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orthotopic

" in MedChemExpress (MCE) Product Catalog:

73

阻害剤およびアゴニスト

1

蛍光色素

2

生化学アッセイ試薬

13

ペプチド

6

阻害性抗体

2

天然物

2

同位体標識化合物

1

クリックケミストリー

2

オリゴヌクレオチド

製品番号 製品名 Target 研究分野 構造式
  • HY-103193
    NKH477

    Colforsin dapropate hydrochloride

    		 Adenylate Cyclase Cardiovascular Disease
    NKH477 (Colforsin dapropate hydrochloride) directly activates the catalytic unit of adenylate cyclase and increases intracellular cAMP. NKH477 is a forskolin derivative that improves cardiac failure mainly through its beneficial effects on diastolic cardiac function. NKH477 exerts an antiproliferative effect in vivo with an altered cytokine profile to inhibit the acute rejection of rat orthotopic lung allografts .
    NKH477
  • HY-P99908
    Efineptakin alfa

    NT-17

    		 Interleukin Related Cancer
    Efineptakin alfa (NT-17) is a long-acting recombinant human IL-7. Efineptakin alfa supports the proliferation and survival CD4 + and CD8 + cells in both human and mice. Efineptakin alfa can be used for glioblastoma research .
    Efineptakin alfa
  • HY-P1416
    Foxy-5
    Maximum Cited Publications
    7 Publications Verification

    		 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 .
    Foxy-5
  • HY-162874
    diABZI-V/C-DBCO

    		STING IFNAR Cancer
    diABZI-V/C-DBCO is a STING agonist with an EC50 of 1.47 nM. diABZI-V/C-DBCO activates the STING pathway, induces the production of IFN-I, and stimulates the secretion of IFN-β. diABZI-V/C-DBCO serves as a substrate for cathepsin B, and releases active diABZI-amine via cathepsin B-mediated cleavage. In an orthotopic mouse model of breast cancer, diABZI-V/C-DBCO increases serum IFN-β levels and the frequency of granzyme B + CD8 + T cells. diABZI-V/C-DBCO is applicable to research related to triple-negative breast cancer .
    diABZI-V/C-DBCO
  • HY-12875
    BQU57

    		Ras Cancer
    BQU57 is a selective inhibitor of RalA/RalB small GTPases, with a binding potency (Kb) of 7.7 μM for RalB-GDP. BQU57 can block its interaction with effector proteins (such as SEC5 and EXO84), inhibiting tumor cell migration, invasion and non-adherent growth. BQU57 downregulates the NF-κB signaling pathway, reduces the expression of IL-6, IL-8 and MMP-13, and inhibits apoptosis by regulating the Bcl-2/Bax balance. BQU57 also protects the extracellular matrix by inhibiting the Ral/NF-κB pathway and can be used for the study of degenerative diseases. BQU57 exhibits significant antitumor activity in triple-negative breast cancer (TNBC) models, inhibiting orthotopic tumor growth and lung metastasis and enhancing paclitaxel chemotherapy sensitivity .
    BQU57
  • HY-19350
    BML-210
    2 Publications Verification

    		 HDAC Apoptosis Cancer
    BML-210 is a potent HDAC inhibitor. BML-210 can inhibit the HDAC4-VP16-driven reporter signal with an apparent IC50 of ∼5 µM. BML-210 has a specific disruptive effect on the HDAC4:MEF2 interaction. BML-210 causes an increase in the G0/G1 phase. BML-210 induces apoptosis and displays antitumour activities in orthotopic mammary tumours in mice .
    BML-210
  • HY-P991316
    KD014

    DX-2400; DX-2410

    		 MMP NO Synthase Inflammation/Immunology Cancer
    KD014 (DX-2400) is a human monoclonal antibody that selectively targets MMP‑14. KD014 inhibits collagen degradation and regulates the polarization of macrophages toward an anti-inflammatory/anti-tumor phenotype. KD014 alleviates joint damage in rheumatoid arthritis and suppresses tumor growth and invasion. KD014 can be used in studies related to breast cancer and rheumatoid arthritis .
    KD014
  • HY-P11287A
    DOTA-Pep-1L TFA

    		Interleukin Related Radionuclide-Drug Conjugates (RDCs) Cancer
    DOTA-Pep-1L TFA is a polypeptide formed by the conjugation of DOTA and Pep-1L. DOTA-Pep-1L TFA specifically binds to IL13RA2 and can be used for the synthesis of targeted polypeptides. DOTA-Pep-1L TFA yields the isotopically labeled product [ 225Ac]DOTA-Pep-1L, which exerts α-radiation killing effects on orthotopic glioma cells and extends the median survival time of mice bearing orthotopic glioma models after stereotactic injection. DOTA-Pep-1L TFA can be used for PET imaging, tumor targeting and glioma research .
    DOTA-Pep-1L TFA
  • HY-P5098
    E(c(RGDfK))2

    		Integrin Neurological Disease Cancer
    E (c (RGDfK)) 2 is a αvβ3 integrin ligand and tumor-targeting agent. E (c (RGDfK)) 2 binds to αvβ3 integrin, mediates receptor-mediated endocytosis of conjugated payloads, and inhibits integrin-dependent cell adhesion to fibrinogen. E (c (RGDfK)) 2 inhibits the proliferation of cancer cells and endothelial cells. E (c (RGDfK)) 2 preferentially accumulates in orthotopic mouse breast tumors and human ovarian cancer xenograft tumors. E (c (RGDfK)) 2 can be used in research related to glioblastoma, lung cancer, breast adenocarcinoma and ovarian cancer .
    E(c(RGDfK))2
  • HY-115677
    ILK-IN-3

    		Ser/Thr Kinase Cancer
    ILK-IN-3 is an orally active integrin linked kinase (ILK) inhibitor. ILK-IN-3 improves the anticancer efficacy of Docetaxel (HY-B0011) in orthotopic LCC6 model .
    ILK-IN-3
  • HY-148409
    MMRi62

    		Ferroptosis Apoptosis Autophagy MDM-2/p53 Cancer
    MMRi62, a ferroptosis inducer targeting MDM2-MDM4 (negative regulators of tumor suppressor p53). MMRi62 shows a P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induce autophagy. MMRi62 inducesferroptosis, resulting in a increase of reactive oxygen and lysosomal degradation of ferritin heavy chain (FTH1). MMRi62 also leads to proteasomal degradation of mutant p53, also inhibits orthotopic xenograft PDAC mouse model in vivo with high frequency mutation characteristics of KRAS and TP53.12 .
    MMRi62
  • HY-160972
    MM0299

    		LXR Neurological Disease Cancer
    MM0299 is a selective lanosterol synthase (LSS) inhibitor with an IC50 value of 2.22 μM. MM0299 depletes intracellular cholesterol and acts as a growth inhibitor for glioma stem-like cells. MM0299 exhibits anti-glioblastoma activity. MM0299 is applicable to research related to glioblastoma .
    MM0299
  • HY-19337
    Ketodarolutamide
    1 Publications Verification

    BAY 1896953; ORM-15341

    		 Androgen Receptor Cancer
    Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a Ki value of 8 nM for rat wild-type AR and an IC50 value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .
    Ketodarolutamide
  • HY-110243
    CAIX Inhibitor S4
    1 Publications Verification

    		 Carbonic Anhydrase Cancer
    CAIX Inhibitor S4 is a potent and selective inhibitor of carbonic anhydrase IX/XII (CA IX/XII), with a Ki of 7 nM and 2 nM, respectively. CAIX Inhibitor S4 also inhibits CA II and CA I (Ki=546 and 5600 nM, respectively). CAIX Inhibitor S4 can inhibit the number of lung metastasis in orthotopic MDA-MB-231 mouse model without affecting primary tumor growth .
    CAIX Inhibitor S4
  • HY-P11058
    OVA(250-264)

    OVAp

    		 MHC Cancer
    OVA(250-264) (OVAvac) (OVAp) is an antigen peptide that can be from ovalbumin (OVA) presented by the class I MHC molecule, H-2Kb. OVA(250-264) combined withαMSLN (anti-MSLN antibody) significantly induces antigen-specific CD8 + T cell generation and infiltration for enhancing antitumor efficacy in orthotopic pancreatic cancer mice model. OVA(250-264) can be used for neoantigen vaccine development in pancreatic cancer immunotherapy research .
    OVA(250-264)
  • HY-114483
    AES-135
    1 Publications Verification

    		 HDAC Cancer
    AES-135, a hydroxamic acid-based pan-HDAC inhibitor, prolongs survival in an orthotopic mouse model of pancreatic cancer. AES-135 inhibits HDAC3, HDAC6, HDAC8, and HDAC11 with IC50s ranging from 190-1100 nM .
    AES-135
  • HY-16726
    Polmacoxib

    CG100649

    		 COX Carbonic Anhydrase Cancer
    Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory agent (NSAID) which is a dual inhibitor of COX-2 (IC50 around 0.1 μg/ml) and carbonic anhydrase . Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models .
    Polmacoxib
  • HY-13545
    ABT-510
    1 Publications Verification

    		 Apoptosis Inflammation/Immunology Cancer
    ABT-510 is an anti-angiogenic TSP peptide (Thrombospondin-1 analogue) that induces apoptosis and inhibits ovarian tumour growth in an orthotopic, syngeneic model of epithelial ovarian cancer. ABT-510 also reduces angiogenesis and inflammatory responses in a murine model of inflammatory bowel disease. ABT-510 can be used in studies of cancer (particularly epithelial ovarian cancer) and inflammatory bowel disease (IBD) .
    ABT-510
  • HY-16785
    Veledimex

    INXN-1001; RG-115932

    		 Interleukin Related Inflammation/Immunology Cancer
    Veledimex (INXN-1001), a synthetic analog of the insect molting hormone ecdysone, is an orally active activator ligand for a proprietary gene therapy promoter system. Veledimex can be used to activate certain genes using the ecdysone receptor (EcR)-based inducible gene regulation system, the RheoSwitch Therapeutic System (RTS). Veledimex can cross blood-brain barrier (BBB) in both orthotopic GL-261 mice and cynomolgus monkeys .
    Veledimex
  • HY-143411
    GEM144

    		HDAC Apoptosis DNA/RNA Synthesis Cancer
    GEM144 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. GEM144 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. GEM144 has significant antitumor activity in human orthotopic malignant pleural mesothelioma xenografts .
    GEM144
  • HY-13545B
    ABT-510 acetate
    1 Publications Verification

    		 Apoptosis Inflammation/Immunology Cancer
    ABT-510 acetate is an anti-angiogenic TSP peptide (Thrombospondin-1 analogue) that induces apoptosis and inhibits ovarian tumour growth in an orthotopic, syngeneic model of epithelial ovarian cancer. ABT-510 acetate also reduces angiogenesis and inflammatory responses in a murine model of inflammatory bowel disease. ABT-510 acetate can be used in studies of cancer (particularly epithelial ovarian cancer) and inflammatory bowel disease (IBD) .
    ABT-510 acetate
  • HY-P1416A
    Foxy-5 TFA
    Maximum Cited Publications
    7 Publications Verification

    		 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 .
    Foxy-5 TFA
  • HY-172699
    DSPE-PEG2000-ANG

    		Liposome LDLR Cancer
    DSPE-PEG2000-ANG is a conjugate of DSPE-PEG2000-MAL and Angiopep-2. Angiopep-2 is a peptide ligand that targets LRP-1. DSPE-PEG2000-ANG is used to synthesize gadolinium-boron bifunctionalized lipid nanoparticles BPA-F&DOTA-Gd@LIPO-ANG with blood-brain barrier and glioma targeting properties .
    DSPE-PEG2000-ANG
  • HY-P11339
    c-RGD-SH

    		Integrin Cancer
    c-RGD-SH is a ligand for integrin αvβ3 (Integrin αvβ3). Conjugation of c-RGD-SH with core-crosslinked polymeric micelles (CCPM) enables the synthesis of a bimodal nanoprobe, which can be labeled with Cy7 and 111In for SPECT and NIRF imaging of tumors .
    c-RGD-SH
  • HY-W440913
    DSPE-PEG5000-Cy5

    		Liposome Fluorescent Dye Cancer
    DSPE-PEG-Cy5, MW 5000 is a fluorescently labeled PEGylated phospholipid with a molecular weight of 5000 Da. After intravenous injection, DSPE-PEG-Cy5, MW 5000 shows only extremely low fluorescence accumulation at tumor sites in orthotopic tumor-bearing mice, and can be used as a negative control for evaluating tumor accumulation of nanoparticles. DSPE-PEG-Cy5, MW 5000 can serve as a fluorescent marker to prepare Cy5-labeled NPs-DPPA and NPs-DPPA (C3F8) for pharmacokinetic and biodistribution studies in mice. DSPE-PEG-Cy5, MW 5000 is widely applicable to research in fields related to triple-negative breast cancer, hepatocellular carcinoma and so on .
    DSPE-PEG5000-Cy5
  • HY-P11287
    DOTA-Pep-1L

    		Interleukin Related Radionuclide-Drug Conjugates (RDCs) Cancer
    DOTA-Pep-1L is a polypeptide formed by the conjugation of DOTA and Pep-1L. DOTA-Pep-1L specifically binds to IL13RA2 and can be used for the synthesis of targeted polypeptides. DOTA-Pep-1L yields the isotopically labeled product [ 225Ac]DOTA-Pep-1L, which exerts α-radiation killing effects on orthotopic glioma cells and extends the median survival time of mice bearing orthotopic glioma models after stereotactic injection. DOTA-Pep-1L can be used for PET imaging, tumor targeting and glioma research .
    DOTA-Pep-1L
  • HY-P4125
    FITC-LC-TAT (47-57)

    		HIV Fluorescent Dye Infection
    FITC-LC-TAT (47-57) is a FITC-labeled TAT peptide (HY-P0281) (λex: 493 nm, λem: 522 nm). Derived from the trans-activator of transcription (TAT) of human immunodeficiency virus (HIV-1), TAT enhances the yield of heterologous proteins .
    FITC-LC-TAT (47-57)
  • HY-139418
    PX20350

    		FXR Cancer
    PX20350 is a FXR agonist with EC50s of 83 and 10 nM for mFXR and hFXR, respectively. PX20350 significantly induces NDRG2 mRNA expression. PX20350 potently reduces liver tumor cells (SK-GI-18 cells) growth and metastasis, and has anti-tumorigenic activity in orthotopic xenograft mouse models .
    PX20350
  • HY-P991660
    ARGX-111

    		c-Met/HGFR Cancer
    ARGX-111 is an anti-MET antibody. ARGX-111 blocks HGF-dependent and -independent signaling, downregulating MET expression on the tumor cell surface. ARGX-111 depletes MET-expressing circulating tumor cells through enhanced antibody-dependent cell-mediated cytotoxicity (ADCC), thereby inhibiting tumor metastasis. ARGX-111 depletes circulating tumor cells and inhibits bone and lung metastasis in an orthotopic mouse model of metastatic breast cancer. ARGX-111 is promising for research in breast cancer and other cancers .
    ARGX-111
  • HY-178777
    BCL6-760

    		PROTACs BCL6 Cancer
    BCL6-760 is an orally active BCL-6 PROTAC degrader with an EC50 of 0.8 nM. BCL6-760 only degrades BCL6 and has no effect on other CRBN substrates. BCL6-760 demonstrates significant efficacy in the orthotopic xenograft mouse model of OCI-LY-1 tumors. BCL6-760 can be used in the research of diffuse Large B-cell Lymphoma (DLBCL) (Pink: BCL-6 ligand (HY-179317); Blue: CRBN ligand (HY-179305); Black: Linker) .
    BCL6-760
  • HY-175874
    Tubulin-IN-55

    		Microtubule/Tubulin PI3K Akt Apoptosis Cancer
    Tubulin-IN-55 is a tubulin inhibitor. Tubulin-IN-55 disrupts the PI3K/Akt signaling pathway in cancer cells. Tubulin-IN-55 exerts broad-spectrum anti-proliferative activity against multiple tumor cells (HeLa, HCT116, 4T1, A549, H1299, MDA-MB231). Tubulin-IN-55 induces G2/M phase arrest and apoptosis, and inhibits tumor cell migration/invasion in cancer cells. Tubulin-IN-55 demonstrates potent antitumor efficacy in orthotopic autologous transplantation mice. Tubulin-IN-55 can be used for the study of cancer .
    Tubulin-IN-55
  • HY-P991229
    MK-4721

    AGS-1C4D4; AGS-PSCA

    		 Complement System Cancer
    AGS-1C4D4 is a fully human IgG1κ monoclonal antibody targeting PSCA, with a Ka value of 0.2 nM. AGS-1C4D4 mediates antibody-dependent cellular cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC) against PSCA-expressing cells. AGS-1C4D4 can be used for the research of pancreatic cancer .
    MK-4721
  • HY-163121
    PST3.1a

    		Glycosyltransferase TGF-β Receptor FAK Galectin Collagen Endocrinology Cancer
    PST3.1a is an orally active and brain-penetrant N-acetylglucosamine glycosyltransferase (MGAT5) inhibitor with a human IC50 of 2 µM. PST3.1a inhibits TGFβR and FAK signaling pathway activity. PST3.1a alters β1,6-GlcNAc N-glycans and microtubule/microfilament integrity, increases OLIG2 expression, and inhibits proliferation, migration, invasiveness, and clonogenic capacities of glioblastoma initiating cells. PST3.1a reduces invasive and proliferative capacity of glioblastoma initiating cells in orthotopic graft models, increases overall survival of orthotopic graft model mice. PST3.1a blunts MGAT5 overexpression, decreases renal fibrosis via collagen 1, collagen 4, and galectin 3 downregulation in a rat chronic kidney disease model. PST3.1a can be used for the research of glioblastoma multiforme and chronic kidney disease .
    PST3.1a
  • HY-122844B
    Ifebemtinib tosylate

    BI-853520 tosylate; IN-10018 tosylate

    		 FAK Cancer
    Ifebemtinib (tosylate) (BI-853520 (tosylate); IN-10018 (tosylate)) is a highly selective PTK2 kinase inhibitor. Ifebemtinib (tosylate) demonstrates anti-tumor activity. Ifebemtinib (tosylate) inhibits FAK autophosphorylation in prostate carcinoma cells. Ifebemtinib (tosylate) can inhibit spheroid formation and orthotopic tumor growth in vivo. Ifebemtinib (tosylate) can be studied in anticancer research such as solid tumors, breast cancer, and malignant pleural mesothelioma .
    Ifebemtinib tosylate
  • HY-173116
    DOTA-XYIMSR-01

    		Carbonic Anhydrase Cancer
    DOTA-XYIMSR-01 is a molecular probe targeting CAIX that can be labeled with 177Lu for the inhibition and localization of malignant gliomas. The uptake of [177Lu] Lu-XYIMSR-01 in U87MG tumors is 6.19 % of the injected dose per gram (% ID/g), and the tumor-to-muscle uptake ratio is 20.14. In the orthotopic glioma model, combined injection with Temozolomide (HY-17364) can significantly improve the survival rate of mice and inhibit tumor growth. DOTA-XYIMSR-01 shows promise for research in the field of anti-cancer therapy .
    DOTA-XYIMSR-01
  • HY-13654
    IPI-269609

    		Smo Hedgehog Cancer
    IPI-269609 is an orally effective Smoothed (SMO) inhibitor that targets the Hedgehog (Hh) signaling pathway. IPI-269609 specifically reduces the ALDH-bright (high aldehyde dehydrogenase activity) cell subset, which is considered the "cancer stem cells" in pancreatic cancer. IPI-269609 significantly inhibits the migration and colony formation of pancreatic cancer cells. IPI-269609 effectively inhibits pancreatic cancer metastasis in a mouse model. IPI-269609 can be used for pancreatic cancer research .
    IPI-269609
  • HY-12401A
    Mps1-IN-3 hydrochloride
    1 Publications Verification

    		 Mps1 Cancer
    Mps1-IN-3 hydrochloride is a potent and selective Mps1 inhibitor with an IC50 value of 50 nM. Mps1-IN-3 hydrochloride can inhibit the proliferation of glioblastoma cells, and effectively sensitizes glioblastomas to Vincristine in orthotopic glioblastoma xenograft model .
    Mps1-IN-3 hydrochloride
  • HY-155249
    KGP591

    		Microtubule/Tubulin Cancer
    KGP591 is a tubulin polymerization inhibitor (IC50 0.57 µM). KGP591 induces significant G2/M stagnation, inhibits cell migration, disrupts microtubule structure and cell morphology in MDA-MB-231 cells. KGP591 shows antitumor activity in orthotopic model of kidney cancer (RENCA) .
    KGP591
  • HY-16726R
    Polmacoxib (Standard)

    CG100649 (Standard)

    		 Reference Standards COX Carbonic Anhydrase Cancer
    Polmacoxib (Standard) is the analytical standard of Polmacoxib. This product is intended for research and analytical applications. Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory agent (NSAID) which is a dual inhibitor of COX-2 (IC50 around 0.1 μg/ml) and carbonic anhydrase . Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models .
    Polmacoxib (Standard)
  • HY-173433
    JV8

    		Epigenetic Reader Domain Cancer
    JV8 is a BRD4 PROTAC degrader. JV8 promotes the ubiquitination and degradation of BRD4 and induces apoptosis. JV8 has antitumor activity in a mouse 4T1 orthotopic tumor model. (Pink: BRD4 ligand (HY-78695); Blue: E3 ligase VHL ligand (HY-173435); Black: Linker (HY-33366); E3 ligase VHL ligand-linker conjugate (HY-173436)) .
    JV8
  • HY-149036
    PAA5

    		Ferroptosis Endogenous Metabolite Reactive Oxygen Species (ROS) Cancer
    PAA5 is a methide carbon-centered polynuclear Au(I) cluster. PAA5 can release Au(I) causing Pro-oxidant response and accelerated ferroptosis. PAA5 increases the expression of pH2AX in a time-dependent manner. PAA5 has anticancer activity .
    PAA5
  • HY-161954
    HDAC8-IN-12

    		HDAC Cancer
    HDAC8-IN-12 (compound 5k) is a non-hydroxamic acid, selective inhibitor of HDAC8 (IC50: 0.12 nM) and a potent inhibitor of breast cancer. HDAC8-IN-12 triggers anti-tumor immunity by activating T cells, increasing the proportion of M1 macrophages and decreasing the proportion of M2 macrophages. HDAC8-IN-12 (50 mg/kg) exerts tumor suppressive effects in an orthotopic mouse model of breast cancer .
    HDAC8-IN-12
  • HY-170321
    Apoptosis inducer 31

    		Apoptosis Cancer
    Apoptosis inducer 31 (compound 19) induces caspase-dependent apoptosis. Apoptosis inducer 31 plays an important role in cancer research .
    Apoptosis inducer 31
  • HY-162494
    PAD4-IN-4

    		Protein Arginine Deiminase Cancer
    PAD4-IN-4 (compound 28) is a potent PAD4 inhibitor (IC50=0.79±0.09 μM). PAD4-IN-4 improves the tumor immune microenvironment by reshaping neutrophil phenotype, upregulating the proportions of dendritic cells and M1 macrophages, and reducing the amount of myeloid-derived suppressor cells. PAD4-IN-4 can be used for Triple-negative breast cancer research .
    PAD4-IN-4
  • HY-163434
    PRMT5/EGFR-IN-1

    		EGFR Histone Methyltransferase Cancer
    PRMT5/EGFR-IN-1 (Compound 10p) is an orally active dual PRMT5/EGFR inhibitor, with IC50s of 15.47 and 19.31 μM, respectively. PRMT5/EGFR-IN-1 exhibits antiproliferative activity against A549, MCF7, HeLa, and MDA-MB-231 cell lines. PRMT5/EGFR-IN-1 has favorable in vivo PK and PD properties. PRMT5/EGFR-IN-1 can significantly inhibit the growth of MCF7 orthotopic xenograft tumors .
    PRMT5/EGFR-IN-1
  • HY-116504
    WB-308

    		EGFR Akt ERK Apoptosis Cancer
    WB-308 is a novel small molecule that was identified as an inhibitor of EGFR by an in vitro EGFR kinase activity system. WB-308 was able to reduce the proliferation and clonogenicity of NSCLC cells, causing G2/M phase arrest and apoptosis. In addition, WB-308 inhibited tumor growth in two in vivo animal models (lung orthotopic transplantation model and patient-derived clonal mouse model). WB-308 impaired the phosphorylation of EGFR, AKT, and ERK1/2 proteins. Compared with Gefitinib, WB-308 had lower cytotoxicity. This study showed that WB-308 is a new EGFR-TKI that may be considered as an alternative to Gefitinib in the clinical treatment of NSCLC.
    WB-308
  • HY-N4189
    Isocucurbitacin B

    		PI3K Akt p38 MAPK STAT Apoptosis Cancer
    Isocucurbitacin B is a natural terpenoid compound found in Pedicellus Melo. Isocucurbitacin B can inhibit the PI3K/AKT, MAPK, and STAT3 signaling pathways and downregulate CAV1 expression. Isocucurbitacin B can inhbit cancer cell proliferation, migration and invision. Isocucurbitacin B can induce apoptosis and cause G2/M phase arrest. Isocucurbitacin B can decrease intracellular cholesterol and PH levels and increase intracellular calcium levels. Isocucurbitacin B can be used for the research of cancer, such as glioma [1][2].
    Isocucurbitacin B
  • HY-149035
    PAA4

    		Others Cancer
    PAA4 is a methide carbon-centered polynuclear Au(I) clusters. PAA4 shows antiproliferative activity. PAA4 increases the expression of pH2AX in a time dependent manner. PAA4 shows anti-tumor effect in orthotopic bladder cancer mouse model .
    PAA4
  • HY-181073
    Apoptosis/necroptosis inducer 1

    		Apoptosis Necroptosis NF-κB p38 MAPK Neurological Disease Cancer
    Apoptosis/necroptosis inducer 1 is an orally active and brain-penetrant apoptosis and necroptosis inducer. Apoptosis/necroptosis inducer 1 induces mitochondria-dependent (intrinsic pathway) apoptosis. Apoptosis/necroptosis inducer 1 induces necroptosis by activating the TNF-α/NF-κB/MAPK signaling pathway. Apoptosis/necroptosis inducer 1 exhibits antiproliferative activity in glioblastoma cell lines and multiple solid tumor types. Apoptosis/necroptosis inducer 1 inhibits growth of orthotopic glioblastoma in animal models and improves survival rate. Apoptosis/necroptosis inducer 1 can be used for the research of glioblastoma .
    Apoptosis/necroptosis inducer 1
  • HY-181789
    DOT1L808

    		PROTACs Histone Methyltransferase Cancer
    DOT1L808 is a potent and highly selective DOT1L PROTAC degrader with a DC50 value of 5 nM. DOT1L808 can promote the ubiquitination and degradation of DOT1L. DOT1L808 exhibits antitumor activity in an orthotopic leukemia model .
    DOT1L808

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