Search Result
Results for "
syngeneic mouse models
" in MedChemExpress (MCE) Product Catalog:
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-136927
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MSA-2
Maximum Cited Publications
30 Publications Verification
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STING
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Inflammation/Immunology
Cancer
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MSA-2, a potent and orally available non-nucleotide STING agonist, is bound to STING as a noncovalent dimer with nanomolar affinity. MSA-2 shows EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models .
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- HY-114409
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Galectin
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Cancer
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GB1107 is a potent, selective, orally active inhibitor of Galectin-3 (Gal-3) with a Kd of 37 nM for human Galectin-3. GB1107 reduces human and mouse lung adenocarcinoma growth and blocks metastasis in the syngeneic model .
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- HY-152830
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Q702
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c-Fms
TAM Receptor
MHC
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Cancer
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Adrixetinib (Q702) is an orally active triple inhibitor against CSF1R, Mer, and Axl, with Kd values of 8.7 nM, 0.8 nM, and 0.3 nM, respectively. Adrixetinib acts as a potent immune modulator that remodels the tumor microenvironment. Adrixetinib increases the abundance of M1 macrophages and CD8⁺ T cells, while decreasing the levels of M2 macrophages and myeloid-derived suppressor cells (MDSCs). Adrixetinib upregulates the expression of MHC class I and E-cadherin in tumor cells. Adrixetinib shows remarkable antitumor efficacy in syngeneic mouse tumor models. Adrixetinib is suitable for the research of breast cancer, renal adenocarcinoma, colon carcinoma, and melanoma .
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- HY-119357
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Microtubule/Tubulin
Apoptosis
Autophagy
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Neurological Disease
Cancer
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TN-16 is a Microtubule polymerization inhibitor. TN-16 induces G2/M cell cycle arrest, metaphase mitotic arrest and Apoptotic cell death in cells, and blocks late Autophagic flux by inhibiting autophagosome-lysosome fusion. TN-16 suppresses tumor growth in syngeneic mouse breast cancer models. TN-16 can be used in research related to neuroblastoma, cervical cancer, breast cancer and other tumors .
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- HY-137655
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Protein Arginine Deiminase
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Cancer
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BMS-P5 is a selective and orally active peptidylarginine deiminase 4 (PAD4) inhibitor with an IC50 of 98 nM. BMS-P5 shows selective for PAD4 over PAD1, PAD2, and PAD3. BMS-P5 blocks multiple myeloma (MM)-induced neutrophil extracellular trap (NET) formation and delays progression of MM in a syngeneic mouse model .
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- HY-137655A
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Protein Arginine Deiminase
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Cancer
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BMS-P5 free base is a selective and orally active peptidylarginine deiminase 4 (PAD4) inhibitor with an IC50 of 98 nM. BMS-P5 free base shows selective for PAD4 over PAD1, PAD2, and PAD3. BMS-P5 free base blocks multiple myeloma (MM)-induced neutrophil extracellular trap (NET) formation and delays progression of MM in a syngeneic mouse model .
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- HY-170510
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Galectin
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Cancer
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GB2095 is an orally active and selective galectin-3 inhibitor. GB2095 shows superior selectivity for both human (KD = 0.036 μM) and mouse galectin-3 (KD = 0.35 μM) over other galectins (such as h-Gal-1/4N/4C/8N/8C/9N/9C and m-galectin-1). GB2095 inhibits tumor growth in syngeneic mouse models of breast and melanoma cancers. GB2095 can be used for breast and melanoma cancer research .
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- HY-144088
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ZYF0033
2 Publications Verification
HPK1-IN-22
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MAP4K
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Inflammation/Immunology
Cancer
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ZYF0033 is an orally active inhibitor of the hematopoietic progenitor cell kinase HPK1 with an IC50 of less than 10 nM based on the phosphorylation inhibition of MBP protein. ZYF0033 promotes anti-cancer immune responses and reduces phosphorylation of SLP76 (serine 376). ZYF0033 inhibits tumor growth in the 4T-1 syngeneic mouse model and leads to increased intratumoral infiltration of DCs, NK cells, and CD107a +CD8 + T cells, but not T cells, PD-1 +CD8 + T cells, TIM-3 +CD8 + Infiltration of T cells and LAG3 +CD8 + T cells was reduced .
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- HY-175370
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PROTACs
RIP kinase
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Cancer
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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) .
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- HY-163081
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PARP
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Cancer
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PARP7-IN-17 is a potent inhibitor of PARP7 with IC50 of 4.5 nM that has oral bioavailability. PARP7-IN-17 displays antitumor effect .
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- HY-163719
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PARP
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Cancer
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PARP7-IN-22 (XLY-1) is a PARP7 inhibitor with an IC50 of 0.6 nM. PARP7-IN-22 (XLY-1) is orally active, enhances type I interferon signaling in vitro, restores type I interferon signaling, promotes T cell infiltration into tumor tissues, and significantly inhibits tumor growth. PARP7-IN-22 shows promise for research in the field of cancer immunotherapy .
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- HY-149667
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DGK
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Cancer
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BMS-332 is a dual DGKα/ζ lipid kinase inhibitor, with IC50s of 5 and 1 nM against DGKα and DGKζ, respectively. BMS-332 enhances the antigen-specific T cell response. BMS-332 reduces the viral load in the liver and spleen when combined with anti-PD-1 in chronic infection models. BMS-332 can be used for the study of T cell immune checkpoint strategy .
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- HY-175478
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Phosphodiesterase (PDE)
STING
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Inflammation/Immunology
Cancer
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Enpp-1-IN-27 is a selective ENPP1 inhibitor with an IC50 of 14.68 nM, exhibiting approximately 410-fold selectivity against ENPP2 and 10-fold selectivity against ENPP3. Enpp-1-IN-27 stabilizes cGAMP levels and activates the STING pathway, promoting cytokine release and enhancing innate immune responses. Enpp-1-IN-27 induces ISRE activation and amplified cGAMP-mediated immune responses and shows the desired antitumor efficacy in the 4T1 and CT26 syngeneic mouse models. Enpp-1-IN-27 can used for the studies of breast cancer and colon cancer .
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- HY-145239
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PD-1/PD-L1
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Cancer
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PD-1/PD-L1-IN-13 (Compound 43) is a potent immune checkpoint PD-1/PD-L1 inhibitor with an IC50 value of 10.2 nM. PD-1/PD-L1-IN-13 promots CD8 + T cell activation and delays the tumor growth in the Hepa1-6 syngeneic mouse model .
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- HY-178716
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Phosphatase
IFNAR
STAT
JAK
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Cancer
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PTPN2/1-IN-4 (Compound WS35) is an orally active, dual-functional inhibitor of PTPN1 and PTPN2 with IC50s of 12.8 and 5.8 nM for PTPN1 and PTPN2, respectively. PTPN2/1-IN-4 modulates the IFNγ-JAK-STAT signaling pathway and significantly augments CD8+ T-cell tumor infiltration. PTPN2/1-IN-4 has potent anticancer activity, robustly inhibiting tumor growth both as a monotherapy and in combination with an anti-PD-1 antibody in B16-OVA syngeneic mouse models .
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- HY-179578
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Enolase
AMPK
Autophagy
Apoptosis
mTOR
Caspase
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Metabolic Disease
Cancer
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SU212 is a podophyllotoxin-derived ENO1 inhibitor and AMPK activator. SU212 can selectively induce oxidative phosphorylation, reduce glycolysis activity and glucose uptake in tumor cells, and directly bind to ENO1 without affecting these pathways in normal cells. SU212 induces apoptosis and promotes ENO1 degradation via proteasomal and autophagic pathways without inhibiting the catalytic activity. SU212 leads to mitotic arrest and apoptosis in TNBC (triple-negative breast cancer) cells by activating AMPK, demonstrating potent anti-tumor activity in vitro. SU212 inhibits tumor growth and metastasis in syngeneic, xenograft, and diabetic mouse models, exhibiting an excellent safety profile. SU212 can be used in research on t TNBC, diabetes, and fatty liver disease .
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- HY-149666
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DGK
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Cancer
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BMS-496 is adualDGKα/ζlipid kinase inhibitor, with theIC50of 0.09 (DGKα) and 0.006 μM (DGKζ) .
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- HY-152830A
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Q702 TFA
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c-Fms
TAM Receptor
MHC
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Cancer
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Adrixetinib (Q702) TFA is an orally active triple inhibitor against CSF1R, Mer, and Axl, with Kd values of 8.7 nM, 0.8 nM, and 0.3 nM, respectively. Adrixetinib TFA acts as a potent immune modulator that remodels the tumor microenvironment. Adrixetinib TFA increases the abundance of M1 macrophages and CD8⁺ T cells, while decreasing the levels of M2 macrophages and myeloid-derived suppressor cells (MDSCs). Adrixetinib TFA upregulates the expression of MHC class I and E-cadherin in tumor cells. Adrixetinib TFA shows remarkable antitumor efficacy in syngeneic mouse tumor models. Adrixetinib TFA is suitable for the research of breast cancer, renal adenocarcinoma, colon carcinoma, and melanoma .
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- HY-P991181
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Transmembrane Glycoprotein
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Cancer
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VTX-1218 is a VSIG4 inhibitor with human Kd 7.4 nM. VTX-1218 blocks VSIG4 activity, relieves VSIG4-mediated macrophage suppression, repolarizes tumor-associated macrophages and induces T cell activation. VTX-1218 upregulates cytokines and chemokines linked to immune cell recruitment. VTX-1218 can be used for the research of multiple cancer types .
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- HY-P991004
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LB-101
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CD47
PD-1/PD-L1
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Cancer
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Itanistomig (LB-101) is a tetravalent bispecific antibody targeting PD-L1 and CD47. Itanistomig blocks PD-L1 and achieves tumor enrichment through binding to PD-L1, and also exerts conditional CD47 blocking activity via cleavage of the hinge linker in the PD-L1-positive tumor microenvironment. Itanistomig induces antibody-dependent cellular phagocytosis in human CD14 + cells and drives tumor regression. Itanistomig can be used in research related to solid tumors .
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- HY-129085
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C5OH
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Drug Derivative
Apoptosis
NF-κB
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Cancer
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5-Methyl cromolyn (C5OH) disodium, an analog of Cromolyn (HY-B1619), is a S100P inhibitor. 5-Methyl cromolyn disodium inhibits the binding of S100P to its receptor RAGE, NF-κB activity and cell proliferation, and promotes Gemcitabine (HY-17026)-induced apoptosis. 5-Methyl cromolyn disodium reduces tumor growth and metastasis, and prolongs survival in mouse models of syngeneic PDAC. 5-Methyl cromolyn disodium can be used for pancreatic cancer like pancreatic ductal adenocarcinoma (PDAC) research .
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- HY-172453
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Indoleamine 2,3-Dioxygenase (IDO)
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Cancer
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XW-032 is an apo-IDO1 inhibitor, with an IC50 of 21 nM. XW-032 (TGI = 63%) exhibits potent in vivo anti-tumor efficacy in the CT26 syngeneic mouse model and is expected to be applied in the research of the field of cancer .
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- HY-162554
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CD73
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Inflammation/Immunology
Cancer
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CD73-IN-15 (compound 12f) is a potent inhibitor of CD73, with the IC50 of 60 nM. CD73-IN-15 plays an important role in cancer research .
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- HY-P991468
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Interleukin Related
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Cancer
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IMM20324 is a human monoclonal antibody (mAb) targeting IL38. IMM20324 inhibits the interaction of IL-38 with human IL1RAPL1-Fc and human IL-36R-Fc with IC50 values of 1.267 nM and 1.4667 nM, respectively. IMM20324 has antitumor activity in the B16.F10 syngeneic mouse model. IMM20324 can be used in antitumor immunity research. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
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- HY-150609
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SHP2
Phosphatase
CDK
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Cancer
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SHP2/CDK4-IN-1 (compound 10) is an orally active and potent SHP2 and CDK4 dual inhibitor, with IC50 values of 4.3 and 18.2 nM, respectively. SHP2/CDK4-IN-1 effectively induces G0/G1 arrest to prevent the proliferation of TNBC cell lines. SHP2/CDK4-IN-1 shows significant antitumor efficacy in the EMT6 syngeneic mouse model. SHP2/CDK4-IN-1 can be used for triple-negative breast cancer (TNBC) research .
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- HY-175547
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PROTACs
MAP4K
ERK
Interleukin Related
IFNAR
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Inflammation/Immunology
Cancer
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PROTAC HPK1 Degrader-5 is a potent and orally active HPK1 PROTAC degrader (DC50 = 5.0 nM; Dmax ≥ 99%). PROTAC HPK1 Degrader-5 significantly inhibits SLP76 phosphorylation and enhanced ERK pathway activation through degrading HPK1, thereby stimulating IL-2 and IFN-γ release. PROTAC HPK1 Degrader-5 exhibits the ability to overcome the immunosuppressive effects imposed by PGE2, NECA or TGF-β. PROTAC HPK1 Degrader-5 alone efficaciously inhibits tumor growth in an MC38 syngeneic mouse model. PROTAC HPK1 Degrader-5 can be used for the study of tumor (such as colorectal cancer) immunotherapy (Pink: Target protein ligand (HY-175549); Blue: E3 ligand (HY-W023573); Black: Linker; E3 ligand + Linker (HY-175551)) .
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- HY-185098
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PD-1/PD-L1
Transmembrane Glycoprotein
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Cancer
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PD1-PDL1-IN-4 (compound 19) is a potent and orally active PD1-PDL1 inhibitor that modulates TIGIT and PD-1 signalling pathways. PD1-PDL1-IN-4 can rescue CD8 + T cell and mouse splenocyte proliferation. PD1-PDL1-IN-4 inhibits tumor growth in a CT26 syngeneic colon adenocarcinoma mouse model. PD1-PDL1-IN-4 can be used for research on colon cancer .
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- HY-181932
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MAP4K
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Cancer
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HDM2004 is a selective, orally active, blood-brain barrier-penetrant HPK1 inhibitor with an IC50 of 1.89 nM. HDM2004 exhibits anticancer activity against colon cancer. HDM2004 shows synergistic activity when combined with anti-PD-L1 in syngeneic mouse models. HDM2004 can be used for the research of colon cancer .
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- HY-181484
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STING
IKK
IFNAR
Interleukin Related
CXCR
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Cancer
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STING agonist-50 is an orally active STING agonist with an IC50 of 3.457 μM. STING agonist-50 activates the STING signaling pathway and promotes the phosphorylation of downstream TBK1 and IRF3. STING agonist-50 induces the expression of IFN-β, CXCL10 and IL-6. STING agonist-50 inhibits tumor growth in syngeneic mouse models. STING agonist-50 can be used for the research of colorectal cancer .
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- HY-181667
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Phosphodiesterase (PDE)
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Cancer
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Enpp-1-IN-30 (compound 44a) is an orally bioavailable ENPP1 inhibitor with a human IC50 of 13.1 nM. Enpp-1-IN-30 prevents cGAMP degradation, activates the STING pathway. Enpp-1-IN-30 induces cytokine release to enhance innate immune response. Enpp-1-IN-30 exerts antitumor efficacy in syngeneic mouse models. Enpp-1-IN-30 can be used for the research of colon carcinoma .
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- HY-182238
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MAP4K
Interleukin Related
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Cancer
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HPK1-IN-69 is an orally active HPK1 inhibitor with an IC50 of 1.7 nM. HPK1-IN-69 inhibits the HPK1-mediated TCR signaling pathway, reduces the phosphorylation level of SLP76, and promotes the release of IL-2. HPK1-IN-69 exhibits in vivo anti-tumor activity in mouse models. HPK1-IN-69 can be used for the research of colorectal cancer and MC38 syngeneic tumors .
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- HY-P992352
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ES005 is an anti-tumor compound and LAG3 inhibitor. ES005 blocks the interactions of LAG3 with MHC-II, LSECtin and FGL1, thereby effectively reversing the LAG3-mediated inhibition of T cell activation and NFAT reporter gene expression. ES005 exhibits significant tumor growth inhibitory effects in syngeneic mouse breast tumor models using humanized LAG3 knock-in mice. ES005 can be used for breast tumor-related research .
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- HY-P991960
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CTLA-4
Interleukin Related
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Cancer
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JS007 is a humanized IgG1 monoclonal antibody and also a CTLA-4 binder, with a Kd of 0.21 nM for CTLA-4. JS007 blocks the interaction between CTLA-4 and B7-1. JS007 activates T cells, promotes increased IL-2 secretion, and inhibits tumor growth in CTLA-4 knock-in mouse syngeneic tumor models. JS007 is applicable to research related to cancer and advanced solid tumors.
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- HY-182242
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c-Myc
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Cancer
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AGB-374 is an orally active NDUFS7 inhibitor. AGB-374 destabilizes NDUFS7 protein and inhibits oxidative phosphorylation by targeting mitochondrial complex I. AGB-374 reduces MYC protein levels in colon cancer cells in vivo and delays tumor growth in syngeneic mouse models of colon cancer. AGB-374 synergistically enhances the cytotoxicity of copper chelators against cancer cells. AGB-374 cooperates with copper chelators to downregulate MYC and NDUFS7 protein levels in cancer cells. AGB-374 can be used for the research of colon cancer .
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- HY-182241
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c-Myc
Early 2 Factor (E2F)
TNF Receptor
MDM-2/p53
Reactive Oxygen Species (ROS)
Apoptosis
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Cancer
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JR4-187 is an orally active, copper-dependent anticancer agent. JR4-187 downregulates genes involved in oxidative phosphorylation, MYC targets and E2F targets in cancer cells, while upregulates genes involved in the TNF-α signaling pathway, p53 pathway and KRAS signaling pathway, and downregulates CTR1 protein . JR4-187 induces ROS production, apoptosis, copper-dependent cytotoxicity, and exhibits selective cytotoxicity against KRAS-mutant cancer cells. JR4-187 is well tolerated in mouse models of pancreatic cancer. JR4-187 can be used in research related to cancers such as pancreatic ductal adenocarcinoma, colon cancer and rectal cancer .
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- HY-P991864
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MDX-124
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Formyl Peptide Receptor (FPR)
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Cancer
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Annexuzlimab is a humanised IgG1 monoclonal antibody which specifically binds to ANXA1 disrupting its interaction with formyl peptide receptors 1 and 2 (FPR1/2). Annexuzlimab arrests cell cycle progression with cancer cells accumulating in the G1 phase. Annexuzlimab targets secreted ANXA1, preventing FPR1/2 activation and reducing cancer progression. Annexuzlimab can be used for the research of triple negative breast cancer, pancreatic cancer and osteosarcoma .
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- HY-182071
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Drug Derivative
Apoptosis
CDK
ASK1
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Cancer
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MG16 is a prodrug of 10-Methoxycamptothecin (HY-N0446). MG16 downregulates CDK6 and upregulates ASK1. MG16 induces cell cycle arrest and Apoptosis. MG16 exhibits anticancer activity against Lewis lung carcinoma, small cell lung cancer, and non-small cell lung cancer .
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- HY-179617
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E1/E2/E3 Enzyme
Interleukin Related
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Cancer
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Cbl-b-IN-30 is an orally active Casitas B-lineage lymphoma-b (CBLB) inhibitor. Cbl-b-IN-30 specifically binds to CBLB and inhibits its E3 ubiquitin ligase activity with an IC50 of 9.1 nM. Cbl-b-IN-30 can promote IL-2 secretion (EC50 = 187.5 nM) and enhance T cell activation. Cbl-b-IN-30 exerts antitumor activity and can induce immune memory. Cbl-b-IN-30 can be used for the research of colon cancer .
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| Cat. No. |
Product Name |
Target |
Research Area |
Image |
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- HY-P991181
-
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Transmembrane Glycoprotein
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Cancer
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VTX-1218 is a VSIG4 inhibitor with human Kd 7.4 nM. VTX-1218 blocks VSIG4 activity, relieves VSIG4-mediated macrophage suppression, repolarizes tumor-associated macrophages and induces T cell activation. VTX-1218 upregulates cytokines and chemokines linked to immune cell recruitment. VTX-1218 can be used for the research of multiple cancer types .
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(5)
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- HY-P991004
-
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LB-101
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CD47
PD-1/PD-L1
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Cancer
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Itanistomig (LB-101) is a tetravalent bispecific antibody targeting PD-L1 and CD47. Itanistomig blocks PD-L1 and achieves tumor enrichment through binding to PD-L1, and also exerts conditional CD47 blocking activity via cleavage of the hinge linker in the PD-L1-positive tumor microenvironment. Itanistomig induces antibody-dependent cellular phagocytosis in human CD14 + cells and drives tumor regression. Itanistomig can be used in research related to solid tumors .
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(5)
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- HY-P991468
-
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Interleukin Related
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Cancer
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IMM20324 is a human monoclonal antibody (mAb) targeting IL38. IMM20324 inhibits the interaction of IL-38 with human IL1RAPL1-Fc and human IL-36R-Fc with IC50 values of 1.267 nM and 1.4667 nM, respectively. IMM20324 has antitumor activity in the B16.F10 syngeneic mouse model. IMM20324 can be used in antitumor immunity research. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
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(5)
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- HY-P992352
-
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ES005 is an anti-tumor compound and LAG3 inhibitor. ES005 blocks the interactions of LAG3 with MHC-II, LSECtin and FGL1, thereby effectively reversing the LAG3-mediated inhibition of T cell activation and NFAT reporter gene expression. ES005 exhibits significant tumor growth inhibitory effects in syngeneic mouse breast tumor models using humanized LAG3 knock-in mice. ES005 can be used for breast tumor-related research .
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(5)
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- HY-P991960
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CTLA-4
Interleukin Related
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Cancer
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JS007 is a humanized IgG1 monoclonal antibody and also a CTLA-4 binder, with a Kd of 0.21 nM for CTLA-4. JS007 blocks the interaction between CTLA-4 and B7-1. JS007 activates T cells, promotes increased IL-2 secretion, and inhibits tumor growth in CTLA-4 knock-in mouse syngeneic tumor models. JS007 is applicable to research related to cancer and advanced solid tumors.
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(5)
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- HY-P991864
-
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MDX-124
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Formyl Peptide Receptor (FPR)
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Cancer
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Annexuzlimab is a humanised IgG1 monoclonal antibody which specifically binds to ANXA1 disrupting its interaction with formyl peptide receptors 1 and 2 (FPR1/2). Annexuzlimab arrests cell cycle progression with cancer cells accumulating in the G1 phase. Annexuzlimab targets secreted ANXA1, preventing FPR1/2 activation and reducing cancer progression. Annexuzlimab can be used for the research of triple negative breast cancer, pancreatic cancer and osteosarcoma .
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(5)
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