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NSG mouse

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16

Inhibitors & Agonists

1

Inhibitory Antibodies

1

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P2989
    Pyruvate carboxylase

    		Endogenous Metabolite Metabolic Disease Cancer
    Pyruvate carboxylase is a key mitochondrial anaplerotic enzyme that catalyzes the conversion of pyruvate to oxaloacetate. Pyruvate carboxylase not only maintains tricarboxylic acid cycle activity and redox homeostasis, but also drives hepatic gluconeogenesis and fatty acid synthesis. The activity of Pyruvate carboxylase is upregulated in insulin-resistant states, exacerbating hepatic glucose production. Pyruvate carboxylase also shows significantly enhanced expression in early-stage non-small cell lung cancer (NSCLC). Pyruvate carboxylase promotes tumor proliferation by supporting nucleotide and lipid synthesis, and its functional deficiency cannot be compensated by glutaminolysis. Pyruvate carboxylase can be used in the research of prediabetes type 2 and NSCLC .
    Pyruvate carboxylase
  • HY-109179
    Itacnosertib

    TP-0184

    		 JAK Anaplastic lymphoma kinase (ALK) FLT3 STAT PI3K Akt mTOR TGF-beta/Smad TGF-β Receptor Cancer
    Itacnosertib (TP-0184) is the inhibitor for FLT3, ACVR1 (ALK2, IC50=8 nM) and JAK2 (IC50=8540 nM). Itacnosertib exhibits anti-leukemic activity .
    Itacnosertib
  • HY-175370
    PROTAC RIPK1 Degrader-1

    		PROTACs RIP kinase Cancer
    PROTAC RIPK1 Degrader-1 is a selective RIPK1 PROTAC degrader. PROTAC RIPK1 Degrader-1 degrades RIPK1 in multiple cancer cell lines (e.g., A375, B16F10 cells). PROTAC RIPK1 Degrader-1 enhances the anti-cancer effect of radiotherapy in syngeneic and humanized mouse models. PROTAC RIPK1 Degrader-1 can be used to study cancers such as melanoma. (Pink: RIPK1-ligand-2: HY-175371, Blue: (S,R,S)-AHPC-Me: HY-112078, Pink + Black: RIPK1 ligand-Linker Conjugate-1: HY-175374, Black: Bispiperidin-piperazin-acetater: HY-175373) .
    PROTAC RIPK1 Degrader-1
  • HY-178775
    PI4K-IN-3

    		PI4K Parasite MAP4K PI3K Infection
    PI4K-IN-3 (Compound 27) is an orally active PI4K inhibitor with an IC50 of 1.9  nM for Plasmodium vivax PI4K. PI4K-IN-3 has no hERG channel inhibition and mammalian cytotoxicity. PI4K-IN-3 has significant selectivity against the human MINK1 and MAP4K4 kinases but with low selectivity against human PI3Kα and PI4Kβ. PI4K-IN-3 has potent antimalarial activity and significantly reduces parasitaemia in NSG mice mouse models of Plasmodium falciparum malaria .
    PI4K-IN-3
  • HY-170453
    iHAC

    		Epigenetic Reader Domain Cancer
    iHAC is an inhibitor HSP90-anchoring chimera, that covalently binds BRD4 ligand (+)-JQ-1 to HSP90, and inhibits the proliferation of cancer cells. iHAC activates the anti-tumor immune response, inhibits the recurrence and metastasis of 4T1 breast cancer in mouse models .
    iHAC
  • HY-162343
    PD-1/PD-L1-IN-41

    		PD-1/PD-L1 Inflammation/Immunology Cancer
    PD-1/ PD-L1-in-41 (Compound 5c) is a PD-L1 and PD-1 inhibitor with IC50 value of 10.2 nM .
    PD-1/PD-L1-IN-41
  • HY-148178
    MMV688533

    		Parasite Infection
    MMV688533 is an antimalarial agent. MMV688533 interferes with intracellular trafficking, lipid utilization, and endocytosis pathways in Plasmodium falciparum. MMV688533 rapidly kills asexual blood-stage Plasmodium falciparum and Plasmodium vivax parasites in vitro and reduces parasitemia in a Plasmodium falciparum NSG mouse model. MMV688533 can be used for the research of malaria .
    MMV688533
  • HY-163765
    Antimalarial agent 41

    		PI4K Potassium Channel Infection
    Antimalarial agent 41 (Compound 17) exhibits antimalarial activity, which inhibits Plasmodium falciparum with an IC50 of 40 nM (NF54 strain) and 76 nM (K1 strain). Antimalarial agent 41 is an inhibitor for P. falciparum phosphatidylinositol-4-kinase β (Pf PI4K) and hERG channel, with an IC50 of 53 nM and 3 μM. Antimalarial agent 41 exhibits cytotoxicity to CHO cells with an IC50 of 34 μM. Antimalarial agent 41 ameliorates the malaria infection and exhibits good pharmacokinetic characters in mouse models .
    Antimalarial agent 41
  • HY-172953
    Insecticidal agent 24

    		Parasite Infection
    Insecticidal agent 24 is an orally active pyridylspiroindoline frontrunner. Insecticidal agent 24 has antiplasmodial activity (Pf NF54 IC50: 0.08 μM). Insecticidal agent 24 inhibits hERG activity (IC50: 6.5 μM). Insecticidal agent 24 reduces parasitemia in a humanized immunodeficient NSG mouse Plasmodium falciparum infection model .
    Insecticidal agent 24
  • HY-156920
    VDX-111

    		Necroptosis RIP kinase Inflammation/Immunology Cancer
    VDX-111 is an analog of vitamin D. VDX-111 exhibits cytotoxicity in ovarian cancer cells through upregulation of RIPK1/RIPK3 pathway and induction of necroptosis. VDX-111 promotes expressions of cytokines and exhibits antitumor activity in mouse model .
    VDX-111
  • HY-163538
    TYM-3-98

    		PI3K Apoptosis Cancer
    TYM-3-98 is a selective inhibitor for PI3Kδ, with an IC50 of 7.1 nM. TYM-3-98 inhibits proliferationso of B-lymphoma cells. TYM-3-98 inhibits PI3K/AKT/mTOR signaling pathway through induction of apoptosis. TYM-3-98 exhibits good pahrmacokinetic characters and antitumor efficacy in mouse/rat model, without significant toxicity .
    TYM-3-98
  • HY-101266A
    Milademetan tosylate

    DS-3032 tosylate

    		 MDM-2/p53 Cancer
    Milademetan tosylate is the tosylate salt form of Milademetan (HY-101266). Milademetan tosylate is an orally active inhibitor for MDM2. Milademetan tosylate arrests the cell cycle at G1 pahse, induces the apoptosis Milademetan tosylate restores the p53 activity by targeting the p53-MDM2 interaction, and exhibits anticancer activity against Merkel cell carcinoma (MCC) .
    Milademetan tosylate
  • HY-181260
    PRMT5-MTA-IN-8

    		Histone Methyltransferase Apoptosis Cancer
    PRMT5-MTA-IN-8 is an orally active PRMT5-MTA complex inhibitor (IC50 = 4.4 nM). PRMT5-MTA-IN-8 inhibits the intracellular production of symmetric dimethylarginine (SDMA) as well as the proliferation of MTAP-deficient cells. PRMT5-MTA-IN-8 exerts antitumor efficacy by inhibiting PRMT5, reducing SDMA levels and inducing tumor cell apoptosis in mouse models of triple-negative breast cancer. PRMT5-MTA-IN-8 can be used in research related to cancers such as triple-negative breast cancer .
    PRMT5-MTA-IN-8
  • HY-181849
    MS2928

    		Histone Methyltransferase Cancer
    MS2928 is a selective SETD8 inhibitor with an IC50 of 0.14 μM against SETD8 methyltransferase activity. MS2928 reduces cellular H4K20me1 levels and inhibits proliferation of SETD8-overexpressing multiple myeloma cells. MS2928 inhibits tumor growth in xenograft mouse models of SETD8-overexpressing multiple myeloma. MS2928 can be used for the study of SETD8 biological functions and multiple myeloma .
    MS2928
  • HY-182685
    MMV693183

    		Acetyl-CoA synthetase Parasite Infection
    MMV693183 is an orally active inhibitor of Plasmodium falciparum acetyl-CoA synthetase (AcAS), with an IC50 of 300 nM against Plasmodium falciparum. MMV693183 exhibits potent inhibitory activity against clinical isolates of malaria parasites, including Artemisinin (HY-B0094)-resistant strains. MMV693183 is metabolized in vivo into the active antimetabolite CoA-MMV693183, which exerts effects of killing asexual blood-stage parasites and blocking transmission to Anopheles mosquitoes by binding to and inhibiting the function of acetyl-CoA synthetase, thereby reducing the levels of acetyl-CoA and 4'-phosphopantetheine. In humanized mouse models, MMV693183 shows favorable in vivo efficacy, drug-like properties, and no significant cytotoxicity or off-target activity against human cells. MMV693183 is widely used in malaria-related research as a parasiticide and metabolic disruptor .
    MMV693183
  • HY-P991896
    AT1412

    AT14-012

    		 Transmembrane Glycoprotein Inflammation/Immunology Cancer
    AT1412 is a CD9-binding antibody. AT1412 binds to the tetraspanin protein CD9 and modulates CD9 function by enhancing T cell adhesion to endothelial cells (HUVECs) and transendothelial migration. AT1412 binds to B-ALL cell lines but not to T-ALL. AT1412 induces antibody-dependent cellular cytotoxicity in B-ALL cell lines. AT1412 binds to melanoma cells, B-ALL, gastric cancer, colorectal cancer, and pancreatic cancer cells [1] .
    AT1412

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