterone (HY-70013). Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, and shows antitumor activity in CRPC (castration-resistant prostate cancer).
  • HY-132292
    ARD-2128

    PROTACs Androgen Receptor Cancer
    ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer.
  • HY-145388
    AU-15330

    PROTACs Epigenetic Reader Domain Cancer
    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.
  • HY-16079
    AZD3514

    Androgen Receptor Cancer
    AZD3514 is an orally activie and selective androgen receptor (AR) inhibitor. AZD3514 androgen-dependently and -independently inhibits AR signal. AZD351 down-regulates nuclear AR levels in human LNCaP prostate cancer cells in the absence of androgen with an pIC50 value of 5.75. AZD3514 can be used for the research of prostate cancer.
  • HY-131724
    4-(Dodecylamino)phenol

    p-DDAP; p-Dodecylaminophenol

    Apoptosis Cancer
    4-(Dodecylamino)phenol (p-DDAP) is an anticancer agent. 4-(Dodecylamino)phenol has anti-tumor activity and can suppress proliferation, arrest the cell cycle and induce apoptotic cell death. 4-(Dodecylamino)phenol can be used for the research of cancer, such as prostate cancer.
  • HY-146397
    TD-802

    PROTACs Androgen Receptor Cancer
    TD-802 (Compound 33c) is an androgen receptor (AR) PROTAC degrader with good microsomal stability. TD-802 has good antitumor efficacy in vivo and can be used for metastatic castration-resistant prostate cancer research.
  • HY-116501
    VPC-14449

    Androgen Receptor Cancer
    VPC-14449 is a potent and selective inhibitor of the DNA-binding domain of the androgen receptor (AR-DBD), with IC50 of 0.34 μM for full-length human AR. VPC-14449 reduces the ability of full-length AR as well as AR variants to interact with chromatin. VPC-14449 can be used for the research of prostate cancer.
  • HY-N6601
    Pomolic acid

    Randialic acid A

    Apoptosis Cancer
    Randialic acid A (Pomolic acid) is a pentacyclic triterpene isolated from Euscaphis japonica (Tunb.). Randialic acid A (Pomolic acid) inhibits tumor cells growth and induces cell apoptosis. Randialic acid A (Pomolic acid) has a potential for the treatment of prostate cancer (PC).
  • HY-W412264
    Pim-1/2 kinase inhibitor 1

    Pim Cancer
    Pim-1/2 kinase inhibitor 1 is an orally active pim-1/2 kinase inhibitor. Pim-1/2 kinase inhibitor 1 blocks the ability of Pim kinases to phosphorylate peptides, and inhibits the pim protein kinase directed phosphorylation of 4E-BP1 and p27 Kip1. Pim-1/2 kinase inhibitor 1 can be used in study of cancer, especially prostate cancer.
  • HY-144094
    EZH2-IN-9

    Histone Methyltransferase Cancer
    EZH2-IN-9 is a potent inhibitor of EZH2. EZH2 overexpression or mutations in the SET region (Y641F, Y641N, A687V, A677G point mutations) all lead to abnormal elevation of H3K27me3 and promote the growth and development of many types of tumors, such as breast cancer, prostate cancer, leukemia, etc. EZH2-IN-9 has the potential for the research of cancer diseases (extracted from patent WO2021180235A1, compound 17).
  • HY-143616
    EZH2-IN-7

    Histone Methyltransferase Cancer
    EZH2-IN-7 is a potent inhibitor of EZH2. EZH2 overexpression or mutations in the SET region (Y641F, Y641N, A687V, A677G point mutations) all lead to abnormal elevation of H3K27me3 and promote the growth and development of many types of tumors, such as breast cancer, prostate cancer, leukemia, etc. EZH2-IN-7 has the potential for the research of cancer diseases (extracted from patent WO2021129629A1, compound 259).
  • HY-142743
    Y08175

    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-13702
    Nilutamide

    Nilandron; RU 23908

    Androgen Receptor Parasite Cancer Infection Endocrinology
    Nilutamide (Nilandron) is an orally active nonsteroidal androgen receptor antagonist with affinity for androgen receptors but not for progestogen, estrogen or glucocorticoid receptors. Nilutamide can be used to research prostate cancer. Nilutamide also has antischistosomal properties.
  • HY-122605
    TRPM4-IN-1

    CBA

    TRP Channel Cancer Cardiovascular Disease
    TRPM4-IN-1 (CBA) is a potent and selective inhibitor of the cation channel TRPM4, with an IC50 of 1.5 μM. TRPM4-IN-1 can be used for the research of cardiac diseases and prostate cancer.
  • HY-145709
    Ar-V7-IN-1

    Androgen Receptor Cancer
    Ar-V7-IN-1 is a potent inhibitor of Ar-V7. AR-V7 is a hormone-independent splice variant of the androgen receptor. Ar-V7-IN-1 has the potential for the research of various indications, in particular cancers such as prostate cancer (extracted from patent WO2018114781A1, compound 43).
  • HY-17423E
    Abacavir hydrochloride

    HIV Apoptosis Reverse Transcriptase Telomerase Cancer Infection
    Abacavir hydrochloride is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir hydrochloride can inhibits the replication of HIV. Abacavir hydrochloride shows anticancer activity in prostate cancer cell lines. Abacavir hydrochloride can trespass the blood-brain-barrier and suppresses telomerase activity.
  • HY-17423
    Abacavir

    HIV Reverse Transcriptase Telomerase Apoptosis Cancer Infection
    Abacavir is an orally active and competitive nucleoside reverse transcriptase inhibitor. Abacavir can inhibits the replication of HIV. Abacavir shows anticancer activity in prostate cancer cell lines. Abacavir can trespass the blood-brain-barrier and suppresses telomerase activity.
  • HY-146433
    Anticancer agent 55

    Apoptosis Cancer
    Anticancer agent 55 is a potent anticancer agent. Anticancer agent 55 shows anticancer activity via reducing the cell viability and cell migration in a dose-dependent manner. Anticancer agent 55 induces apoptosis. Anticancer agent 55 has the potential for the research of prostate cancer and breast cancer.
  • HY-P3229
    SN52

    NF-κB Cancer
    SN52 is a potent, competitive, and cell-permeable inhibitor of NF-κB2. SN52 is a variant of the SN50 peptide and inhibits the nuclear translocation of p52-RelB heterodimers. SN52 has a strong radiosensitization effect on prostate cancer cells. SN52 can be used for cancer research.
  • HY-19527
    IST5-002

    N6-Benzyladenosine-5'-phosphate

    STAT Apoptosis Cancer
    IST5-002, a potent Stat5a/b inhibitor, selectively inhibits transcriptional activity of Stat5a/b (IC50s: 1.5 μM for Stat5a, 3.5 μM for Stat5b). IST5-002 inducs cell apoptotic and death of prostate cancer cells and chronic myeloid leukemia (CML) cells. IST5-002 can be used in the research of prostate cancer and chronic myeloid leukemia (CML).
  • HY-17423B
    Abacavir monosulfate

    HIV Reverse Transcriptase Telomerase Apoptosis Cancer Infection
    Abacavir monosulfate is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir monosulfate can inhibits the replication of HIV. Abacavir monosulfate shows anticancer activity in prostate cancer cell lines. Abacavir monosulfate can trespass the blood-brain-barrier and suppresses telomerase activity.
  • HY-114402
    ARD-69

    Androgen Receptor PROTACs Cancer
    ARD-69 (compound 34) is a potent PROTAC androgen receptor degrader. ARD-69 induces degradation of androgen receptor (AR) protein in AR-positive prostate cancer cell lines. ARD-69 suppresses AR-regulated gene expression.
  • HY-138555
    PROTAC BRD4 Degrader-8

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD4 Degrader-8 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells.
  • HY-138634
    PROTAC BRD4 Degrader-11

    PROTACs Epigenetic Reader Domain ADC Cytotoxin Cancer
    PROTAC BRD4 Degrader-11 (compound 9a) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-11 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 0.23 nM and 0.38 nM, respectively.
  • HY-138637
    PROTAC BRD4 Degrader-14

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD4 Degrader-14 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 1.8 nM and 1.7 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-14 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells.
  • HY-138633
    PROTAC BRD4 Degrader-10

    PROTACs Epigenetic Reader Domain ADC Cytotoxin Cancer
    PROTAC BRD4 Degrader-10 (compound 8b) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-10 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 1.3 nM and 18 nM, respectively.
  • HY-B1150
    Clofoctol

    Bacterial SARS-CoV Antibiotic Cancer Infection
    Clofoctol is a bacteriostatic antibiotic. Clofoctol is used in the treatment of respiratory tract and ear, nose and throat infections caused by Gram-positive bacteria. Clofoctol is only functional against Gram-positive bacteria and can penetrate into human lung tissue. Clofoctol is also an inhibitor of prostate cancer. Clofoctol has antiviral potency.
  • HY-17423A
    Abacavir sulfate

    Abacavir Hemisulfate; ABC sulfate

    Reverse Transcriptase HIV Telomerase Apoptosis Infection
    Abacavir sulfate (Abacavir Hemisulfate) is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir sulfate can inhibits the replication of HIV. Abacavir sulfate shows anticancer activity in prostate cancer cell lines. Abacavir sulfate can trespass the blood-brain-barrier and suppresses telomerase activity.
  • HY-N10578
    Genkwadaphnin

    Others Cancer
    Genkwadaphnin is a daphnane diterpenoid, targeting of importin-β1 to reduce the nuclear accumulation of key CRPC drivers, and shut down their downstream oncogenic signaling. Genkwadaphnin shows potent anti-tumor activity and inhibits castration-resistant prostate cancer (CRPC) in vivo in mice.
  • HY-146494
    Androgen receptor antagonist 5

    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-P0056
    Histrelin

    GnRH Receptor Cancer
    Histrelin, a GnRH analogue, is a GnRH Receptor agonist. Histrelin increases serum luteinising hormone (LH), follicle stimulating hormone (FSH) and testosterone levels. Histrelin can be used in the research of prostate cancer, endometriosis.
  • HY-110127
    NU9056

    Histone Acetyltransferase Apoptosis Cancer
    NU9056 is a potent and selective Tip60 (KAT5) histone acetyltransferase inhibitor with an of 2 µM. NU9056 shows >16-fold selectivity for Tip60 over PCAF, p300 and GCN5. NU9056 induces apoptosis of prostate cancer cells.
  • HY-146170
    Anticancer agent 69

    Reactive Oxygen Species EGFR Apoptosis Cancer
    Anticancer agent 69 (Compound 34), a potent and selective anticancer agent , potently and selectively inhibits human prostate cancer cell line PC3 (IC50=26 nM). Anticancer agent 69 increases ROS level, down-regulates EGFR and induces apoptosis.
  • HY-13627
    Estramustine phosphate sodium

    Microtubule/Tubulin Apoptosis Cancer Endocrinology Inflammation/Immunology
    Estramustine phosphate sodium, an estradiol analog, is an orally active antimicrotubule chemotherapy agent. Estramustine phosphate sodium depolymerises microtubules by binding to microtubule associated proteins (MAPs) and/or to tubulin. Estramustine phosphate sodium can interfere mitosis, trigger cell death and induce apoptosis, which can be used for the research of cancer like prostate cancer.
  • HY-13627A
    Estramustine phosphate

    Apoptosis Microtubule/Tubulin Cancer Endocrinology Inflammation/Immunology
    Estramustine phosphate, an estradiol analog, is an orally active antimicrotubule chemotherapy agent. Estramustine phosphate depolymerises microtubules by binding to microtubule associated proteins (MAPs) and/or to tubulin. Estramustine phosphate can interfere mitosis, trigger cell death and induce apoptosis, which can be used for the research of cancer like prostate cancer.
  • HY-100886
    BAY1082439

    PI3K Apoptosis Cancer
    BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth.
  • HY-139294
    PROTAC BRD4 Degrader-15

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD4 Degrader-15 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 7.2 nM and 8.1 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-15 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells.
  • HY-139180
    PRGL493

    Others Cancer
    PRGL493 is a potent and selective long-chain acyl-CoA synthetase 4 (ACSL4) inhibitor. PRGL493 blocks cell proliferation and tumor growth in both breast and prostate cellular and animal models. PRGL493 is used for cancer research.
  • HY-P1416
    Foxy-5

    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-N0551
    Wedelolactone

    Caspase Lipoxygenase Apoptosis Cancer Inflammation/Immunology
    Wedelolactone suppresses LPS-induced caspase-11 expression by directly inhibits the IKK Complex. Wedelolactone also inhibits 5-lipoxygenase (5-Lox) with an IC50 of 2.5 μM. Wedelolactone induces caspase-dependent apoptosis in prostate cancer cells via downregulation of PKCε without inhibiting Akt. Wedelolactone can extract from Eclipta alba, and it can be used for the research of cancer.
  • HY-138280
    DTHIB

    HSP Cancer
    DTHIB is a direct and selective heat shock factor 1 (HSF1) inhibitor with a Kd of 160 nM for DTHIB binding to the HSF1 DNA binding domain (DBD). DTHIB inhibits HSF1 cancer gene signature (HSF1 CaSig) and selectively stimulates degradation of nuclear HSF1. DTHIB has potently anticancer activities and can be used for prostate cancer research.
  • HY-142772
    Y08284

    Epigenetic Reader Domain Cancer
    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.
  • HY-138635
    PROTAC BRD4 Degrader-12

    PROTACs Epigenetic Reader Domain ADC Cytotoxin Cancer
    PROTAC BRD4 Degrader-12 (compound 9c) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-12 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 0.39 nM and 0.24 nM, respectively.
  • HY-122611A
    CSRM617 hydrochloride

    Androgen Receptor Apoptosis Cancer
    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
  • HY-138636
    PROTAC BRD4 Degrader-13

    PROTACs Epigenetic Reader Domain ADC Cytotoxin Cancer
    PROTAC BRD4 Degrader-13 (compound 9d) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-13 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 0.025 nM and 6.0 nM, respectively.
  • HY-P1416A
    Foxy-5 TFA

    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-151576
    PRMT5:MEP50 PPI

    Others Cancer
    PRMT5:MEP50 PPI is a novel PRMT5:MEP50 protein-protein interaction (PRMT5:MEP50 PPI) inhibitor, shows anti-tumor activity and anti-proliferative activity of lung and prostate cancer cells.
  • HY-143247
    Tubulin polymerization-IN-2

    Microtubule/Tubulin Cancer
    Tubulin polymerization-IN-2 is a potent anticancer agent targeting to β-tubulin with an IC50 value of 0.92 μM. Tubulin polymerization-IN-2 shows promising activity against various leukemia, non-small lung, renal, prostate, and breast cancer cell lines.
  • HY-P99217
    Rilotumumab

    AMG 102

    c-Met/HGFR Cancer
    Rilotumumab (AMG 102) is an anti-HGF (anti-hepatocyte growth factor) monoclonal antibody, inhibits HGF/MET-driven signaling. Rilotumumab shows anti-tumor activity, and can be used in castration-resistant prostate cancer (CRPC) and solid tumor research.
  • HY-138632
    PROTAC BRD4 Degrader-9

    PROTACs Epigenetic Reader Domain ADC Cytotoxin Cancer
    PROTAC BRD4 Degrader-9 (compound 8a) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-9 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 0.86 nM and 7.6 nM, respectively.
  • HY-107640
    WAY-170523

    MMP Cancer
    WAY-170523 is a potent and selective MMP-13 (matrix metalloproteinase-13) inhibitor, with an IC50 of 17 nM. WAY-170523 can directly attenuate ERK1/2 phosphorylation. WAY-170523 inhibits the invasion of PC-3 cells, can be used for prostate cancer research.
  • HY-107408
    SANT 2

    Hedgehog Cancer
    SANT 2 is a potent antagonist of Hh-signaling pathway. Hedgehog (Hh) signaling plays an important role in cell signaling of embryonic development and adult tissue homeostasis. SANT 2 has the potential for the research of several malignancies including Gorlin syndrome (a disorder predisposing to basal cell carcinoma, medulloblastoma and rhabdomyosarcoma), prostate, pancreatic and breast cancers.
  • HY-109070
    Ralaniten

    EPI-002

    Androgen Receptor Cancer
    Ralaniten (EPI-002) is a potent and orally active antagonist of the androgen receptor-N-terminal domain (AR-NTD). Ralaniten inhibits AR transcriptional activity, with IC50 of 7.4 μM. Ralaniten can be used for the research of castration-resistant prostate cancer (CRPC).
  • HY-115282A
    JNJ-63576253

    TRC-253

    Androgen Receptor Cancer
    JNJ-63576253 (TRC-253) is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 can be used for the research of castration-resistant prostate cancer (CRPC).
  • HY-143660
    LG308

    Microtubule/Tubulin Apoptosis Cancer
    LG308 is a novel synthetic compound with antimicrotubule activity. LG308 induces mitotic phase arrest and inhibits G2/M progression significantly which is associated with the upregulation of cyclin B1 and mitotic marker MPM-2 and the dephosphorylation of cdc2. LG308 also induces apoptosis and cell death. LG308 significantly suppresses tumor growth. LG308 with antimitotic activity has the potential for the research of prostate cancer.
  • HY-N0790
    Lupeol

    Clerodol; Monogynol B; Fagarasterol

    Androgen Receptor Apoptosis Cancer
    Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent androgen receptor (AR) inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC).
  • HY-P2161B
    TAK-683 acetate

    Kisspeptin Receptor Cancer
    TAK-683 acetate is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively. TAK-683 acetate depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer.
  • HY-P2161A
    TAK-683 TFA

    Kisspeptin Receptor Cancer
    TAK-683 TFA is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 TFA is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively. TAK-683 TFA depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer.
  • HY-P2161
    TAK-683

    Kisspeptin Receptor Cancer
    TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively. TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer.
  • HY-151247
    GnRH-R antagonist 1

    GnRH Receptor Cancer
    GnRH-R antagonist 1 (compound 21a) is an orally safe and membrane-permeable GnRH-R antagonist with high binding affinity (IC50=0.57 nM) and potent in vitro antagonistic activity (IC50=2.18 nM). GnRH-R antagonist 1 can be used in studies of advanced prostate cancer and premature LH peaks preventing.
  • HY-115747
    Namoline

    Histone Demethylase Cancer
    Namoline, a γ-pyrone, is a selective and reversible Lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 51 μM in a HRP-coupled enzymatic assay. Namoline impairs LSD1 demethylase activity and blocks cell proliferation. Namoline has the potential for androgen-dependent prostate cancer research.
  • HY-113289
    Brassicasterol

    Androgen Receptor HSV Bacterial Drug Metabolite Cancer Infection
    Brassicasterol, a metabolite of Ergosterol, plays a role in the inhibitory effect on bladder carcinogenesis promotion via androgen signaling. Brassicasterol shows dual anti-infective properties against HSV-1 (IC50=1.2 µM) and Mycobacterium tuberculosis, and cardiovascular protective effect. Brassicasterol exerts an anti-cancer effect by dual-targeting AKT and androgen receptor signaling in prostate cancer.
  • HY-115282
    JNJ-63576253 free base

    TRC-253 free base

    Androgen Receptor Cancer
    JNJ-63576253 (TRC-253) free base is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 free base can be used for the research of castration-resistant prostate cancer (CRPC).
  • HY-122678
    LQZ-7F

    Survivin Apoptosis Cancer
    LQZ-7F, a survivin dimerization inhibitor, induces spontaneous apoptosis and synergizes with Docetaxel in prostate cancer cells. LQZ-7F dose-dependently inhibits survival of both PC-3 and C4-2 cells with IC50s of 2.99 and 2.47 µM, respectively.
  • HY-138557
    AKR1C3-IN-4

    Others Cancer
    AKR1C3-IN-4 is a potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitor with an IC50 of 0.56 μM. AKR1C3-IN-4 has the potential for castrate resistant prostate cancer (CRPC) research.
  • HY-12830
    M-110

    Pim Cancer
    M-110 is a highly selective, ATP-competitive inhibitor of PIM kinases with a preference for PIM-3 (IC50=47 nM). M-110 inhibits PIM-1 and PIM-2 with similar IC50s of 2.5 μM. M-110 inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 μM.
  • HY-144755
    MC2652

    Histone Demethylase Cancer
    MC2652 (compound 1a) is a potent LSD1 inhibitor. MC2652 displays high inhibiting effects in MV4-11 and NB4 leukaemia cells. MC2652 shows antiproliferative activity against prostate cancer LNCaP cells.
  • HY-124628
    IPI-9119

    Fatty Acid Synthase (FASN) Cancer
    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.
  • HY-111614
    Melengestrol acetate

    Progesterone Receptor Cancer Metabolic Disease
    Melengestrol acetate is a progesterone derivative, acts as an orally active corticosteroid hormone to promote endometrial proliferation, pregnancy maintenance, and delay of menstrual activity. Melengestrol Acetate is used as a contraceptive agent for growth promoting effects and suppression of estrus in animals. Melengestrol acetate inhibits both the androgen-dependent and -independent prostatic tumors in vivo and can be used for cancer research.
  • HY-17473
    Embelin

    Embelic acid; Emberine; NSC 91874

    IAP NF-κB Apoptosis Autophagy Cancer
    Embelin (Embelic acid), a potent, nonpeptidic XIAP inhibitor (IC50=4.1 μM), inhibits cell growth, induces apoptosis, and activates caspase-9 in prostate cancer cells with high levels of XIAP. Embelin blocks NF-kappaB signaling pathway leading to suppression of NF-kappaB-regulated antiapoptotic and metastatic gene products. Embelin also induces autophagic and apoptotic cell death in human oral squamous cell carcinoma cells.
  • HY-111784
    Inobrodib

    CCS1477

    Epigenetic Reader Domain Cancer
    Inobrodib (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain. Inobrodib binds to p300 and CBP with Kd values of 1.3 and 1.7 nM, respectively, and with 170/130-fold selectivity compared with BRD4 with a Kd of 222 nM. CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression.
  • HY-121524
    DJ101

    Microtubule/Tubulin Cancer
    DJ101 is a potent and metabolically stable tubulin inhibitor. DJ101 targets the colchicine binding site and overcomes taxane resistance. DJ101 also inhibits melanoma tumor growth and lung metastasis. DJ101 can be used for prostate cancer research.
  • HY-16993
    OICR-9429

    Histone Methyltransferase Apoptosis Cancer
    OICR-9429 is high affinity WD repeat domain 5 (WDR5) inhibitor, competitively blocks WDR5 interaction with MLL protein via binding the central peptide-binding pocket of WDR5. OICR-9429 can suppress histone H3K4 trimethylation and can be used for the research of various cancers including non-MLL-rearranged leukaemia, colon, pancreatic, prostate cancer and bladder cancer (BCa) .
  • HY-10617D
    Rucaparib acetate

    AG014699 acetate; PF-01367338 acetate

    PARP Cancer
    Rucaparib (AG014699) acetate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib acetate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib acetate has the potential for castration-resistant prostate cancer (CRPC) research.
  • HY-10617B
    Rucaparib hydrochloride

    AG014699 hydrochloride; PF-01367338 hydrochloride

    PARP Cancer
    Rucaparib (AG014699) hydrochloride is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib hydrochloride is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib hydrochloride has the potential for castration-resistant prostate cancer (CRPC) research.
  • HY-144636
    Atg4B-IN-2

    Cathepsin Phospholipase Autophagy Cancer
    Atg4B-IN-2 is a potent competitive Atg4B inhibitor with Ki value of 3.1 μM, also possesses declining PLA2 inhibitory potency, IC50s of 11 μM and 3.5 μM for Atg4B and PLA2, respectively. Atg4B-IN-2 enhances the anticancer activity of anti-castration-resistant prostate cancer drugs via autophagy inhibition.
  • HY-144060
    AKT-IN-10

    Akt Cancer
    AKT-IN-10 is a potent inhibitor of AKT. Protein kinase B (PKB, also known as AKT) is central to PI3K/AKT/mTOR signaling in cells, and its function is important for cell growth, survival, differentiation and metabolism. AKT-IN-10 has the potential for the research of breast and prostate cancer (extracted from patent WO2021185238A1, compound 4).
  • HY-147854
    B-Raf IN 9

    Raf Apoptosis Cancer
    B-Raf IN 9 (compound 8b) is a potent B-Raf inhibitor, with an IC50 of 24.79 nM. B-Raf IN 9 induces apoptosis and shows cell cycle arrest at G2/M phase. B-Raf IN 9 exhibits potent antitumor activity against human prostate cancer PC-3 cell line, with an IC50 of 7.83 µM.
  • HY-10617C
    Rucaparib tartrate

    AG-014699 tartrate; PF-01367338 tartrate

    PARP Cancer
    Rucaparib (AG014699) tartrate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib tartrate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib tartrate has the potential for castration-resistant prostate cancer (CRPC) research.
  • HY-144059
    AKT-IN-9

    Akt Cancer
    AKT-IN-9 is a potent inhibitor of AKT. Protein kinase B (PKB, also known as AKT) is central to PI3K/AKT/mTOR signaling in cells, and its function is important for cell growth, survival, differentiation and metabolism. AKT-IN-9 has the potential for the research of breast and prostate cancer (extracted from patent WO2021185238A1, compound 1).
  • HY-16474
    Relugolix

    TAK-385

    GnRH Receptor Cancer Endocrinology
    Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209). Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al.
  • HY-147853
    B-Raf IN 8

    Raf Cancer
    B-Raf IN 8 (compound 7g) is a potent B-Raf inhibitor, with an IC50 of 70.65 nM. B-Raf IN 8 exhibits antitumor activity against hepatocellular carcinoma (HEPG-2), colon carcinoma (HCT-116), mammary gland (MCF-7) and human prostate cancer (PC-3) cells, with IC50 values of 9.78, 13.78, 18.52 and 29.85 µM.
  • HY-143235
    BRD4 Inhibitor-15

    Epigenetic Reader Domain Apoptosis Bcl-2 Family Caspase c-Myc Cancer
    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.
  • HY-130709
    PROTAC CDK2/9 Degrader-1

    PROTACs CDK Cancer
    PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC50=62 nM) and CDK9 (DC50=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC50=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with Cereblon ligand.
  • HY-B1012
    Quinestrol

    W-3566

    Estrogen Receptor/ERR Endocrinology Cancer
    Quinestrol is a synthetic estrogen, used in hormone replacement therapy, and occasionally to treat breast cancer and prostate cancer
  • HY-136242
    UT-34

    Androgen Receptor Cancer Endocrinology
    UT-34 is a potent, selective and orally active second-generation pan-androgen receptor (AR) antagonist and degrader with IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively. UT-34 binds to ligand-binding domain (LBD) and function-1 (AF-1) domains and requires ubiquitin proteasome pathway to degrade the AR. UT-34 has anti-prostate cancer efficacy.
  • HY-U00091
    Gestonorone Capronate

    Gestonorone caproate

    Progesterone Receptor Cancer
    Gestonorone Capronate is a progestin for the treatment of benign prostatic hypertrophy and endometrial cancer.
  • HY-N0058
    4,5-Dicaffeoylquinic acid

    Isochlorogenic acid C

    HBV Endogenous Metabolite Apoptosis Glucosidase Infection
    4,5-Dicaffeoylquinic acid (Isochlorogenic acid C) is an antioxidant, can be isolated from Gynura divaricata and Laggera alata. 4,5-Dicaffeoylquinic acid reduces islet cell apoptosis and improves pancreatic function in type 2 diabetic mice, and has obvious inhibitory activities against yeast α-glucosidase. 4,5-Dicaffeoylquinic acid inhibits prostate cancer cells through cell cycle arrest. 4,5-Dicaffeoylquinic acid also has anti-apoptotic, anti-injury and anti-hepatitis B virus effects.
  • HY-103591
    DUPA(OtBu)-OH

    Others Cancer
    DUPA(OtBu)-OH is a DUPA precursor. DUPA is used as the targeting moiety to actively deliver Docetaxel (DTX) for treatment of Prostate-Specific Membrane Antigen (PSMA) expressing prostate cancer.
  • HY-147852
    B-Raf IN 7

    Raf Cancer
    B-Raf IN 7 (compound 6a) is a potent B-Raf inhibitor, with an IC50 of 110.23 nM. B-Raf IN 7 exhibits antitumor activity against colon carcinoma (HCT-116), mammary gland (MCF-7), hepatocellular carcinoma (HEPG-2), human cervical carcinoma (Hela) and human prostate cancer (PC-3) cells, with IC50 values of 7.50, 9.87, 10.57, 11.63 and 12.83 µM.
  • HY-146393
    PROTAC CYP1B1 degrader-1

    PROTACs Cytochrome P450 Cancer
    PROTAC CYP1B1 degrader-1 (Compound 6C), a α-naphthoflavone chimera derivative, is able to eliminate cytochrome P450 (CYP)1B1-mediated drug resistance via targeted CYP1B1 degradation, with IC50s of 95.1 and 9838.6 nM for CYP1B1 and CYP1A2, respectively. PROTAC CYP1B1 degrader-1 can be used for the research of CYP1B1-overexpressing prostate cancer.
  • HY-137448
    Rezvilutamide

    SHR3680

    Androgen Receptor Cancer
    Rezvilutamide (SHR3680) is an androgen receptor antagonist. Rezvilutamide (SHR3680) is used for the study of prostate cancer.
  • HY-N0288
    Lycorine

    Fatty Acid Synthase (FASN) Virus Protease Bacterial Apoptosis Cancer Inflammation/Immunology
    Lycorine is a natural alkaloid extracted from the Amaryllidaceae plant. Lycorine is a potent and orally active SCAP inhibitor with a Kd value 15.24 nM. Lycorine downregulates the SCAP protein level without changing its transcription. Lycorine is also a melanoma vasculogenic inhibitor. Lycorine can be used for the study of prostate cancer and metabolic diseases.
  • HY-144758
    LSD1-IN-17

    Histone Demethylase Monoamine Oxidase Cancer
    LSD1-IN-17 (compound 5b) is a potent LSD1 inhibitor. LSD1-IN-17 can inhibit LSD1-CoREST, MAO-A and MAO-B, with IC50 values of 0.005, 0.028, and 0.820 μM, respectively. LSD1-IN-17 displays cell growth arrest in prostate cancer LNCaP cells, with an IC50 of 17.2 μM.
  • HY-144756
    LSD1-IN-15

    Histone Demethylase Monoamine Oxidase Cancer
    LSD1-IN-15 (compound 1b) is a potent LSD1 inhibitor. LSD1-IN-15 can inhibit LSD1-CoREST, MAO-A and MAO-B, with IC50 values of 0.149, 0.028, and 0.327 μM, respectively. LSD1-IN-15 displays cell growth arrest in prostate cancer LNCaP cells, with an IC50 of 9.9 μM.
  • HY-144757
    LSD1-IN-16

    Histone Demethylase Monoamine Oxidase Cancer
    LSD1-IN-16 (compound 4b) is a potent LSD1 inhibitor. LSD1-IN-16 can inhibit LSD1-CoREST, MAO-A and MAO-B, with IC50 values of 0.015, 0.024, and 0.366 μM, respectively. LSD1-IN-16 displays cell growth arrest in prostate cancer LNCaP cells, with an IC50 of 15.2 μM.
  • HY-128938
    EC1167

    ADC Linker Cancer
    EC1167 is the linker for EC1169. EC1169 is prostate-specific membrane antigen targeting-tubulysin conjugate. EC1169 has the potential to treat recurrent metastatic, castration-resistant prostate cancer (MCRPC).
  • HY-128938A
    EC1167 hydrochloride

    ADC Linker Cancer
    EC1167 hydrochloride is the linker for EC1169. EC1169 is prostate-specific membrane antigen targeting-tubulysin conjugate. EC1169 hydrochloride has the potential to treat recurrent metastatic, castration-resistant prostate cancer (MCRPC).
  • HY-139623
    A4B17

    Androgen Receptor Cancer
    A4B17 is an androgen receptor N-terminal inhibitor for treating androgen-responsive prostate cancer.
  • HY-120599
    Sabizabulin

    VERU-111; ABI-231

    Microtubule/Tubulin Apoptosis HPV Cancer
    VERU-111 (ABI-231) is a potent and orally active α and β tubulin inhibitor, which displays strong antiproliferative activity, with an average IC50 of 5.2 nM against panels of melanoma and prostate cancer cell lines. VERU-111 (ABI-231) suppresses tumor growth and metastatic phenotypes of cervical cancer cells via targeting HPV E6 and E7, and has potential for the treatment of prostate cancer.
  • HY-13534
    Abarelix

    R3827; PPI 149

    GnRH Receptor Cancer Endocrinology
    Abarelix (R3827; PPI 149) is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer treatment.
  • HY-143535
    HG122

    Androgen Receptor Cancer
    HG122 promotes androgen receptor (AR) degradation through the proteasome pathway inhibiting the castration-resistant prostate cancer.
  • HY-78884
    Anticancer agent 9

    Others Cancer
    Anticancer agent 9, a glycine derivative, is an anticancer agent. Anticancer agent 9 can inhibit tumor cells viability of myelogenous leukemia and human prostate cancer.
  • HY-B0022
    Flutamide

    SCH 13521

    Androgen Receptor Cancer
    Flutamide is an antiandrogen drug, with its active metablolite binding at androgen receptor with Ki values of 55 nM, and primarily used to treat prostate cancer.
  • HY-147100
    α1A-AR Degrader 9c

    PROTACs Adrenergic Receptor Cancer
    α1A-AR Degrader 9c (compound 9c) is a potent, selective and reversible α1A-AR (Adrenergic receptor) PROTAC degrader, with a DC50 of 2.86 μM. α1A-AR Degrader 9c induces α1A-AR degradation can be attributed to proteasomal degradation. α1A-AR Degrader 9c inhibits the proliferation of PC-3 cells, with an IC50 of 6.12 μM. α1A-AR Degrader 9c shows antitumor activity, and can be used for prostate cancer research.
  • HY-14249S
    Bicalutamide-d4

    Androgen Receptor Autophagy Cancer
    Bicalutamide-d4 is the deuterium labeled Bicalutamide. Bicalutamide is an orally active non-steroidal androgen receptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer.
  • HY-114988
    PGE-M

    tetranor-PGEM

    Endogenous Metabolite Cancer Inflammation/Immunology
    PGE-M is a metabolite of prostaglandin E2 (PEG2) as a biomarker of inflammation and cancer including advanced colorectal neoplasia, ovarian cancer, prostate cancer and so on. Urinary PGE-M is positively associated with obesity, smoking and lung metastases with breast cancer.
  • HY-13534A
    Abarelix Acetate

    PPI 149 Acetate; R 3827 Acetate

    GnRH Receptor Cancer Endocrinology
    Abarelix Acetate (PPI 149 Acetate; R 3827 Acetate) is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer research.
  • HY-141860
    PSMA-Val-Cit-PAB-MMAE

    Drug-Linker Conjugates for ADC Cancer
    PSMA-Val-Cit-PAB-MMAE is a novel small-molecule PSMA-targeted conjugate based on the monomethyl auristatin E for the chemotherapy of prostate cancer.
  • HY-15194
    Dimethylcurcumin

    ASC-J9; GO-Y025

    Androgen Receptor Cancer
    Dimethylcurcumin (ASC-J9) is an androgen receptor degradation enhancer that effectively suppresses castration resistant prostate cancer cell proliferation and invasion.
  • HY-N0610A
    Cinnamic acid

    3-Phenylacrylic acid; β-Phenylacrylic acid

    Endogenous Metabolite Cancer
    Cinnamic acid has potential use in cancer intervention, with IC50s of 1-4.5 mM in glioblastoma, melanoma, prostate and lung carcinoma cells.
  • HY-70006
    Galeterone

    TOK-001; VN-124-1

    Cytochrome P450 Cancer
    Galeterone (TOK-001) is a multifunctional antiandrogen and CYP17 inhibitor (IC50=47 nM) in castration resistant prostate cancer (CRPC).
  • HY-16187
    EL-102

    HIF/HIF Prolyl-Hydroxylase Apoptosis Cancer
    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.
  • HY-125170
    Galiellalactone

    STAT Cancer
    Galiellalactone is a is a small non-toxic and non-mutagenic fungal metabolite, a selective inhibitor of STAT3 signaling, with an IC50 of 250-500 nM. Galiellalactone can be used to research castration-resistant prostate cancer.
  • HY-139893
    ERGi-USU-6 mesylate

    Others Cancer
    ERGi-USU-6 (mesylate) is an ERGi-USU-6 salt derivative that is a new selective inhibitor of ERG positive prostate cancer ( IC50 = 0.089 μM).
  • HY-111606
    DUPA

    Ligands for Target Protein for PROTAC Cancer
    DUPA, belongs to a class of glutamate ureas, is used as the targeting moiety in drug conjugate to selectively deliver cytotoxic drugs to prostate cancer cells.
  • HY-15694
    SMIP004

    E1/E2/E3 Enzyme Apoptosis Cancer
    SMIP004 is a SKP2 E3 ligase inhibitor, which downregulates SKP2 and to stabilise p27. SMIP004 is a cancer cell selective apoptosis inducer of human prostate cancer cells.
  • HY-19960
    BCTC

    TRP Channel Cancer
    BCTC is a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells.
  • HY-N3755
    Dihydroresveratrol

    Estrogen Receptor/ERR Cancer
    Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator. Dihydroresveratrol exhibits proliferative effects in androgen-independent prostate and breast cancer cells at picomolar and nanomolar concentrations.
  • HY-111145
    RD162

    Androgen Receptor Cancer
    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.
  • HY-132896
    KDM4-IN-3

    Histone Demethylase Cancer
    KDM4-IN-3 is a KDM4 inhibitor that exhibits improved potency in biochemical assays, is cell-permeable, and kills prostate cancer cells at low micromolar concentrations.
  • HY-103687
    Abiraterone metabolite 1

    3β-OH-5α-Abi

    Drug Metabolite Cancer
    Abiraterone metabolite 1 is a 5β-reduced metabolite of abiraterone. Abiraterone, a steroidal drug, inhibits CYP17A1, blocks androgen synthesis and prolongs survival in prostate cancer.
  • HY-111503
    Y06137

    Epigenetic Reader Domain Cancer
    Y06137 is a potent and selective BET inhibitor for treatment of castration-resistant prostate cancer (CRPC). Y06137 binds to the BRD4(1) bromodomain with a Kd of 81 nM.
  • HY-144667
    ALDH1A3-IN-1

    Aldehyde Dehydrogenase (ALDH) Cancer
    ALDH1A3-IN-1 (Compound 14) is a potent ALDH1A3 inhibitor, with an IC50 of 0.63 µM and a Ki of 0.46 µM. ALDH1A3-IN-1 can be studied in prostate cancer.
  • HY-108250S
    (R)-Bicalutamide-d4

    Androgen Receptor Cancer
    (R)-Bicalutamide-d4 is the deuterium labeled (R)-Bicalutamide. (R)-Bicalutamide is the (R)-enantiomer of Bicalutamide (HY-14249). (R)-Bicalutamide is an androgen receptor (AR) antagonist, with antineoplastic activity. (R)-Bicalutamide is widely used for the research of prostate cancer.
  • HY-103385
    NCX4040

    NO-Aspirin

    Apoptosis Cancer Inflammation/Immunology
    NCX4040 (NO-Aspirin), a non-steroidal anti-inflammatory drug (NSAID), is a nitric oxide (NO) releasing form of Aspirin. NCX4040 induces apoptosis in PC3 metastatic prostate cancer cells. NCX4040 has anti-inflammatory and anti-cancer effects.
  • HY-101017
    Palmitoylcarnitine chloride

    Endogenous Metabolite Cancer Inflammation/Immunology
    Palmitoylcarnitine chloride is a fatty acid-derived mitochondrial substrate, and selectively decreases cell survival in colorectal and prostate cancer cells by affecting on pro-inflammatory pathways, Ca 2+ influx, and DHT-like effects.
  • HY-32345
    Elocalcitol

    BXL-628; Ro-26-9228

    VD/VDR Cancer Inflammation/Immunology
    Elocalcitol (BXL-628) is a selective, orally active vitamin D receptor (VDR) agonist. Elocalcitol shows anti-inflammatory activity. Elocalcitol inhibits growth of prostate cancer cells.
  • HY-12364
    C75

    Fatty Acid Synthase (FASN) Cancer
    C75 is a synthetic fatty-acid synthase (FASN) inhibitor; inhibits prostate cancer cells PC3 with an IC50 of 35 μM. C75 is a potent CPT1A activator.
  • HY-139453
    LP-184

    Others Cancer
    LP-184 (compound 6), an acylfulvene analog, inhibits tumor growth. LP-184 has potent anti-cancer activity in the ovarian, colon, prostate and pancreatic cell lines. (patent WO2007019308A2).
  • HY-109564
    5α-Pregnane-3β,6α-diol-20-one

    Others Cancer
    5α-Pregnane-3β,6α-diol-20-one is a mitogenic metabolite of progesterone, and it can be produced in starved androgen-responsive prostate cancer cells.
  • HY-N7043
    Isosilybin A

    Apoptosis Cancer
    Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis.
  • HY-13215
    Avasimibe

    CI-1011; PD-148515

    Acyltransferase Cancer
    Avasimibe (CI-1011; PD-148515) is an orally active acyl coenzyme A-cholesterol acyltransferase (ACAT; also called SOAT)) inhibitor with IC50s of 24 and 9.2 µM for ACAT1 and ACAT2, respectively. Avasimibe can be used for the research of prostate cancer.
  • HY-15214A
    CARM1-IN-3 dihydrochloride

    Histone Methyltransferase Cancer
    CARM1-IN-3 dihydrochloride (compound 17b) is a potent and selective co-activator associated arginine methyltransferase (CARM1) inhibitor with IC50 values of 0.07, >25 µM for CARM1 and CARM3, respectively.
  • HY-111237
    Butyrolactone I

    Olomoucin

    CDK Cancer
    Butyrolactone I is an ATP-competitive inhibitor of CDK1 as a secondary metabolite from A. terreus. Butyrolactone I has antitumor effects in non-small cell lung, small cell lung, and prostate cancer cell lines.
  • HY-N7045
    Isosilybin B

    Androgen Receptor Apoptosis Cancer
    Isosilybin B, a flavonolignan isolated from Silybum marianum, has anti-prostate cancer (PCA) activity via inhibiting proliferation and inducing G1 phase arrest and apoptosis. Isosilybin B causes androgen receptor (AR) degradation.
  • HY-10088
    Zibotentan

    ZD4054

    Endothelin Receptor Apoptosis Cancer Endocrinology
    Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research.
  • HY-136938
    NEO2734

    EP31670

    Epigenetic Reader Domain Histone Acetyltransferase Cancer
    NEO2734 (EP31670) is an orally active dual p300/CBP and BET bromodomain selective inhibitor, with IC50 values of <30 nM for both p300/CBP and BET bromodomains. NEO2734 is active in SPOP mutant and wild-type prostate cancer.
  • HY-110066
    (Z)-Guggulsterone

    Apoptosis VEGFR Akt Cancer
    Z-guggulsterone, a constituent of Indian Ayurvedic medicinal plant Commiphora mukul, inhibits the growth of human prostate cancer cells by causing apoptosis. Z-guggulsterone inhibits angiogenesis by suppressing the VEGF–VEGF-R2–Akt signaling axis.
  • HY-N0610AS
    Cinnamic acid-d6

    3-Phenylacrylic acid-d6; β-Phenylacrylic acid-d6

    Endogenous Metabolite Cancer
    Cinnamic acid-d6 (3-Phenylacrylic acid-d6) is the deuterium labeled Cinnamic acid. Cinnamic acid has potential use in cancer intervention, with IC50s of 1-4.5 mM in glioblastoma, melanoma, prostate and lung carcinoma cells.
  • HY-10528
    Tasquinimod

    ABR-215050

    HDAC Cancer
    Tasquinimod is an oral antiangiogenic agent, which has the potential for castration-resistant prostate cancer treatment. Tasquinimod binds to the regulatory Zn 2+ binding domain of HDAC4 with Kd of 10-30 nM. Tasquinimod also is a S100A9 inhibitor.
  • HY-50901
    ONO-AE3-208

    AE 3-208

    Prostaglandin Receptor Cancer Endocrinology
    ONO-AE3-208 is a selective and orally active EP4 receptor antagonist with a Ki of 1.3 nM. ONO-AE3-208 shows less potently affects EP3, FP, and TP receptors (Ki of 30 nM, 790 nM, and 2400 nM, respectively). ONO-AE3-208 suppresses cell invasion, migration, and metastasis of prostate cancer.
  • HY-N0103A
    Sophocarpine monohydrate

    Autophagy Apoptosis PI3K Akt Influenza Virus Cancer Infection Inflammation/Immunology
    Sophocarpine (monohydrate) is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine (monohydrate) significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine (monohydrate) has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer.
  • HY-N0103
    Sophocarpine

    Autophagy Apoptosis PI3K Akt Influenza Virus Cancer Infection Inflammation/Immunology
    Sophocarpine is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer.
  • HY-129746
    Arylquin 1

    Apoptosis Cancer
    Arylquin 1, a prostate-apoptosis-response-4 (Par-4) secretagogue, targets vimentin to induce Par-4 secretion. Arylquin 1 induces non-apoptotic cell death in cancer cells through the induction of lysosomal membrane permeabilization (LMP).
  • HY-111024
    2,2,5,7,8-Pentamethyl-6-Chromanol

    PMC

    Androgen Receptor Cancer
    2,2,5,7,8-Pentamethyl-6-Chromanol (PMC) is the anti-oxidant moiety of vitamin E (α-tocopherol). 2,2,5,7,8-Pentamethyl-6-Chromanol has potent androgen receptor (AR) signaling modulation and anti-cancer activity against prostate cancer cell lines.
  • HY-146574
    AKR1C3-IN-7

    Others 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-146575
    AKR1C3-IN-8

    Others 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-146573
    AKR1C3-IN-6

    Others 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-N0819
    Raddeanin A

    Apoptosis Cancer
    Raddeanin A is a natural triterpenoid saponin component of Anemone raddeana, with anti-cancer activities. Raddeanin A exerts anticancer effect on human osteosarcoma via the ROS/JNK and NF-κB signal pathway.
  • HY-141524
    RMC-3943

    SHP2 Phosphatase Cancer
    RMC-3943 is an allosteric SHP2 inhibitor (inhibition of full-length SHP2 in biochemical assay, IC50 = 2.19 nM).
  • HY-109050
    Alobresib

    GS-5829

    Epigenetic Reader Domain Cancer
    Alobresib (GS-5829) is a BET bromodomain inhibitor, which represents a highly effective therapeutics agent against recurrent/chemotherapy resistant uterine serous carcinoma (USC) overexpressing c-Myc. Alobresib can be used in the metastatic castration-resistant prostate cancer (mCRPC) research.
  • HY-19702
    PKR-IN-2

    Pyruvate Kinase Cancer Metabolic Disease Inflammation/Immunology
    PKR-IN-2 is a pyruvate kinase isoform PKR activator extracted from patent WO2014139144A1, compound 160. PKR-IN-2 can be used for the research of PKR function related diseases, including cancer, diabetes, obesity, autoimmune disorders, and benign prostatic hyperplasia.
  • HY-12842
    UC-112

    IAP Apoptosis Cancer
    UC-112 is a novel potent IAP(Inhibitor of apoptosis) inhibitor; potently inhibit cell growth in two human melanoma (A375 and M14) and two human prostate (PC-3 and DU145) cancer cell lines(IC50=0.7-3.4 uM).
  • HY-13721
    Phenoxodiol

    Idronoxil; Dehydroequol; Haginin E

    Caspase Apoptosis Topoisomerase Cancer
    Phenoxodiol (Idronoxil), a synthetic analog of Genestein, activates the mitochondrial caspase system, inhibits XIAP (an apoptosis inhibitor), and sensitizes the cancer cells to Fas-mediated apoptosis. Phenoxodiol also inhibits DNA topoisomerase II by stabilizing the cleavable complex. Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21 WAF1 via a p53 independent manner.
  • HY-100348
    EPI-001

    Androgen Receptor PPAR Apoptosis Cancer
    EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer.
  • HY-139970
    VPC-13789

    Androgen Receptor Cancer Endocrinology
    VPC-13789 is a potent, selective, and orally bioavailable antiandrogen. VPC-13789 can be used for the research of castration-resistant prostate cancer (CRPC) therapeutics. VPC-13789 inhibits androgen receptor (AR) transcriptional activity in LNCaP cells (IC50=0.19 μM).
  • HY-118480
    4-MMPB

    Lipoxygenase Apoptosis Cancer
    4-MMPB is a selective inhibitor of 15-lipoxygenase, with an IC50 of 18 μM. 4-MMPB has IC50s of 19.5 μM and 19.1 μM for soybean 15-lipoxygenase (SLO) and human 15-lipoxygenase-1 (15-LOX-1), respectively. 4-MMPB has potential for the research of prostate cancer.
  • HY-W058849
    MT 63-78

    AMPK mTOR Apoptosis Cancer
    MT 63-78 is a specific and potent direct AMPK activator with an EC50 of 25 μM. MT 63–78 also induces cell mitotic arrest and apoptosis. MT 63-78 blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. MT 63-78 has antitumor effects.
  • HY-124573
    OBI-3424

    TH-3424

    DNA Alkylator/Crosslinker Cancer
    OBI-3424 (TH-3424) is a prodrug that is selectively converted by AKR1C3 (aldo-keto reductase 1C3) to a potent DNA-alkylating agent. OBI-3424 can be used for hepatocellular carcinoma, castrate-resistant prostate cancer, and acute lymphoblastic leukemia (ALL) research.
  • HY-146230
    VEGFR-2-IN-26

    VEGFR Cancer
    VEGFR-2-IN-26 (compound 5h) is a highly potent VEGFR-2 inhibitor with an IC50 value of 15.5 nM. VEGFR-2-IN-26 has good antiproliferative activity against the leukemic, non-small lung, CNS, ovarian, renal, prostate and breast cancer cells.
  • HY-119037
    UK-101

    Proteasome Apoptosis Cancer
    UK-101 is a potent and selective immunoproteasome β1i (LMP2) inhibitor with an IC50 value of 104 nM, displays 144- and 10-fold selectivity over β1c (IC50=15 μM) and β5 subunit (IC50=1 μM), respectivey. UK-101 induces cell apoptosis and can be used for the study of prostate cancer.
  • HY-150102
    EPI-7170

    Androgen Receptor Cancer
    EPI-7170, a ralaniten analogue, is a potent androgen receptor N-terminal structural domain antagonist that blocks the transcriptional activity of full-length AR (FL-AR) and AR splice variants (AR-Vs). EPI-7170 has antitumor effects against enzalutamide resistant castration-resistant prostate cancer (CRPC).
  • HY-N2415
    Podophyllotoxone

    Microtubule/Tubulin Cancer
    Podophyllotoxone is isolated from the roots of Dysosma versipellis and has anti-cancer activities.Podophyllotoxone is able to inhibit the tubulin polymerization.
  • HY-70002S1
    Enzalutamide-d6

    MDV3100-d6

    Androgen Receptor Cancer
    Enzalutamide D3 is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells.
  • HY-43869
    Vipivotide tetraxetan Ligand-Linker Conjugate

    PSMA-617 Ligand-Linker Conjugate

    ADC Linker Cancer
    Vipivotide tetraxetan Ligand-Linker Conjugate (PSMA-617 Ligand-Linker Conjugate) is composed of a linker and Glutamate-urea-Lysine, can be used to synthesize Vipivotide tetraxetan (PSMA-617). Glutamate-urea-Lysine is is the selective pharmacophore to bind to prostate specific membrane antigen (PSMA).
  • HY-122234
    VPC-18005

    Others Cancer
    VPC-18005 inhibits ERG-induced transcription and interacts directly with the ERG-ETS domain, and disrupts the ERG binding to DNA. VPC-18005 is a potent inhibitor of luciferase activity.
  • HY-141487
    CLP-3094

    Androgen Receptor Metabolic Disease Inflammation/Immunology
    CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the androgen receptor (AR). CLP-3094 inhibits AR transcriptional activity (IC50=4 μM). CLP-3094 is a selective, potent GPR142 antagonist.
  • HY-W013249
    Boc-piperazine-benzoic acid

    PROTAC Linkers Cancer
    Boc-piperazine-benzoic acid is a PROTAC linker and can be used in the synthesis of PROTACs, such as PROTAC androgen receptor (AR) degrader ARD-2128 (HY-13229).
  • HY-70002S
    Deutenzalutamide

    Enzalutamide-d3; MDV3100-d3

    Androgen Receptor Autophagy Cancer
    Deutenzalutamide (Enzalutamide-d3) is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells.
  • HY-139436
    ARD-2585

    PROTACs Androgen Receptor Cancer
    ARD-2585 is an exceptionally potent and orally active PROTAC degrader of androgen receptor.
  • HY-133020
    ARD-266

    PROTACs Androgen Receptor Cancer
    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.
  • HY-147261
    B026

    Histone Acetyltransferase Cancer
    B026 is a selective, potent, orally active p300/CBP histone acetyltransferase (HAT) inhibitor with IC50 values of 1.8 nM and 9.5 nM for p300 and CBP enzyme, respectively. B026 has anticancer activity for androgen receptor-positive (AR+) prostate cancer cell lines.
  • HY-114372
    Lycopodine

    Lipoxygenase Caspase Apoptosis Cancer
    Lycopodine, a pharmacologically important bioactive component derived from Lycopodium clavatumspores, triggers apoptosis by modulating 5-lipoxygenase, and depolarizing mitochondrial membrane potential in refractory prostate cancer cells without modulating p53 activity. Lycopodine inhibits proliferation of HeLa cells through induction of apoptosis via caspase-3 activation.
  • HY-10617
    Rucaparib phosphate

    AG-014699 phosphate; PF-01367338 phosphate

    PARP Cancer
    Rucaparib (AG014699) phosphate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib phosphate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib phosphate has the potential for castration-resistant prostate cancer (CRPC) research.
  • HY-10617A
    Rucaparib

    AG014699; PF-01367338

    PARP Cancer
    Rucaparib (AG014699) is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib has the potential for castration-resistant prostate cancer (CRPC) research.
  • HY-147734
    Calpain Inhibitor-2

    Others Cancer
    Calpain inhibitors are lipophilic and show moderate to good antiproliferative activity in vitro compared with melanoma cell lines (a-375 and b-16f1) and PC-3 prostate cancer cells. In addition, a member of this group (compound 3) expressed 2 μ M concentration inhibited the invasion of DU-145 cells by 80%.
  • HY-110112
    BTT-3033

    Integrin Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    BTT-3033 is an orally active conformation-selective inhibitor of α2β1 (EC50: 130 nM) by binding to the α2I domain. BTT-3033 inhibits platelet binding to collagen Ⅰ and cell proliferation, and induces cell apoptosis. BTT-3033 can be used in the research of prostate cancer, inflammation and cardiovascular disease.
  • HY-122611
    CSRM617

    Androgen Receptor Apoptosis Cancer
    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-147874
    ANO1-IN-3

    Chloride Channel Apoptosis Cancer
    ANO1-IN-3 (Compound 3n) is a potent and selective ANO1 inhibitor with an IC50 of 1.23 μM. ANO1-IN-3 induces apoptosis.
  • HY-120574
    TH1338

    Others Cancer
    TH1338 (compound 3b), an orally active camptothecin derivative and a potent chemotherapeutic agent for cancer, demonstrates excellent cytotoxic potency against human tumor cell lines in vitro. TH1338 (compound 3b) possesses significant brain penetration, favorable efflux pump properties, and hematological toxicity profile.
  • HY-19539
    NSC-658497

    Ras Cancer
    NSC-658497 is an effective inhibitor of Ras-GEF, SOS1. NSC-658497 binds to SOS1, competitively suppresses SOS1-Ras interaction, and dose-dependently inhibits SOS1 GEF activity. NSC-658497 showed dose-dependent efficacy in inhibiting Ras, downstream signaling activities, and associated cell proliferation.
  • HY-P3668
    [D-Lys6]-LH-RH

    GnRH Receptor Cancer Endocrinology
    [D-Lys6]-LH-RH is a Luteinizing-hormone-releasing hormone (LHRH) analogue. [D-Lys6]-LH-RH acts as a GnRH receptor agonist.
  • HY-146027
    Androgen receptor antagonist 4

    Androgen Receptor Cancer
    Androgen receptor antagonist 4 (Compound AT2) is an androgen receptor (AR) antagonist with an IC50 of 0.15 μM. Androgen receptor antagonist 4 efficiently antagonizes AR transcriptional activity, suppresses downstream target gene of AR, and blocks the DHT-induced AR nuclear translocation. Androgen receptor antagonist 4 shows anticancer activities.
  • HY-120210
    XY018

    ROR Cancer Inflammation/Immunology
    XY018 is a potent ROR-γ-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC50, 190 nM). XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD).
  • HY-146026
    Androgen receptor antagonist 3

    Androgen Receptor Cancer
    Androgen receptor antagonist 3 (Compound C18) is an androgen receptor (AR) antagonist with an IC50 of 2.4 μM. Androgen receptor antagonist 3 shows anticancer activities.
  • HY-19319
    MI-136

    Epigenetic Reader Domain Androgen Receptor Apoptosis Cancer
    MI-136 is an inhibitor of the menin-MLL protein-protein interaction (PPI), with an IC50 of 31 nM and a Kd of 23.6 nM. MI-136 shows to block AR signaling and has the potential for the study in castration-resistant tumors.
  • HY-111614S
    Melengestrol acetate-d6

    Progesterone Receptor Cancer Metabolic Disease
    Melengestrol acetate-d6 is the deuterium labeled Melengestrol acetate. Melengestrol acetate is a progesterone derivative, acts as an orally active corticosteroid hormone to promote endometrial proliferation, pregnancy maintenance, and delay of menstrual activity. Melengestrol Acetate is used as a contraceptive agent for growth promoting effects and suppression of estrus in animals. Melengestrol acetate inhibits both the androgen-dependent and -independent prostatic tumors in vivo and can be used for cancer research.
  • HY-111614S2
    Melengestrol acetate-d3

    Progesterone Receptor Cancer Metabolic Disease
    Melengestrol acetate-d3 is the deuterium labeled Melengestrol acetate. Melengestrol acetate is a progesterone derivative, acts as an orally active corticosteroid hormone to promote endometrial proliferation, pregnancy maintenance, and delay of menstrual activity. Melengestrol Acetate is used as a contraceptive agent for growth promoting effects and suppression of estrus in animals. Melengestrol acetate inhibits both the androgen-dependent and -independent prostatic tumors in vivo and can be used for cancer research.
  • HY-119344
    MS37452

    Histone Methyltransferase Cancer
    MS37452 is a potent inhibitor of CBX7 chromodomain binding to H3K27me3, with a Kd of 27.7 μM. MS37452 can derepress transcription of polycomb repressive complex target gene p16/CDKN2A by displacing CBX7 binding to the INK4A/ARF locus in prostate cancer cells.
  • HY-102003A
    Rucaparib camsylate

    AG014699 camsylate; PF-01367338 camsylate

    PARP Cancer
    Rucaparib (AG014699) camsylate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib camsylate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib camsylate has the potential for castration-resistant prostate cancer (CRPC) research.
  • HY-110028
    Leelamine hydrochloride

    Cannabinoid Receptor Fatty Acid Synthase (FASN) Androgen Receptor Cancer Endocrinology
    Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees. Leelamine hydrochloride is a cannabinoid receptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells that is not affected by androgen receptor status. Leelamine hydrochloride suppresses transcriptional activity of androgen receptor, which is known to regulate fatty acid synthesis[2,3].
  • HY-111614S1
    Melengestrol acetate-d2

    Progesterone Receptor Cancer Metabolic Disease
    Melengestrol acetate-d2 is the deuterium labeled Melengestrol acetate. Melengestrol acetate is a progesterone derivative, acts as an orally active corticosteroid hormone to promote endometrial proliferation, pregnancy maintenance, and delay of menstrual activity. Melengestrol Acetate is used as a contraceptive agent for growth promoting effects and suppression of estrus in animals. Melengestrol acetate inhibits both the androgen-dependent and -independent prostatic tumors in vivo and can be used for cancer research.
  • HY-102003
    Rucaparib monocamsylate

    AG014699 monocamsylate; PF-01367338 monocamsylate

    PARP Cancer
    Rucaparib (AG014699) monocamsylate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib monocamsylate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib monocamsylate has the potential for castration-resistant prostate cancer (CRPC) research.
  • HY-104040
    MKC8866

    IRE1 Cancer
    MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC50 of 0.29 μM in human vitro. MKC8866 strongly inhibits Dithiothreitol-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC50 of 0.52 μM and unstresses RPMI 8226 cells with an IC50 of 0.14 μM. MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibits prostate cancer (PCa) tumor growth.
  • HY-118487
    OB-24

    Others Cancer
    OB-24 is a potent inhibitor of heme oxygenase-1 (HO-1). Heme oxygenase-1, a member of the heat shock protein family, plays a key role as a sensor and regulator of oxidative stress. OB-24 significantly inhibited cell proliferation in vitro and tumor growth and lymph node/lung metastases in vivo. OB-24 has potential for the research of advanced prostate cancer (PCA).
  • HY-112083
    BAY-3827

    AMPK Cancer
    BAY-3827 is a potent and selective AMPK inhibitor with IC50 values of 1.4 nM at low (10 µM ATP concentration) and 15 nM at high (2 mM ATP concentration). BAY-3827 shows over 500-fold selectivity for most of the 331 kinases. BAY-3827 prevents phosphorylation of acetyl-CoA carboxylase 1 and shows strongest anti-proliferative activity in androgen-dependent prostate cancer cell lines.
  • HY-13604
    Cyproterone acetate

    Androgen Receptor Cancer Endocrinology
    Cyproterone acetate is an anti-androgen (IC50=7.1 nM) and progestogen synthetic steroid. Cyproterone acetate has affinity with progesteron and with glucocorticoidal receptors.
  • HY-145259
    HDAC6-IN-3

    HDAC Histone Demethylase Cancer
    HDAC6-IN-3 (Compound 14), an antiprostate cancer agent, is a potent, orally active HDAC6 inhibitor with IC50s ranging from 0.02-1.54 μM for HDAC1/2/3/6/8/10. HDAC6-IN-3 is also an effective MAO-A (IC50=0.79 μM) and LSD1 inhibitor.
  • HY-70002B
    Enzalutamide carboxylic acid

    MDV3100 carboxylic acid

    Drug Metabolite Cancer
    Enzalutamide carboxylic acid (MDV3100 carboxylic acid) is an inactive metabolite of Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist.
  • HY-123875A
    Ralaniten triacetate

    EPI-506

    Androgen Receptor Cancer
    Ralaniten triacetate (EPI-506), the pro-drug of Ralaniten, is a first-in-class, orally active androgen receptor (AR) N-terminal domain (NTD) inhibitor. Ralaniten triacetate shows activity against both full length and resistance-related AR species, including AR-v7.
  • HY-133045
    VHL Ligand 8

    Ligands for E3 Ligase Cancer
    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.
  • HY-135794
    11-Ketodihydrotestosterone

    11-KDHT; 5α-Dihydro-11-keto testosterone

    Androgen Receptor Endocrinology
    11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells.
  • HY-110028S
    Leelamine-d4 hydrochloride

    Cannabinoid Receptor Fatty Acid Synthase (FASN) Androgen Receptor Cancer Endocrinology
    Leelamine-d4 hydrochloride is the deuterium labeled Leelamine hydrochloride. Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees. Leelamine hydrochloride is a cannabinoid receptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells that is not affected by androgen receptor status. Leelamine hydrochloride suppresses transcriptional activity of androgen receptor, which is known to regulate fatty acid synthesis[2,3].
  • HY-133044
    Boc-Pip-alkyne-Ph-COOH

    PROTAC Linkers Cancer
    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.
  • HY-147185
    PRMT7-IN-1

    Histone Methyltransferase Cancer
    PRMT7-IN-1 (Compound 14) is a PRMT7 inhibitor with an IC50 of 2.1 μM. PRMT7-IN-1 shows anticancer activity against different cancer cells.
  • HY-15792
    (R)-FL118

    10,11-(Methylenedioxy)-20(R)-camptothecin

    Others Cancer
    (R)-FL118 (10,11-(Methylenedioxy)-20(R)-camptothecin) is the R-enantiomer of FL118 (HY-12486). (R)-FL118 shows anticancer activity.
  • HY-10211
    Tanespimycin

    17-AAG; NSC 330507; CP 127374

    HSP Autophagy Mitophagy Bacterial Apoptosis Antibiotic Cancer Infection
    Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90. Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression.
  • HY-135732
    SK33

    Androgen Receptor Cancer
    SK33, a trifluoromethylated enobosarm analog, is a potent, and tissue selective anti-androgen. SK33reduces androgen receptor (AR) transcriptional activity.
  • HY-147868
    DC-CPin711

    Epigenetic Reader Domain Apoptosis Cancer
    DC-CPin711 is a potent and selective inhibitor of CREB-binding protein (CBP) bromodomain with an IC50 of 0.0626 μM. DC-CPin711 arrests cell cycle at G1 phase and induces apoptosis.
  • HY-147864
    c-Fms-IN-12

    c-Fms c-Kit Apoptosis Cancer
    c-Fms-IN-12 (Compound 4g) is an FMS kinase inhibitor. c-Fms-IN-12 can also inhibits c-KIT. c-Fms-IN-12 is a potential broad-spectrum anticancer agent against multiple cancer types. c-Fms-IN-12 induces A549 cell apoptosis.
  • HY-17503C
    Metoprolol fumarate

    CGP 2175C; Lopressor OROS

    Adrenergic Receptor Apoptosis Cancer Infection Endocrinology Cardiovascular Disease
    Metoprolol fumarate (CGP 2175C) is an orally active, selective β1-adrenoceptor antagonist. Metoprolol fumarate shows anti-inflammation, antitumor and anti-angiogenic properties.
  • HY-17503
    Metoprolol

    Adrenergic Receptor Apoptosis Cancer Infection Endocrinology Cardiovascular Disease
    Metoprolol is an orally active, selective β1-adrenoceptor antagonist. Metoprolol shows anti-inflammation, antitumor and anti-angiogenic properties.
  • HY-17503B
    Metoprolol tartrate

    Adrenergic Receptor Apoptosis Cancer Infection Endocrinology Cardiovascular Disease
    Metoprolol tartrate is an orally active, selective β1-adrenoceptor antagonist. Metoprolol tartrate shows anti-inflammation, antitumor and anti-angiogenic properties.
  • HY-17503A
    Metoprolol succinate

    Adrenergic Receptor Apoptosis Cardiovascular Disease Endocrinology Cancer
    Metoprolol succinate is an orally active, selective β1-adrenoceptor antagonist. Metoprolol succinate shows anti-inflammation, antitumor and anti-angiogenic properties.
  • HY-42424
    (S,R,S)-AHPC-Me hydrochloride

    VHL ligand 2 hydrochloride; E3 ligase Ligand 1

    Ligands for E3 Ligase Cancer
    (S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me hydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
  • HY-42424A
    (S,R,S)-AHPC-Me dihydrochloride

    VHL ligand 2 dihydrochloride; E3 ligase Ligand 1 dihydrochloride

    Ligands for E3 Ligase Cancer
    (S,R,S)-AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me dihydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
  • HY-147696
    SMTIN-T140

    HSP AMPK Reactive Oxygen Species Cancer
    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.
  • HY-112078
    (S,R,S)-AHPC-Me

    VHL ligand 2; E3 ligase Ligand 1A

    Ligands for E3 Ligase Cancer
    (S,R,S)-AHPC-Me (VHL ligand 2) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
  • HY-16474S
    Relugolix-d6

    TAK-385-d6

    GnRH Receptor Cancer Endocrinology
    Relugolix-d6 is deuterium labeled Relugolix. Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209). Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al.
  • HY-110368
    BS-181 dihydrochloride

    CDK Cancer
    BS-181 dihydrochloride is a potent and selective CDK7 inhibitor (IC50=21 nM) than Seliciclib (HY-30237). BS-181 is also against CDK2, CDK5 and CDK9 with IC50 values of 880 nM, 3000 nM and 4200 nM, respectively (fails to block CDK1, 4 and 6). BS-181 dihydrochloride inhibits a panel of cancer cells growth (IC50=11.5 μM-37.3 μM) and induces cell apoptosis. BS-181 dihydrochloride has the potential for the research of cancer therapy.
  • HY-114759
    MS-PPOH

    Cytochrome P450 Cancer Metabolic Disease Neurological Disease
    MS-PPOH is a potent and selective cytochrome P450 (CYP) epoxygenase inhibitor. MS-PPOH inhibits CYP2C8 and CYP2C9 with IC50s of 15 and 11 µM, respectively.
  • HY-135794S
    11-Ketodihydrotestosterone-d3

    11-KDHT-d3; 5α-Dihydro-11-keto testosterone-d3

    Androgen Receptor Endocrinology
    11-Ketodihydrotestosterone-d3 (11-KDHT-d3) is the deuterium labeled 11-Ketodihydrotestosterone. 11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells.
  • HY-123295
    HDAC3-IN-T247

    HDAC Cancer Infection
    HDAC3-IN-T247 is a potent and selective HDAC3 (histone deacetylase 3) inhibitor, with an IC50 of 0.24 µM. HDAC3-IN-T247 induces a selective increase of NF-κB acetylation in HCT116 cells. HDAC3-IN-T247 shows anticancer and antiviral activity. HDAC3-IN-T247 inhibits growth of cancer cells, and activates HIV gene expression in latent HIV-infected cells.
  • HY-10122
    Silodosin

    KAD 3213; KMD 3213

    Adrenergic Receptor Bacterial Cancer Endocrinology
    Silodosin (KAD 3213; KMD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH.
  • HY-103345
    2-MPPA

    GPI-5693

    Carboxypeptidase Cancer Neurological Disease
    2-MPPA (GPI-5693) is an orally active and selective glutamate carboxypeptidase II (GCP II; PSMA) inhibitor with an IC50 of 90 nM.
  • HY-13963
    ZCL278

    Ras Cancer
    ZCL278 is a selective Cdc42 modulator that directly binds to Cdc42 and inhibits its functions with Kd of 11.4 μM for Cdc42-ZCL278 affinity in surface plasmon resonance (SPR) experiment.
  • HY-13610
    N1,N11-Diethylnorspermine

    Caspase Cancer
    N1,N11-Diethylnorspermine (DENSPM) is a potent anticancer agent. N1,N11-Diethylnorspermine is a spermine analog that activates polyamine catabolism. N1,N11-Diethylnorspermine induces the release of cytochrome c from mitochondria, resulting in activation of caspase 3. N1,N11-Diethylnorspermine kills glioblastoma multiforme (GBM) cells through induction of SSAT (spermidine/spermine N1-acetyltransferase) coupled with H2O2 production.
  • HY-114250
    Cantrixil

    TRX-E-002-1

    Apoptosis Cancer
    Cantrixil (TRX-E-002-1), an active enantiomer of TRX-E-002, is a second-generation super-benzopyran (SBP) compound. Cantrixil increases phosphorylated c-Jun levels resulting in caspase-mediated apoptosis in ovarian cancer cells. Cantrixil has potent pan anti-cancer activity against a broad range of cancer phenotypes.
  • HY-125108
    PHPS1 sodium

    SHP2 Phosphatase Cancer Cardiovascular Disease
    PHPS1 sodium is a potent and selective Shp2 inhibitor with Kis of 0.73, 5.8, 10.7, 5.8, and 0.47 μM for Shp2, Shp2-R362K, Shp1, PTP1B, and PTP1B-Q, respectively.
  • HY-151266
    AR antagonist 4

    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-14452
    Fatostatin

    125B11

    Fatty Acid Synthase (FASN) Cancer
    Fatostatin (125B11), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin decreases the transcription of lipogenic genes in cells. Fatostatin possesses antitumor properties, and lowers hyperglycemia in ob/ob mice.
  • HY-14452A
    Fatostatin hydrobromide

    125B11 hydrobromide

    Fatty Acid Synthase (FASN) Cancer
    Fatostatin hydrobromide (125B11 hydrobromide), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin hydrobromide binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin hydrobromide decreases the transcription of lipogenic genes in cells. Fatostatin hydrobromide possesses antitumor properties, and lowers hyperglycemia in ob/ob mice.
  • HY-15371
    Forskolin

    Coleonol; Colforsin; HL 362

    Adenylate Cyclase FXR Autophagy Cancer Endocrinology Metabolic Disease Inflammation/Immunology
    Forskolin (Coleonol) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase. Forskolin is also an inducer of intracellular cAMP formation. Forskolin induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR. Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy.
  • HY-112368
    PHPS1

    SHP2 Phosphatase Cancer Cardiovascular Disease
    PHPS1 is a potent and selective Shp2 inhibitor with Kis of 0.73, 5.8, 10.7, 5.8, and 0.47 μM for Shp2, Shp2-R362K, Shp1, PTP1B, and PTP1B-Q, respectively.
  • HY-125355
    SEC

    Apoptosis Cancer
    SEC induces activation of ANXA7 GTPase via the AMPK/mTORC1/STAT3 signaling pathway. SEC selectively promotes apoptosis in cancer cells, expressing a high level of ITGB4 by inducing ITGB4 nuclear translocation.
  • HY-N0704
    Agrimol B

    Sirtuin PPAR Fatty Acid Synthase (FASN) c-Myc Bacterial Cancer Infection Metabolic Disease
    Agrimol B, a polyphenol, is an orally active and potent SIRT1 activator. Agrimol B shows anti-adipogenic and anticancer activity. Agrimol B shows antibacterial activity against plant pathogens. Agrimol B dramatically inhibits 3T3-L1 adipocyte differentiation by reducing PPARγ, C/EBPα, FAS, UCP-1, and apoE expression. The action of Agrimol B on the cancer cells is likely derived from its effect on c-MYC, SKP2 and p27.
  • HY-13818
    Stattic

    STAT Apoptosis Cancer Inflammation/Immunology
    Stattic is a potent STAT3 inhibitor and inhibits STAT3 phosphorylation (at Y705 and S727). Stattic inhibits the binding of a high affinity phosphopeptide for the SH2 domain of STAT3. Stattic ameliorates the renal dysfunction in Alport syndrome (AS) mice.
  • HY-108986
    JFD00244

    Sirtuin SARS-CoV Cancer
    JFD00244 is a sirtuin 2 (SIRT2) inhibitor, with anti-tumor effect. JFD00244 is also a Nsp-16 inhibitor against SARS-CoV-2.
  • HY-17437
    Mefloquine

    Mefloquin

    Parasite Autophagy SARS-CoV Potassium Channel ROS Kinase Cancer Infection Metabolic Disease Inflammation/Immunology
    Mefloquine (Mefloquin), an orally active and potent quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor. Mefloquine is also a K + channel (KvQT1/minK) antagonist with an IC50 of ~1 μM. Mefloquine can be used for malaria, systemic lupus erythematosus and cancer research.
  • HY-135849
    Catalase

    Reactive Oxygen Species Cancer
    Catalase is a key enzyme in the metabolism of H2O2 and reactive oxygen species (ROS), and its expression and localization is markedly altered in tumors. Free oxygen radical scavenger.
  • HY-118762
    KGP94

    Cathepsin Cancer
    KGP94 is a selective inhibitor of cathepsin L with an IC50 of 189 nM. KGP94 inhibits migration and invasion of metastatic carcinoma and shows low cytotoxicity (GI50=26.9 µM) against various human cell lines.
  • HY-133136
    PROTAC BRD4 Degrader-2

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD4 Degrader-2 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC50 of 14.2 nM against BRD4 BD1.
  • HY-N0171A
    Beta-Sitosterol (purity>98%)

    β-Sitosterol (purity>98%); 22,23-Dihydrostigmasterol (purity>98%)

    Apoptosis Endogenous Metabolite Cancer Inflammation/Immunology Cardiovascular Disease
    Beta-Sitosterol (purity>98%) is a plant sterol. Beta-Sitosterol (purity>98%) interfere with multiple cell signaling pathways, including cell cycle, apoptosis, proliferation, survival, invasion, angiogenesis, metastasis and inflammation.
  • HY-N0171B
    Beta-Sitosterol (purity>75%)

    β-Sitosterol (purity>75%); 22,23-Dihydrostigmasterol (purity>75%)

    Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    Beta-Sitosterol (purity>75%) includes 75% β-sitosterol and 10% campesterol. Beta-Sitosterol is a plant sterol. Beta-Sitosterol (purity>75%) interfere with multiple cell signaling pathways, including cell cycle, apoptosis, proliferation, survival, invasion, angiogenesis, metastasis and inflammation.
  • HY-N0171
    Beta-Sitosterol (purity>80%)

    β-Sitosterol (purity>80%); 22,23-Dihydrostigmasterol (purity>80%)

    Endogenous Metabolite Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    Beta-Sitosterol (purity>80%) includes β-sitosterol (≥80%), stigmasterol, campesterol and brassicasterol mainly. Beta-Sitosterol is a plant sterol. Beta-Sitosterol (purity>80%) interfere with multiple cell signaling pathways, including cell cycle, apoptosis, proliferation, survival, invasion, angiogenesis, metastasis and inflammation.
  • HY-117987
    CPS-11

    N-(Hydroxymethyl)thalidomide

    Nuclear Factor of activated T Cells (NFAT) NF-κB Reactive Oxygen Species Cancer
    CPS-11 (N-(Hydroxymethyl)thalidomide) a Thalidomide (HY-14658) analogue, is a potent anti-cancer agent. CPS-11 inhibits NF-κB, activates NFAT, and repress cytokine expression through elevated ROS. CPS-11 exhibits a wider activity spectrum and higher potency against MM (multiple myeloma) cell lines.