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ZR-75-1

" in MedChemExpress (MCE) Product Catalog:

25

Inhibitors & Agonists

1

Peptides

1

Inhibitory Antibodies

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-153444
    Prifetrastat

    PF-07248144

    		 Histone Acetyltransferase Cancer
    Prifetrastat (PF-07248144), a first-in-class, selective, and orally active KAT6A and KAT6AB inhibitor. Prifetrastat can be used for the study of ER+/HER2− breast cancer .
    Prifetrastat
  • HY-133120
    INY-03-041
    1 Publications Verification

    		 PROTACs Akt Cancer
    INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003, Cereblon ligand). INY-03-041 inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0, 6.8 and 3.5 nM, respectively .
    INY-03-041
  • HY-13702
    Nilutamide

    Nilandron; RU 23908

    		 Androgen Receptor Parasite Infection Endocrinology Cancer
    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 .
    Nilutamide
  • HY-14543
    Sertindole
    3 Publications Verification

    Lu 23-174

    		 5-HT Receptor Dopamine Receptor Adrenergic Receptor Autophagy Neurological Disease Cancer
    Sertindole (Lu 23-174) is an orally active 5-HT2A, 5-HT2C, dopamine D2, and αl-adrenergic receptors antagonist. Sertindole shows antipsychotic activity and anti-proliferative activity to multiple cancer cells .
    Sertindole
  • HY-142035
    N-Propargylglycine
    1 Publications Verification

    		 Mitochondrial Metabolism Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    N-Propargylglycine is a brain-penetrant and orally active PRODH inhibitor. N-Propargylglycine covalently modifies enzyme-bound FAD and active site lysine, causing enzyme structural distortion, protein decay, and irreversible inhibition of proline and 4-hydroxyproline catabolism. N-Propargylglycine induces UPRmt, upregulates mitochondrial chaperones and YME1L1, enhances mitochondrial proteostasis, blocks astrocytic L-proline consumption, and abolishes L-proline’s ATP-maintaining and viability-protective effects. N-Propargylglycine stimulates neural processes, increases brain proline, hydroxyproline, and sarcosine levels, partially normalizes Huntington’s disease whole brain transcriptomes. N-Propargylglycine reduces hyperoxaluria, prevents calcium oxalate stone formation, reduces kidney tubular damage, and restores weight and survival in Grhpr knockout mice. N-Propargylglycine can be used for the research of breast cancer, neurodegenerative disorders, Huntington’s disease, and primary hyperoxaluria type 2 .
    N-Propargylglycine
  • HY-U00447
    PK11000

    		MDM-2/p53 DNA Alkylator/Crosslinker Cancer
    PK11000 is an alkylating agent, and stabilizes the DNA-binding domain of both WT and mutant p53 proteins by covalent cysteine modification without compromising DNA binding. PK11000 has anti-tumor activities .
    PK11000
  • HY-P99591
    Sontuzumab

    AS1402; huHMFG-1; Epitumomab

    		 Mucin Cancer
    Sontuzumab (AS1402) is a humanizedised IgG1κ MUC1 specific monoclonal antibody. Sontuzumab binds the extracellular MUC1 peptide sequence PDTR with a Kd of ~1 nM. Sontuzumab can be used for the research of breast cancer .
    Sontuzumab
  • HY-16023A
    Acolbifene
    2 Publications Verification

    EM-652; SCH 57068

    		 Estrogen Receptor/ERR Cancer
    Acolbifene (EM-652), the active metabolite of EM800, is an orally active pure antiestrogen and selective estrogen receptor antagonist. Acolbifene (EM-652) inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50 = 2 nM) and ERβ (IC50 = 0.4 nM). Acolbifene (EM-652) possesses potent and pure anticarcinogenic properties .
    Acolbifene
  • HY-100764
    YUKA1
    1 Publications Verification

    		 Histone Demethylase Cancer
    YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM. YUKA1 has less inhibitory active on KDM5C (IC50 = 7.12 μM) and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 can increase H3K4me3 levels and inhibit cell proliferation. YUKA1 can be used for the research of cancer, such as lung and breast cancers .
    YUKA1
  • HY-122182
    OTS193320

    		Histone Methyltransferase Apoptosis Cancer
    OTS193320, a imidazo[1,2-a]pyridine compound, is a SUV39H2 methyltransferase activity inhibitor. OTS193320 decreases global histone H3 lysine 9 tri-methylation levels in breast cancer cells and triggers apoptotic cell death. Combination of OTS193320 with Doxorubicin (HY-15142A) results in reduction of γ-H2AX levels as well as cancer cell viability compared to a single agent OTS193320 or DOX .
    OTS193320
  • HY-133120A
    INY-03-041 trihydrochloride
    1 Publications Verification

    		 PROTACs Akt Cancer
    INY-03-041 trihydrochloride is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003). INY-03-041 trihydrochloride inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0, 6.8 and 3.5 nM, respectively .
    INY-03-041 trihydrochloride
  • HY-122665
    HTH-01-091

    		MELK DYRK Pim mTOR CDK GSK-3 RIP kinase Cancer
    HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM. HTH-01-091 also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK and CLK2. HTH-01-091 can be uesd for breast cancer research .
    HTH-01-091
  • HY-121435
    K-8012

    		RAR/RXR Akt Apoptosis Drug Derivative TNF Receptor Cancer
    K-8012 is a Sulindac (HY-B0008) analog and RXRα antagonist with an IC50 of 9.2 µM. K-8012 inhibits the activation of AKT. K-8012 induces Apoptosis, redirecting the TNFα signaling pathway from survival to death. K-8012 exerts anticancer activity against lung cancer, prostate cancer, and breast cancer. K-8012 can be used in research related to lung cancer, prostate cancer, breast cancer, and hepatocellular carcinoma .
    K-8012
  • HY-123868
    KW-2581

    		Steroid Sulfatase Cancer
    KW-2581 is a steroidal selective steroid sulfatase (STS) inhibitor with an IC50 of 4 nM. KW-2581 inhibits STS activity of ZR-75-1 cells with an IC50 of 13 nM. KW-2581 inhibits the E1S-stimulated growth of ZR-75-1 cells with an IC50 of 0.18 nM. KW-2581 inhibits sulfated-estrogen dependent growth of breast cancer cells both in vitro and in vivo. KW-2581 induced regression in E1S-induced tumor growth. KW-2581 can be studied in research on hormone receptors-positive breast cancer .
    KW-2581
  • HY-122665A
    HTH-01-091 TFA

    		MELK DYRK Pim mTOR CDK GSK-3 RIP kinase Cancer
    HTH-01-091 TFA is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM. HTH-01-091 TFA also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK and CLK2. HTH-01-091 TFA can be uesd for breast cancer research .
    HTH-01-091 TFA
  • HY-N2741
    Vitexin B-1

    		Bcl-2 Family Cancer
    Vitexin B-1 is an inhibitor of Bcl-2 and the agonist of Caspase. Vitexin B-1 has cytotoxic effect and induces apoptosis in MCF-7, ZR-75-1, MDA-MB-231, and COC1 cells with IC50s of 3.2, 2.1, 1.8 and 0.39 μM, respectively .
    Vitexin B-1
  • HY-16023
    Acolbifene hydrochloride
    2 Publications Verification

    EM-652 hydrochloride; SCH 57068 hydrochloride

    		 Estrogen Receptor/ERR Cancer
    Acolbifene (EM-652) hydrochloride, an active metabolite of EM800, is an orally active, cancer-preventing selective estrogen receptor modulator (SERM). Acolbifene (EM-652) hydrochloride inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50=2 nM) and ERβ (IC50=0.4 nM). Acolbifene (EM-652) hydrochloride exerts a potent and pure antiestrogenic action in the mammary gland and uterus. Anticarcinogenic properties .
    Acolbifene hydrochloride
  • HY-P11255
    SPDI-48-T1

    		MDM-2/p53 Cancer
    SPDI-48-T1 is a lysine-stapled peptide. SPDI-48-T1 exhibits discernible binding affinities for MDM2 and MDMX, with Kd values of 396 nM and 456 nM, respectively. SPDI-48-T1 exhibits anticancer activity against breast cancer, colorectal cancer, non-small cell lung cancer, cervical cancer, and malignant melanoma .
    SPDI-48-T1
  • 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 .
    BS-181 dihydrochloride
  • HY-121149B
    (E/Z)-Droloxifene

    (E/Z)-3-Hydroxytamoxifen

    		 Estrogen Receptor/ERR Apoptosis Cancer
    (E/Z)-Droloxifene is a mixture of (E)-droloxifene (a selective estrogen receptor modulator) and (Z)-droloxifene. (E)-Droloxifene binds to the estrogen receptor (ER) with an IC50 value of 24 nM in rabbit uterine homogenates. (E)-Droloxifene increases uterine weight in immature rats, and reduces estradiol-induced increases in uterine weight in juvenile rats. (E)-Droloxifene also inhibits 17β-estradiol-stimulated growth of MCF-7, ZR-75-1, and T47D human breast cancer cells. (Z)-Droloxifene binds weakly to ER and has no estrogenic or antiestrogenic activity .
    (E/Z)-Droloxifene
  • HY-114631
    EM-800

    		Estrogen Receptor/ERR Cancer
    EM-800, an orally active anti-estrogen, serves as an antagonist to the transcriptional functions of estrogen receptors α (ERα) and β (ERβ). EM-800 possesses anticancer activity, capable of inhibiting the growth of breast cancer induced by 7,12-Dimethylbenz[a]anthracene (DMBA) (HY-W011845). Furthermore, in ovariectomized animals, EM-800 effectively slows down bone loss. Additionally, EM-800 shows potential in the research of breast and endometrial cancers, while exerting beneficial effects on bone and lipid metabolism .
    EM-800
  • HY-13702R
    Nilutamide (Standard)

    Nilandron (Standard); RU 23908 (Standard)

    		 Reference Standards Androgen Receptor Parasite Infection Endocrinology Cancer
    Nilutamide (Standard) is the analytical standard of Nilutamide. This product is intended for research and analytical applications. 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 .
    Nilutamide (Standard)
  • HY-14543R
    Sertindole (Standard)

    Lu 23-174 (Standard)

    		 5-HT Receptor Dopamine Receptor Adrenergic Receptor Autophagy Reference Standards Neurological Disease Cancer
    Sertindole (Standard) is the analytical standard of Sertindole. This product is intended for research and analytical applications. Sertindole (Lu 23-174) is an orally active 5-HT2A, 5-HT2C, dopamine D2, and αl-adrenergic receptors antagonist. Sertindole shows antipsychotic activity and anti-proliferative activity to multiple cancer cells .
    Sertindole (Standard)
  • HY-100764R
    YUKA1 (Standard)

    		Histone Demethylase Reference Standards Cancer
    YUKA1 (Standard) is the analytical standard of YUKA1 (HY-100764). This product is intended for research and analytical applications. YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM. YUKA1 has less inhibitory active on KDM5C (IC50 = 7.12 μM) and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 can increase H3K4me3 levels and inhibit cell proliferation. YUKA1 can be used for the research of cancer, such as lung and breast cancers .
    YUKA1 (Standard)
  • HY-183139
    CD666

    		RAR/RXR AP-1 Cancer
    CD666 is a selective retinoic acid receptor-γ (RAR-γ) agonist with a Kd of 68 nM. CD666 inhibits proliferation of cancer cells and shows synergistical effects and anti-AP-1 activity with IFN-γ. CD666 can be used for the research of breast cancer .
    CD666

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