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42

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Click Chemistry

Cat. No. Nombre del producto Target Áreas de investigación Chemical Structure
  • HY-16985
    Darolutamide
    5+ Cited Publications

    ODM-201; BAY-1841788

    		 Androgen Receptor Cancer
    Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist. Darolutamide has a Ki of 11 nM for rat wild-type AR (wtAR) and IC50 of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .
    Darolutamide
  • HY-112683
    V-9302
    Maximum Cited Publications
    34 Publications Verification

    		 ASCT Cancer
    V-9302 is a competitive antagonist of transmembrane glutamine flux. V-9302 selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 inhibits ASCT2-mediated glutamine uptake (IC50=9.6 μM) in HEK-293 cells .
    V-9302
  • HY-112683A
    V-9302 hydrochloride
    Maximum Cited Publications
    34 Publications Verification

    		 ASCT Cancer
    V-9302 hydrochloride is a competitive antagonist of transmembrane glutamine flux. V-9302 hydrochloride selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 hydrochloride inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells .
    V-9302 hydrochloride
  • HY-136789
    Tuxobertinib
    1 Publications Verification

    BDTX-189

    		 EGFR Cancer
    Tuxobertinib (BDTX-189) is a potent, orally active and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, including EGFR/HER2 exon 20 insertion mutants. Tuxobertinib shows KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. Anticancer activity .
    Tuxobertinib
  • HY-100433
    PACMA 31
    5 Publications Verification

    		 PDI Cancer
    PACMA 31 is an irreversible, orally active protein disulfide isomerase (PDI) inhibitor with an IC50 of 10 μM. PACMA 31 forms a covalent bond with the active site cysteines of PDI. PACMA 31 shows tumor targeting ability and significantly suppresses ovarian tumor growth without causing toxicity to normal tissues . PACMA 31 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    PACMA 31
  • HY-124675
    MYCMI-6
    1 Publications Verification

    NSC354961

    		 c-Myc Apoptosis Cancer
    MYCMI-6 (NSC354961) is a potent and selective endogenous MYC:MAX protein interactions inhibitor. MYCMI-6 blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain with a Kd of 1.6 μM. MYCMI-6 inhibits tumor cell growth in a MYC-dependent manner (IC50<0.5 μM). MYCMI-6 is not cytotoxic to normal human cells. MYCMI-6 induces apoptosis .
    MYCMI-6
  • HY-79139
    Pteroic acid
    1 Publications Verification

    		 Drug Intermediate Metabolic Disease
    Pteroic acid is a precursor to significant compounds like Folic acid (HY-16637) and Vitamin B12 (HY-B0315). Pteroic acid facilitates the examination of how different compounds influence cell growth and development .
    Pteroic acid
  • HY-176763
    KZR-261

    		Sec61 Cancer
    KZR-261 is a Sec61 translocase inhibitor. KZR-261 binds directly to the Sec61 channel, thereby inhibiting the biosynthesis of certain Sec61 substrate proteins, including oncogenic factors. KZR-261 activates the endoplasmic reticulum stress response. KZR-261 exhibits broad in vitro anticancer activity. KZR-261 shows antitumor efficacy in mouse models of cancer. KZR-261 can be used for the research of multiple myeloma, colorectal cancer, small cell lung cancer, pancreatic cancer, prostate cancer, non-Hodgkin's lymphoma, and mantle cell lymphoma .
    KZR-261
  • HY-W250574
    NOTA-bis(tBu)ester

    NOTA-bis(t-Butyl ester)

    		 Biochemical Assay Reagents Radionuclide-Drug Conjugates (RDCs) Drug Derivative Cancer
    NOTA-bis (tBu) ester is a derivative of NOTA (HY-134418). NOTA-bis (tBu) ester is radiolabeled with 68Ga to form ZD2-( 68Ga-NOTA) after conjugation with ZD2. ZD2-( 68Ga-NOTA) can be used for PET imaging studies of pancreatic cancer .
    NOTA-bis(tBu)ester
  • HY-P991584
    HuGAL-FR21

    		FGFR Cancer
    HuGAL-FR21 is a humanized antiFGFR2IIIb IgG1 monoclonal antibody. HuGAL-FR21 can block the binding of FGF2, FGF7, and FGF10 to FGFR2IIIb and inhibit FGF-induced phosphorylation of FGFR2IIIb. HuGAL-FR21 can downregulate the expression of FGFR2 in SNU-16 cells. HuGAL-FR21 shows the significant anti-tumor activity in athymic nude mice bearing gastric cancer xenograft models. HuGAL-FR21 can be used for research on cancer such as gastric cancer .
    HuGAL-FR21
  • HY-117280
    GN25

    		MDM-2/p53 Cancer
    GN25 is a specific p53-Snail binding inhibitor with antitumor effects .
    GN25
  • HY-14674
    CP-724714
    4 Publications Verification

    		 EGFR Apoptosis Cancer
    CP-724714 is a potent, selective and orally active ErbB2 (HER2) tyrosine kinase inhibitor, with an IC50 of 10 nM. CP-724714 displays a marked selectivity against EGFR kinase (IC50=6400 nM). CP-724714 potently inhibits ErbB2 receptor autophosphorylation in intact cells. Antitumor activities .
    CP-724714
  • HY-114750
    Mebendazole-amine

    		Drug Metabolite Infection
    Mebendazole-amine is a metabolite of Mebendazole (HY-17595). Mebendazole is a broad-spectrum benzimidazole anthelmintic .
    Mebendazole-amine
  • HY-110201
    Estrogen receptor modulator 1

    		Estrogen Receptor/ERR Cancer
    Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors .
    Estrogen receptor modulator 1
  • HY-106892
    BW 348U87

    348U87

    		 DNA/RNA Synthesis Infection
    BW 348U87 is an inhibitor for ribonucleotide reductase, which exhibits synergistic effect with Acyclovir (HY-17422), potentiate the antiviral activity of Acyclovir against herpes simplex virus (HSV) in athymic nude mouse model .
    BW 348U87
  • HY-156959
    Ovalicin

    		JAK TRP Channel MetAP Infection Inflammation/Immunology
    Ovalicin is a multi-target inhibitor that targets MetAP2, HRH2, JAK2 and TRPV1, with anti-inflammatory and anti-atopic dermatitis activities. Ovalicin covalently binds to MetAP2 to inhibit its function, thereby blocking the replication of Enterocytozoon bieneusi and Vittaforma corneae. Ovalicin alleviates intestinal injury and prolongs survival in infected mouse models, without showing obvious hepatorenal toxicity. Ovalicin attenuates LPS-induced calcium influx, reduces the infiltration of macrophages and mast cells in the skin, and regulates the expression of inflammation-related genes such as IL-31, effectively relieving allergic symptoms in mouse models. Ovalicin can be used for the research of microsporidiosis and atopic dermatitis .
    Ovalicin
  • HY-110151
    Bengamide B

    		NF-κB Interleukin Related Inflammation/Immunology Cancer
    Bengamide B is an alkaloid with anti-tumor and anti-inflammatory activities. Bengamide B reduces the phosphorylation level of IκBα, thereby blocking the activation of NF-κB. Bengamide B inhibits the proliferation of tumor cells. Bengamide B can be used in research related to inflammatory diseases and cancers .
    Bengamide B
  • HY-16985S
    Darolutamide-d4

    ODM-201-d4; BAY-1841788-d4

    		 Isotope-Labeled Compounds Androgen Receptor Cancer
    Darolutamide-d4 (ODM-201-d4) is deuterium labeled Darolutamide (HY-16985). Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist, with a Ki of 11 nM for rat wild-type AR (wtAR) and an IC50 of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .
    Darolutamide-d4
  • HY-176847
    DHQZ-17

    		Orphan Nuclear Receptor Apoptosis Cancer
    DHQZ-17 is a HNF4A inhibitor. DHQZ-17 triggers apoptosis in head and neck squamous cell carcinoma cells. DHQZ-17 can be used for the research of head & neck squamous cell carcinoma .
    DHQZ-17
  • HY-158006
    SDX-7539

    		MetAP Cancer
    SDX-7539 is a selective inhibitor for Methionine aminopeptidase type 2 (MetAP2). SDX-7539 inhibits proliferarion of HUVECs with an IC50 of 120 μM. SDX-7539 exhibits antitumor activity in NSCLC xenograft athymic nude mice .
    SDX-7539
  • HY-158005
    Anticancer agent 195

    		Apoptosis Cancer
    Anticancer agent 195 (Compound 10) is an inhibitor for ELF3-MED23 PPI with Ki of 0.68 μM. Anticancer agent 195 induces apoptosis and exhibits antitumor activity .
    Anticancer agent 195
  • HY-16985R
    Darolutamide (Standard)

    ODM-201 (Standard); BAY-1841788 (Standard)

    		 Reference Standards Androgen Receptor Cancer
    Darolutamide (Standard) is the analytical standard of Darolutamide (HY-16985). This product is intended for research and analytical applications. Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist, with a Ki of 11 nM for rat wild-type AR (wtAR) and an IC50 of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .
    Darolutamide (Standard)
  • HY-W854385
    Sialyl Lewis A

    SLeA

    		 Biochemical Assay Reagents E-Selectin Cancer
    Sialyl Lewis A (SLeA) is a tumor-associated carbohydrate antigen, also known as carbohydrate antigen 19-9 (CA19-9), that binds to E-selectin (ELAM-1) and selectins to mediate cell-endothelium adhesion. Sialyl Lewis A promotes cancer cell-vascular endothelium adhesion, and its surface presence correlates with increased tumorigenicity and invasiveness in cancer cells. Sialyl Lewis A shows elevated expression in human adenocarcinomas of the colon, pancreas, and stomach, with expression levels linked to tumor progression and poor prognosis in colorectal and gastric carcinomas. Sialyl Lewis A can be used for the research of cancers, such as colon, pancreas, stomach, and squamous lung cancer .
    Sialyl Lewis A
  • HY-161618
    MJ04

    		JAK EGFR PI3K IGF-1R GSK-3 Inflammation/Immunology Endocrinology
    MJ04 is a selective inhibitor for Janus Kinase 3 (JAK 3) with an IC50 of 2.03 nM. MJ04 inhibits T cell differentation and inhibits the proinfammatory cytokines in Lipopolysaccharides (HY-D1056)‑induced macrophages. MJ04 exhibits good pharmacokinetic characters in mice, promotes hair growth in DHT-induced androgenetic alopecia (AGA) in athymic mice model, without significant toxicity (LD50 >2 g/kg) .
    MJ04
  • HY-107336
    Cyclovalone

    Beveno

    		 COX Inflammation/Immunology
    Cyclovalone (Beveno) is a synthetic curcumin derivate, which inihibits cyclooxygenase and exhibits anti-inflammatory, antitumor and antioxidant activities . Cyclovalone inhibits cell proliferation in normal and malignant prostatic cells. Cyclovalone ist orally active .
    Cyclovalone
  • HY-101021
    Ascochlorin

    Ilicicolin D

    		 STAT Apoptosis Antibiotic Inflammation/Immunology Cancer
    Ascochlorin (Ilicicolin D), an isoprenoid antibiotic, mediates its anti-tumor effects predominantly through the suppression of STAT3 signaling cascade. Ascochlorin induces apoptosis. Anti-inflammatory activity .
    Ascochlorin
  • HY-174870
    PROTAC ERα Degrader-11

    		PROTACs Estrogen Receptor/ERR Apoptosis Fluorescent Dye Cancer
    PROTAC ERα Degrader-11 is a selective and intrinsically fluorescent (Ex: 366 nm, Em: 440 nm) ERα PROTAC degrader. PROTAC ERα Degrader-11 shows good antiproliferative activity, selective ERα degradation and imaging capabilities in MCF-7 breast cancer cell lines. PROTAC ERα Degrader-11 induces G2/M phase arrest and induces apoptosis in MCF-7 cells. PROTAC ERα Degrader-11 is well-tolerated up to a dose of 500 mg/ kg with no acute toxicity in athymic nude mice. PROTAC ERα Degrader-11 can be used for the study of breast cancer.(Pink: ERα ligand (HY-167701), Blue: CRBN Ligand (HY-150831), Black: Linker, E3 ligase ligand-linker conjugate (HY-174880)) .
    PROTAC ERα Degrader-11
  • HY-119218
    LH 1

    		Others Inflammation/Immunology
    LH 1 is a potent immunostimulant used for the anti-PVP (polyvinylpyrrolidone) response in athymic mice .
    LH 1
  • HY-123237
    KRC-108

    		c-Met/HGFR FLT3 Trk Receptor Apoptosis Autophagy Cancer
    KRC-108, an aminopyridine, is an orally active multiple kinase inhibitor with IC50s of 80 nM, 23 nM, 3 nM, 70 nM, 30 nM, 39 nM for c-Met, c-Met M1250T, c-Met Y1230D, Ron, Flt3 and TrkA, respectively. KRC-108 induces cell cycle arrest, apoptotic cell death, and autophagy. KRC-108 exhibits anti-tumor activity in vivo in HT29 colorectal cancer, NCI-H441 lung cancer xenograft models in athymic BALB/c nu/nu mice .
    KRC-108
  • HY-165369
    IBPR002

    		Aurora Kinase Cancer
    IBPR002 is an inhibitor of Aurora kinase A and Aurora kinase B, with IC50 values of 41 nM and 17 nM, respectively. IBPR002 disrupts the nucleation and bundling of kinetochore microtubules, impairs the bipolarity of mitotic spindles, and promotes the binding of non-phosphorylated hepatoma up-regulated protein (HURP) to microtubules derived from the mother centrosome. IBPR002 reduces tumorigenesis levels in a colorectal cancer xenograft model using athymic nude mice. IBPR002 is applicable for research related to colorectal cancer .
    IBPR002
  • HY-100433R
    PACMA 31 (Standard)

    		PDI Reference Standards Cancer
    PACMA 31 (Standard) is the analytical standard of PACMA 31 (HY-100433). This product is intended for research and analytical applications. PACMA 31 is an irreversible, orally active protein disulfide isomerase (PDI) inhibitor with an IC50 of 10 μM. PACMA 31 forms a covalent bond with the active site cysteines of PDI. PACMA 31 shows tumor targeting ability and significantly suppresses ovarian tumor growth without causing toxicity to normal tissues . PACMA 31 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    PACMA 31 (Standard)
  • HY-182240
    Cy5-ZW2-617

    		PSMA Cancer
    Cy5-ZW2-617 is a PSMA ligand with a IC50 of 4.39 nM. Cy5-ZW2-617 specifically binds to PSMA and is thereby internalized by PSMA-positive cells. Cy5-ZW2-617 shows uptake in PSMA-positive tumor cells and tumor xenografts in mice. Cy5-ZW2-617 can be used for the research of prostate cancer .
    Cy5-ZW2-617
  • HY-178248
    PSMA-R2

    		PSMA Cancer
    PSMA ligand 2 is a prostate specific membrane antigen (PSMA) ligand with a glutamate-urea-lysine (GUL) moiety. PSMA ligand 2 can be efficiently labeled with radioactive nuclides such as 68Ga and 177Lu and specifically binds to PSMA-positive tumor cells. PSMA ligand 2 can be used for imaging of PSMA-expressing tumors or cells via PET or SPECT imaging. PSMA ligand 2 can be used for the research of prostate cancer .
    PSMA-R2
  • HY-181573
    TC8026

    		PDI Apoptosis Neurological Disease Cancer
    TC8026 is an allosteric-covalent inhibitor targeting protein disulfide isomerase (PDI), with an IC50 of 7 μM against human PDI. TC8026 induces endoplasmic reticulum stress-mediated apoptosis. TC8026 is a hit compound with PDI inhibitory activity identified via high-throughput screening, and it can be used for the research of glioblastoma .
    TC8026
  • HY-182746
    RG7388-PEG3-Click-F

    		MDM-2/p53 Drug Derivative Cancer
    RG7388-PEG3-Click-F is a fluorinated analog of the MDM2 inhibitor RG7388 (HY-15676), with an IC50 of 16.8 nM against MDM2. [ 18F]RG7388-PEG3-Click-F exhibits high uptake and specificity in MDM2-expressing myeloma cells, and can be used for non-invasive assessment of MDM2 protein expression levels in tumors .
    RG7388-PEG3-Click-F
  • HY-P11773
    3P-RGD2

    		Radionuclide-Drug Conjugates (RDCs) Integrin Others
    3P-RGD2 is a dimeric cyclic RGD (Arg-Gly-Asp) peptide. When radiolabeled with 99mTc, 3P-RGD2 serves as a selective radiotracer for integrin αvβ3. When radiolabeled with 99mTc, 3P-RGD2 enables single-photon emission computed tomography imaging of integrin αvβ3 .
    3P-RGD2
  • HY-P11782
    GTGKT

    		GSK-3 CDK Apoptosis Cancer
    GTGKT is a CAGE inhibitor. GTGKT binds to CAGE and blocks the binding of CAGE to GSK3β. GTGKT alters the localization of CAGE and inhibits the binding of CAGE to the promoter sequence of Cyclin D1. GTGKT enhances the Apoptotic effect of anticancer agents. GTGKT reduces the expression of Cyclin D1. GTGKT decreases the tumorigenic potential of melanoma and hepatocellular carcinoma cells .
    GTGKT
  • HY-P1380
    Difopein

    		Apoptosis Bcl-2 Family Caspase Cancer
    Difopein is a 14-3-3 protein inhibitor. Difopein acts as an apoptosis inducer, regulates apoptosis-related proteins, downregulates Bcl-2, upregulates Bax, activates caspase-9 and caspase-3, and induces nuclear fragmentation, membrane-enclosed apoptotic bodies and DNA ladder formation. Difopein serves as a tumor growth inhibitor, which inhibits the proliferation of glioma cells and induces their apoptosis in in vivo nude mouse models. Difopein is applicable to glioma-related research .
    Difopein
  • HY-165503
    AZ1366

    		Wnt β-catenin Cancer
    AZ1366 is an orally active tankyrase inhibitor. AZ1366 stabilizes Axin2, reduces NuMA levels, disrupts the interaction between tankyrase and NuMA, induces G2/M phase arrest, inhibits the Wnt pathway, and downregulates the expression of β-catenin-dependent genes. AZ1366 inhibits tumor growth in colorectal cancer xenograft models. AZ1366 synergistically inhibits the proliferation of non-small cell lung cancer cells, improves tumor control and significantly prolongs survival in orthotopic non-small cell lung cancer mouse models. AZ1366 is applicable to research related to colorectal cancer and non-small cell lung cancer .
    AZ1366
  • HY-P11781
    HW12

    		Drug Derivative Cancer
    HW12 is a random peptide containing an N-terminal cysteine and is not an EGFR ligand. HW12 can serve as a control for GE11 (HY-P10128)-conjugated mixed micelles targeting EGFR. HW12 is applicable to pancreatic cancer-related research .
    HW12
  • HY-182264
    Masoprocol tetrapivalate

    Nordihydroguaiaretic acid tetrapivalate

    		 IGF-1R EGFR Drug Metabolite Cancer
    Masoprocol tetrapivalate (Nordihydroguaiaretic acid tetrapivalate) is a catecholic butane metabolite and also a tyrosine kinase activity inhibitor of IGF-1R and EGFR. Masoprocol tetrapivalate regulates tyrosine kinase signaling pathways associated with cell proliferation. Masoprocol tetrapivalate can be used in the research of proliferative diseases, including malignant, precancerous or benign cancers, and solid tumors .
    Masoprocol tetrapivalate
  • HY-P991883
    Metuzumab

    Licartin; Metuximab; Mehuzumab

    		 Apoptosis CDK Caspase Bcl-2 Family Cancer
    Metuzumab (Licartin) is a human-mouse chimeric IgG1 monoclonal antibody targeting CD147. Metuzumab induces Apoptosis, reduces levels of Cyclin D1, full-length Caspase-3, and Bcl-2, and increases Bax expression. Metuzumab enhances the sensitivity of non-small cell lung cancer (NSCLC) cells to Gemcitabine (HY-17026). Metuzumab is applicable for research on hepatocellular carcinoma and non-small cell lung cancer [1] [2].
    Metuzumab

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