Search Result
Results for "
Non-small cell lung cancer model
" in MedChemExpress (MCE) Product Catalog:
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- HY-17026
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LY 188011
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Nucleoside Antimetabolite/Analog
DNA/RNA Synthesis
Autophagy
Apoptosis
p38 MAPK
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Infection
Inflammation/Immunology
Cancer
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Gemcitabine (LY 188011) is a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent. Gemcitabine inhibits DNA synthesis and repair, and can modulate autophagy. Gemcitabine induces apoptosis through the activation of p38 MAPK. Gemcitabine demonstrates efficacy in mouse models of pancreatic and breast cancer. Gemcitabine can be used for cancer research, such as pancreatic cancer, non-small cell lung cancer, and breast cancer .
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- HY-10201
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Sorafenib
Maximum Cited Publications
283 Publications Verification
Bay 43-9006
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Raf
VEGFR
FLT3
Autophagy
Apoptosis
STAT
Akt
MMP
Cadherin
p38 MAPK
ERK
MEK
PI3K
PARP
Bcl-2 Family
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Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
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Sorafenib (Bay 43-9006) is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib inhibits tumor growth and metastasis in mouse and rat models. Sorafenib can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma .
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- HY-145928
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GDC-6036
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Ras
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Cancer
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Divarasib (GDC-6036) is an orally active, selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds Cys12 in GDP-bound KRAS G12C, occupies the switch II pocket, blocks GTP binding and SOS-mediated reactivation, and inhibits oncogenic KRAS signaling. Divarasib induces tumor shrinkage and robust tumor growth inhibition in KRAS G12C-positive models and cancer cells. Divarasib can be used for the research of non-small cell lung cancer, colorectal adenocarcinoma, pancreatic ductal adenocarcinoma, and other KRAS G12C-mutated solid tumors .
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- HY-10201A
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Bay 43-9006 tosylate
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Raf
VEGFR
FLT3
Autophagy
Apoptosis
STAT
Akt
MMP
Cadherin
p38 MAPK
ERK
MEK
PI3K
PARP
Bcl-2 Family
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Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
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Sorafenib (Bay 43-9006) tosylate is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib tosylate induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib tosylate inhibits tumor growth and metastasis in mouse and rat models. Sorafenib tosylate can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma .
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- HY-156002
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Paluratide
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Ras
ERK
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Cancer
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LUNA18 is an orally-available cyclic peptide KRAS and ERK inhibitor. LUNA18 phosphorylates ERK and AKT and decreases cell proliferation in RAS-mutated cancer cells. LUNA18 exhibits RAS signal inhibition and potent anti-cancer activities through inhibiting interaction between RAS and guanine nucleotide exchange factors (GEFs) in a mouse xenograft model. LUNA18 shows significant cellular efficacy against cell lines with KRAS genetic alterations, such as colon cancer, stomach cancer, non-small cell lung cancer and pancreaticcancer .
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- HY-400902
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YAP
VEGFR
Hippo (MST)
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Cancer
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VT3989 is an orally active pan-TEAD autopalmitoylation inhibitor that modulates the Hippo signaling pathway. VT3989 directly binds to TEAD transcription factors to block their palmitoylation modification, thereby disrupting the formation of YAP/TAZ-TEAD complexes and inhibiting downstream oncogenic transcriptional activity. VT3989 effectively inhibits the growth of NF2-deficient schwannoma and meningioma cells and reverses the Schwann cell phenotype. In addition, VT3989 exerts a synergistic effect when combined with Osimtinib (HY-15772) in EGFR-mutant non-small cell lung cancer models, significantly delaying tumor recurrence and prolonging survival. VT3989 can be used for the research of epithelioid hemangioendothelioma, malignant pleural mesothelioma, type 2 neurofibromatosis and related advanced solid tumors .
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- HY-P9964
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11F8; IMC-11F8; LY3012211
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EGFR
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Cancer
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Necitumumab (11F8; IMC-11F8; LY3012211) is a human IgG monoclonal antibody directed against EGFR. Necitumumab binds to the EGF binding site of EGFR, blocks ligand binding, neutralizes ligand-induced EGFR phosphorylation and downstream signaling, induces EGFR internalization and degradation, and mediates antibody-dependent cellular cytotoxicity (ADCC) in EGFR-expressing cells. Necitumumab enhances antitumour activity in combination with Gemcitabine (HY-17026) and Cisplatin (HY-17394) in murine non-small-cell lung cancer xenograft models. Necitumumab can be used in research on cancers such as non-small cell lung cancer and colorectal cancer .
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- HY-13241A
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LY2228820
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p38 MAPK
Autophagy
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Cancer
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Ralimetinib is an ATP-competitive p38α and p38β MAPK inhibitor with an IC50 of 5.3 nmol/L against human p38α and an IC50 of 3.2 nmol/L against human p38β. Ralimetinib slows tumor growth in preclinical in vivo cancer models, exhibits oral bioavailability in mice, and achieves sustained target inhibition for 4 to 8 h. Ralimetinib is applicable for research on melanoma, non-small cell lung cancer, ovarian cancer, glioma, multiple myeloma, breast cancer, renal cancer, and head and neck squamous cell carcinoma .
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- HY-172429
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ORIC-114
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EGFR
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Neurological Disease
Cancer
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Enozertinib (ORIC-114) is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib can be used for the research of solid tumors and NSCLC .
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- HY-145729
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AZD9150
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STAT
Apoptosis
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Cancer
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Danvatirsen (AZD9150) is an antisense oligonucleotide targeting STAT3. Danvatirsen reduces the viability and promotes apoptosis of leukemia cell lines. Danvatirsen inhibits the expression of endogenous STAT3 and its downstream target genes, and reduces the proliferation and tumorigenicity of neuroblastoma and lymphoma cells. Danvatirsen inhibited tumor growth in mouse models of neuroblastoma, lymphoma, and non-small cell lung cancer. Danvatirsen achieves STAT3 mRNA and protein depletion in a mouse model of epidermoid carcinoma. Danvatirsen can be used in research related to lymphoma, myelodysplastic syndrome, acute myeloid leukemia, neuroblastoma and non-small cell lung cancer .
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- HY-145574
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WX-0593
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Anaplastic lymphoma kinase (ALK)
ROS Kinase
BCRP
Akt
ERK
STAT
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Cancer
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Iruplinalkib (WX-0593) is an orally active and selective ALK/ROS1 inhibitor. Iruplinalkib can effectively inhibit tyrosine autophosphorylation of ALK and mutant ALK, EGFR, with the IC50 between 5.38 and 16.74 nM. Iruplinalkib is also a suppressive agent of the transporter MATE1, MATE2K, P-gp and BCRP. Iruplinalkib can be used in the study of non-small cell lung cancer .
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- HY-N0600
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Interleukin Related
IFNAR
NF-κB
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Inflammation/Immunology
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Ginsenoside F3 is a saponin extracted from the leaves of Panax ginseng with immunoenhancing and antitumor immunostimulatory activities. Ginsenoside F3 upregulates RIPOR2 with a Kd value of 3.77 μM. Ginsenoside F3 enhances NF‑κB activation, upregulates T‑bet and downregulates GATA‑3, increases the production of IL‑2 and IFN‑γ, decreases the production of IL‑4 and IL‑10, reverses CD8⁺ T‑cell exhaustion, restores cytokine secretion, and enhances antitumor immunity in a mouse non‑small cell lung cancer model. Ginsenoside F3 can be used for the research of non-small cell lung cancer .
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- HY-P991669
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AML-01
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Caspase
Apoptosis
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Cancer
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IGN523 is an anti-CD98 antibody (hCD98, KD = 0.55 nM). IGN523 induces antibody-dependent cell-mediated cytotoxicity (ADCC) activity, lysosomal membrane permeabilization, and inhibition of essential amino acid transport, ultimately leading to caspase-3 and caspase-7-mediated apoptosis of tumor cells. IGN523 inhibits tumor growth in multiple tumor xenograft models. IGN523 is useful in the research of non-small cell lung cancer (NSCLC), acute myeloid leukemia (AML), and other cancers. .
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- HY-P99943
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KN-046
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PD-1/PD-L1
CTLA-4
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Cancer
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Erfonrilimab (KN-046) is a monoclonal antibody targeting PD-L1/CTLA-4. Erfonrilimab blocks the PD-L1 and CTLA-4 pathways, thereby regulating T cell function. Erfonrilimab enhances the secretion of IL-2 in superantigen-stimulated peripheral blood mononuclear cells. Erfonrilimab inhibits tumor growth in xenograft and double gene knock-in mouse models. Erfonrilimab can be used in research related to a variety of advanced solid tumors, including non-small cell lung cancer and nasopharyngeal carcinoma.
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- HY-157229
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STX-721
1 Publications Verification
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EGFR
ERK
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Cancer
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STX-721 is an orally active, irreversible, covalent EGFR exon 20 insertion (ex20ins) inhibitor that selectively targets ex20ins-mutant dynamic protein states. STX-721 potently inhibits the kinase activity of EGFR ex20ins mutants (NPG, ASV, SVD). STX-721 inhibits phosphorylation of EGFR (pEGFR Y1068) and downstream ERK (pERK Thr202/Tyr204), and suppresses proliferation of ex20ins-mutant Ba/F3 cells and human NSCLC cell lines (NCI-H2073 ASV KI, CUTO-14 ASV). STX-721 induces tumor regression in EGFR ex20ins-mutant PDX/CDX models. STX-721 can be used for the study of non-small cell lung cancer (NSCLC) harboring EGFR or HER2 ex20ins mutations .
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- HY-113418
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Endogenous Metabolite
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Cancer
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Beta-Cortol is an O-glycosylated compound and cortisol metabolite. It can be isolated from the leaves of mulberry cultivar Yu 711, and its concentration decreases significantly when the plant is subjected to drought stress. Beta-Cortol serves as a biomarker, as serum Beta-Cortol levels in early non-small cell lung cancer models are downregulated to 1/8 of the preoperative level after tumor resection. Due to such dramatic changes under specific pathological conditions, Beta-Cortol is currently widely used in studies related to early non-small cell lung cancer .
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- HY-172429A
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ORIC-114 hemihydrate
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EGFR
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Neurological Disease
Cancer
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Enozertinib (ORIC-114) hemihydrate is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib hemihydrate exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib hemihydrate induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib hemihydrate can be used for the research of solid tumors and NSCLC .
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- HY-175839
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PROTACs
EGFR
ATP Synthase
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Cancer
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PROTAC EGFR degrader 15 is a Pomalidomide (HY-10984)-based Gefitinib (HY-50895) EGFR PROTAC degrader. PROTAC EGFR degrader 15 triggers EGFR degradation via ubiquitin-proteasome-dependent proteolysis and autophagy-lysosome activation pathways. PROTAC EGFR degrader 15 targets ETFA to enhance ATP production. PROTAC EGFR degrader 15 significantly suppresses tumor growth in a Gefitinib-acquired resistant HCC-827 xenograft model. PROTAC EGFR degrader 15 can be used for the study of non-small cell lung cancer (NSCLC) (Pink: EGFR ligand (HY-W109039); Blue: CRBN ligand (HY-10984); Black: Linker (HY-W679737)) .
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- HY-145729A
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AZD9150 sodium
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STAT
Apoptosis
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Cancer
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Danvatirsen sodium (AZD9150 sodium) is an antisense oligonucleotide targeting STAT3. Danvatirsen sodium reduces the viability and promotes apoptosis of leukemia cell lines. Danvatirsen sodium inhibits the expression of endogenous STAT3 and its downstream target genes, and reduces the proliferation and tumorigenicity of neuroblastoma and lymphoma cells. Danvatirsen sodium inhibited tumor growth in mouse models of neuroblastoma, lymphoma, and non-small cell lung cancer. Danvatirsen sodium achieves STAT3 mRNA and protein depletion in a mouse model of epidermoid carcinoma. Danvatirsen sodium can be used in research related to lymphoma, myelodysplastic syndrome, acute myeloid leukemia, neuroblastoma and non-small cell lung cancer .
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- HY-117366
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PKC
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Cancer
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PS432 is a PKC inhibitor with IC50s of 16.9 μM (PKCι) and 18.5 μM (PKCζ), respectively. PS432 effectively inhibits the proliferation of non-small cell lung cancer cells (NSCLCs) and tumor growth in mouse xenograft models .
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- HY-170824
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PROTACs
SWI/SNF Complex
Epigenetic Reader Domain
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Cancer
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SMD-3236 is a SMARCA2 PROTAC degrader with a DC50 of 0.5 nM, a Dmax of 98%, and an IC50 of 42.2 nM against human SMARCA2. SMD-3236 induces proteasome- and ubiquitin-like modification-dependent degradation of SMARCA2 protein by binding to SMARCA2 and VHL-1. SMD-3236 inhibits the growth of SMARCA4-deficient cancer cells. SMD-3236 induces significant and persistent depletion of SMARCA2 in tumor tissues. SMD-3236 suppresses tumor growth in SMARCA4-deficient human cancer xenograft models. SMD-3236 can be used in research related to SMARCA4-deficient cancers such as melanoma, non-small cell lung cancer, and acute myeloid leukemia .
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- HY-161275
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EGFR
Akt
ERK
Ribosomal S6 Kinase (RSK)
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Cancer
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BI-4732 is an orally active, reversible, ATP-competitive EGFR inhibitor with blood-brain barrier penetration. BI-4732 inhibits the kinase activity of EGFR L858R, T790M and C797S with IC50 values of 1 nM while sparing EGFR wild-type. BI-4732 inhibits EGFR and reduces the phosphorylation of AKT, ERK, and S6K. BI-4732 demonstrates excellent intracranial anti-tumor efficacy in YU-1097 xenograft model harboring EGFR_E19del/T790M/C797S. BI-4732 can be used for the study of non-small cell lung cancer (NSCLC) .
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- HY-121811
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Lanceolatin C
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Glycosidase
Phosphatase
Interleukin Related
TNF Receptor
COX
Beclin1
GLUT
FAK
Akt
mTOR
p38 MAPK
Keap1-Nrf2
Apoptosis
Amyloid-β
Tau Protein
Autophagy
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Neurological Disease
Inflammation/Immunology
Cancer
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Pongamol (Lanceolatin C) is an orally active flavonoid with an IC50 of 75 μM and a Ki of 58 μM against PTPase-1B, and an IC50 of 103.5 μM against intestinal α-Glycosidase. Pongamol reduces the release of IL‑1β, TNF‑α, COX‑2 and iNOS in cells, reverses the nuclear translocation of NF‑κB, and upregulates the levels of Beclin 1 and LC3 Ⅱ/LC3 Ⅰ. Pongamol promotes glucose uptake by increasing the level of GLUT4 on the surface of skeletal muscle cells. Pongamol inhibits epithelial-mesenchymal transition by suppressing the FAK/Akt-mTOR signaling pathway. Pongamol inhibits neuronal cytotoxicity, suppresses cell apoptosis and extends the lifespan of Caenorhabditis elegans by activating the MAPKs/Nrf2 signaling pathway. Pongamol exerts hypoglycemic effects in diabetic mouse models. Pongamol exhibits antibacterial activity. Pongamol alleviates oxidative stress, neuroinflammation, Aβ deposition and excessive phosphorylation of Tau Protein, and restores autophagy function in Alzheimer's disease mouse models by inhibiting the Akt/mTOR signaling pathway. Pongamol is applicable to research related to Alzheimer's disease, type 2 diabetes, non-small cell lung cancer and postprandial hyperglycemia .
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- HY-148278
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SOS1
Ras
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Cancer
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BI-0474 is a potent KRAS G12C inhibitor with an IC50 value of 7.0 nM for the GDP-KRAS::SOS1 protein-protein interaction. BI-0474 exhibits good anti-proliferative activity against NCI-H358 cells carrying the G12C mutation. BI-0474 also shows good anti-tumour activity in non-small cell lung cancer xenograft models .
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- HY-145928B
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GDC-6036 adipate
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Ras
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Cancer
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Divarasib (GDC-6036) adipate is an orally active, selective KRASG12C inhibitor with an IC50 of <0.01 μM. Divarasib adipate covalently binds Cys12 in GDP-bound KRASG12C, occupies the switch II pocket, blocks GTP binding and SOS-mediated reactivation, and inhibits oncogenic KRAS signaling. Divarasib adipate induces tumor shrinkage and robust tumor growth inhibition in KRASG12C-positive models and cancer cells. Divarasib adipate can be used for the research of non-small cell lung cancer, colorectal adenocarcinoma, pancreatic ductal adenocarcinoma, and other KRASG12C-mutated solid tumors .
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- HY-P990947
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AZD9592 Antibody
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ADC Antibody
EGFR
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Cancer
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Tilatamig (AZD9592 Antibody) is a human antibody of the Ig (G1-κ_G1-λ2) subtype that targets EGFR/MET. Tilatamig conjugates with the Top1 inhibitor AZ14170133 (HY-145399) to form the antibody-drug conjugate (ADC) Tilatamig samrotecan (HY-171124) (AZD9592). Tilatamig accurately targets NSCLC models including EGFR-mutant, EGFR-wildtype, and EGFR tyrosine kinase inhibitor-treated ones, and its activity correlates with high expression of EGFR, c-MET and SLFN11. Tilatamig is available for in vivo anti-tumor studies in patient-derived xenograft models of non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC) .
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- HY-N7694
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TGF-β Receptor
JAK
STAT
Apoptosis
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Inflammation/Immunology
Cancer
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Isotoosendanin is an orally active TGFβR1 inhibitor and abrogating its kinase activity (IC50 = 6732 nM). Isotoosendanin inhibits the JAK/STAT3 signaling pathway by directly targeting SHP-2, enhancing its stability, and reducing its ubiquitination. Isotoosendanin inhibits TGF-β-induced reduces the migration, invasion, and metastasis in triple-negative breast cancer (TNBC) cells. Isotoosendanin exhibits anti-tumor efficacy in TNBC xenograft models and A549 xenograft tumors. Isotoosendanin exhibits significant anti-inflammatory effects in acetic acid-induced vascular permeability and λ-carrageenan-induced hind paw edema tests. Isotoosendanin can be used for the study of non-small cell lung cancer (NSCLC), TNBC and inflammation .
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- HY-18030A
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Anaplastic lymphoma kinase (ALK)
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Cancer
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CEP-28122 mesylate salt, a diaminopyrimidine derivative, is a potent, selective, and orally active ALK inhibitor with an IC50 value of 1.9 nM. CEP-28122 mesylate salt has antitumor activity in experimental models of ALK-positive human cancers. CEP-28122 mesylate salt has good pharmacodynamic and pharmacokinetic activity. CEP-28122 mesylate salt can be used for the study of ALK-positive anaplastic large-cell lymphoma (ALCL), non-small cell lung cancer (NSCLC), and neuroblastoma cells .
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- HY-18030
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Anaplastic lymphoma kinase (ALK)
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Cancer
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CEP-28122, a diaminopyrimidine derivative, is a potent, selective, and orally active ALK inhibitor with an IC50 value of 1.9 nM. CEP-28122 has antitumor activity in experimental models of ALK-positive human cancers. CEP-28122 has good pharmacodynamic and pharmacokinetic activity. CEP-28122 can be used for the study of ALK-positive anaplastic large-cell lymphoma (ALCL), non-small cell lung cancer (NSCLC), and neuroblastoma cells .
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- HY-177332
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TAM Receptor
SARS-CoV
Akt
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Infection
Cancer
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SLC-391 is an orally active AXL kinase inhibitor with an IC50 of 9.6 nM against AXL kinase. SLC-391 inhibits Gas6-induced AXL-dependent phosphorylation of Akt. SLC-391 inhibits SARS-CoV-2 infection, entry and replication in cells. SLC-391 suppresses cancer cell proliferation. SLC-391 inhibits tumor growth in mouse solid tumor xenograft models. SLC-391 can be used for the research of COVID-19, influenza virus infection, triple-negative breast cancer, chronic myeloid leukemia and non-small cell lung cancer .
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- HY-164429
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Integrin
Elastase
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Cancer
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VIP236 is a small-molecule drug conjugate targeting αvβ3 integrin. VIP236 achieves tumor homing via specific binding to αvβ3 integrin and delivers its payload to the tumor microenvironment. The linker of VIP236 is cleavable by neutrophil elastase, which is highly expressed in the tumor microenvironment, to release the payload 7-ethylcamptothecin. This payload induces DNA damage by inhibiting topoisomerase 1, thereby exerting anti-tumor effects. VIP236 exhibits excellent plasma stability and tumor targeting property, with a tumor/plasma payload ratio 10-fold higher than that of the single administration. It effectively induces tumor regression, reduces metastasis formation, and shows good tolerance in mouse models. VIP236 has been used in studies related to non-small cell lung cancer, clear cell renal cell carcinoma, colon cancer, triple-negative breast cancer, small cell lung cancer, and metastatic solid tumors .
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- HY-124072
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Cyclophilin
LPL Receptor
MDM-2/p53
Apoptosis
Reactive Oxygen Species (ROS)
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Cancer
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HL001 is an orally active small molecule inhibitor of Cyclophilin A (CypA) and a receptor antagonist of Lysophosphatidic acid 1 (LPA1). HL001 induces cell cycle arrest and apoptosis of tumor cells by p53. HL001 stabilizes p53 by down-regulating G3BP1, inducing reactive oxygen species and DNA damage. HL001 disrupts the interaction between MDM2 and p53-72R in a CypA dependent manner. HL001 has antitumor activity. HL001 can also be used to study pulmonary fibrosis .
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- HY-13554
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Antibiotic
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Cancer
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Annamycin is an anthracycline antibiotic with antitumor activity. Annamycin interacts with topoisomerase II, induces double-strand DNA breaks, triggers cell death, and exerts cytotoxic effects. In mice, Annamycin inhibits the growth of advanced subcutaneous melanoma and subcutaneous squamous cell carcinoma, and prolongs the survival of mice with subcutaneous reticulosarcoma and in lung cancer lung metastasis models. Annamycin can be used in research related to melanoma, reticulum cell sarcoma, lung cancer, non-small cell lung cancer, small cell lung cancer .
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- HY-106219
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Microtubule/Tubulin
P-glycoprotein
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Cancer
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BMS 275183 is a potent, orally active analogue of Paclitaxel (HY-B0015). BMS 275183 can stabilize microtubules and exhibits antitumor activity in in vivo tumor models. BMS 275183 is active in vitro against Paclitaxel-resistant tumors including those harboring tubulin mutations or overexpressing P-glycoprotein. BMS 275183 can be used for cancer research, such as non-small cell lung cancer (NSCLC) and prostate carcinoma .
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- HY-174387
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c-Met/HGFR
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Cancer
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KIN-8741 is a highly selective Type IIb c-Met inhibitor. KIN-8741 has broad activity against c-Met kinase mutations. KIN-8741 shows antitumor activity in MET gene amplified and exon 14 deleted non-small cell lung cancer models. KIN-8741 can be used in the research of c-Met driven cancers, especially advanced tumors carrying MET exon 14 jump mutations, acquired drug resistance mutations, etc .
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- HY-112806
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Drug-Linker Conjugates for ADC
HDAC
EGFR
Microtubule/Tubulin
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Cancer
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ST8155AA1 is a part of antibody agent conjugates (ADCs) charged with HDAC inhibitor. ST8155AA1 induces α-tubulin, histone H3/H4 acetylation via direct enzymatic inhibition. ST8155AA1 recognizes and binds EGFR, undergoes internalization into EGFR-expressing tumor cells. ST8155AA1 inhibits cancer cell proliferation and exerts activity in mouse tumor models. ST8155AA1 can be used for the research of non-small cell lung cancer .
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- HY-130133
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PI3K
mTOR
Akt
Apoptosis
Paraptosis
p38 MAPK
Mitochondrial Metabolism
P-glycoprotein
CDK
MMP
HIF/HIF Prolyl-Hydroxylase
VEGFR
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Cancer
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DHW-221 is a potent orally active dual PI3K/mTOR inhibitor, exhibiting low nanomolar potency against all four Class I PI3K isoforms and mTOR (PI3Kα, IC50 = 0.50 nM; PI3Kβ, IC50 = 1.9 nM; PI3Kγ, IC50 = 1.8 nM; PI3Kδ, IC50 = 0.74 nM; mTOR, IC50 = 3.9 nM). DHW-221 exerts antitumor effects by blocking the PI3K/Akt/mTOR pathway and inducing mitochondrial apoptosis and paraptosis (via Endoplasmic Reticulum (ER) stress and MAPK signaling) and arrests cell cycle, thereby inhibiting cell migration, invasion and angiogenesis. DHW-221 inhibits tumor growth in both the A549/Taxol (HY-B0015) and the HCC827 xenograft mouse models. DHW-221 can be used for non-small cell lung cancer (NSCLC), colon and breast cancer research .
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- HY-146223
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Ras
p38 MAPK
PI3K
Apoptosis
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Cancer
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AZD4625 is an orally active, selective irreversible, covalent allosteric GTPase KRASG12C inhibitor with an IC50 of 3 nM. AZD4625 can inhibit the MAPK pathway (with decreased pCRAF, pMEK, and pERK) and the PI3K pathway (with decreased pAKT and pS6), and induce cell apoptosis. AZD4625 has no binding and inhibition of wild-type RAS or isoforms carrying non-KRASG12C mutations. AZD4625 can be used for the study of KRASG12C mutant non-small cell lung cancer .
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- HY-174315
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PROTACs
Anaplastic lymphoma kinase (ALK)
Akt
ERK
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Cancer
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WZH-17-002 is a WZH-15-125-based ALK PROTAC degrader with a DC50 of 25 nM. WZH-17-002 enhances activities against Lorlatinib (HY-12215)-resistant ALK compound mutations. WZH-17-002 significantly reduces drug resistance in ALK-fusion non-small cell lung cancer (NSCLC) and inhibits tumor growth in EML4-ALK G1202R/L1196 M xenograft mice model . Pink: ALK ligand (HY-174314); Blue: CRBN ligase ligand (HY-14658); Black: linker (HY-174316)
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- HY-179418
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Apoptosis
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Cancer
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Ceritinib-platinum(IV)-4-phenylbutyrate (complex 7) is a Ceritinib (HY-15656)-conjugated Platinum(IV) prodrug with anticancer activity. Ceritinib-platinum(IV)-4-phenylbutyrate induces S-phase arrest, DNA damage responses, and apoptosis. Ceritinib-platinum(IV)-4-phenylbutyrate combines cytotoxicity with immune and anti-invasive activation in cancer cell models. Ceritinib-platinum(IV)-4-phenylbutyrate can be used for cancer research, such as non-small cell lung cancer (NSCLC) .
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- HY-105369
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Anaplastic lymphoma kinase (ALK)
Apoptosis
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Cancer
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KF-20444 is an orally active ALK inhibitor with blood-brain barrier penetration. KF-20444 exhibits strong inhibitory activity against ALK fusion proteins (EML4-ALK) and ALK resistance mutations (including L1196M, G1202R, and F1174L). KF-20444 effectively suppresses the phosphorylation of ALK in ALK-driven cancer cell lines, thereby inhibiting cancer cell proliferation and inducing apoptosis. KF-20444 demonstrates anti-tumor efficacy in mouse models bearing ALK-positive non-small cell lung cancer (NSCLC) or neuroblastoma. KF-20444 can be used for the study of ALK-driven malignancies .
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- HY-N2199
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Apoptosis
Autophagy
PI3K
JNK
mTOR
p38 MAPK
CDK
MMP
TGF-beta/Smad
STAT
β-catenin
Reactive Oxygen Species (ROS)
Bcl-2 Family
Caspase
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Inflammation/Immunology
Cancer
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Sotetsuflavone is a flavonoid that can be isolated from Cycas revolute. Sotetsuflavone inhibits phosphorylation of PI3K, Akt, mTOR, JNK, and p38 MAPK; modulates expression of Cyclin D1, CDK4, Bcl-2, Bax, cleaved caspases 3/9, MMP-9, TGF-β, STAT3, and β-catenin. Sotetsuflavone induces G0/G1 cell cycle arrest, apoptosis, autophagy, and intracellular ROS elevation, inhibits cancer cell proliferation. Sotetsuflavone inhibits tumor growth in mouse tumor xenograft models. Sotetsuflavone can be used for the research of non-small cell lung cancer and Crohn’s disease .
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- HY-178391
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ROS Kinase
p38 MAPK
ERK
Apoptosis
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Cancer
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SMU-037 is an orally active and selective ROS1 inhibitor that demonstrates potent activity (IC₅₀ = 6.8 nM) and possesses the ability to penetrate the blood-brain barrier. SMU-037 shows ~25-fold selectivity over ALK, and superior sensitivity against the G2032R mutation. SMU-037 attenuates phosphorylation of ROS1 and downstream MAPK-ERK signaling pathway, leading to cell cycle arrest and apoptosis. SMU-037 effectively suppresses tumor progression in both xenograft and intracranial mouse models. SMU-037 can be used for non-small cell lung cancer (NSCLC) research .
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- HY-174384
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c-Met/HGFR
Apoptosis
G-quadruplex
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Cancer
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MET Transcription-IN-1 (Compound C3) is an orally active MET transcription inhibitor. MET Transcription-IN-1 can efficiently bind and stabilize the G-quadruplex in the MET promoter region, thereby inhibiting c-Met expression. MET Transcription-IN-1 can also overcome drug resistance caused by specific c-Met mutations. MET Transcription-IN-1 is capable of inhibiting tumor cell proliferation, migration, and invasion, as well as inducing cell cycle arrest and apoptosis. MET Transcription-IN-1 has antitumor activity, and can be used in the research of tumors such as non-small cell lung cancer .
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- HY-178008
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Bcl-2 Family
Caspase
Apoptosis
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Cancer
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Mcl-1-IN-16 is an effective macrocyclic myeloid cell leukemia 1 (Mcl-1) inhibitor with a Ki of below 0.08 nM. Mcl-1-IN-16 maintains high selectivity (>50,000-fold) for Mcl-1 over other antiapoptotic Bcl-2 family members Bcl-2 and Bcl-xL. Mcl-1-IN-16 leads to the activation of caspase-3/7, thereby initiating cell apoptosis. Mcl-1-IN-16 achieves tumor regression in a lung cancer-derived tumor xenograft mice model. Mcl-1-IN-16 can be used in the research of solid tumor such as nonsmall cell lung cancer (NSCLC) .
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- HY-162098
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PROTACs
Microtubule/Tubulin
Apoptosis
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Cancer
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PROTAC tubulin-Degrader-1 is a α/β/β3-tubulin PROTAC degrader. PROTAC tubulin-Degrader-1 exhibits potent anti-proliferative activity against multiple human tumor cell lines. PROTAC tubulin-Degrader-1 induces G2/M phase arrest and apoptosis and inhibits colony formation in A549 and A549/Taxol cells. PROTAC tubulin-Degrader-1demonstrates potent anti-tumor efficacy in A549 and A549/Taxol (Taxol-resistant) xenograft model. PROTAC tubulin-Degrader-1 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: Tubulin ligand (HY-N2146), Blue: CRBN Ligand (HY-10984), Black: Linker (HY-N6056)) .
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- HY-175864
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EGFR
Apoptosis
p38 MAPK
ERK
Akt
STAT
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Inflammation/Immunology
Cancer
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EGFR-IN-173 is an orally active, pan-mutant EGFR tyrosine kinase inhibitor that targets EGFR 19del, L858R/T790M and C797S triple-mutations, potently inhibiting EGFR 19del/T790M/C797S with an IC50 of 1.19 nM while showing over 100-fold selectivity for mutant over wild-type EGFR (IC50 = 19.362 μM against WT). EGFR-IN-173 significantly inhibits cell migration, induces apoptosis in non-small cell lung cancer (NSCLC) cells. EGFR-IN-173 inhibits EGFR phosphorylation and suppresses the downstream pathways (MAPK/ERK, AKT, STAT3). EGFR-IN-173 exhibits antitumor efficacy in NSCLC and Ba/F3 xenograft models. EGFR-IN-173 can be used for NSCLC research .
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- HY-175332
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Apoptosis
Bcl-2 Family
Caspase
MDM-2/p53
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Cancer
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Apoptosis inducer 43 is an apoptosis inducer. Apoptosis inducer 43 can induce apoptosis, SubG0-G1 cell cycle arrest, secondary necrosis, and upregulate caspase-3, p53, and Bax/Bcl-2 expression in HCT116 cells. Apoptosis inducer 43 can inhibit tumor growth in a solid Ehrlich carcinoma (SEC) mouse model. Apoptosis inducer 43 can be used to study cancers such as colon cancer, leukemia, and non-small cell lung cancer .
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- HY-175206
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P-glycoprotein
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Cancer
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P-gp-IN-30 (Compound 13) is a P-glycoprotein (P-gp) inhibitor by targeting YB-1. P-gp-IN-30 significantly enhances sensitivity to Paclitaxel by reducing total YB-1 and nucleus YB-1 protein expression, inhibiting the expression and function of downstream P-gp, further suppressing the efflux rate of Paclitaxel. P-gp-IN-30 potently inhibits tumor growth in A549/Taxol xenografts mice model with combination of Paclitaxel (HY-B0015). P-gp-IN-30 can be used for non-small cell lung cancer (NSCLC) research .
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- HY-170968
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EGFR
Apoptosis
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Cancer
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EGFR-IN-150 is an EGFR inhibitor that effectively suppresses the phosphorylation of mutant epidermal growth factor receptor (EGFR) and its downstream AKT signaling pathway, thereby exerting antitumor effects and inducing HMOX1 expression to trigger ferroptosis. EGFR-IN-150 exhibits an IC50 of 0.386 μM against the non-small cell lung cancer (NSCLC) cell line H1975, and significantly inhibits colony formation and migration of both H1975 and A549 cells while inducing apoptosis. In addition, EGFR-IN-150 markedly suppresses tumor growth in the H1975 cell-derived xenograft (CDX) mouse model. EGFR-IN-150 holds promise for research related to non-small cell lung cancer .
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- HY-172881
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Pyruvate Kinase
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Cancer
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PKM2-IN-10 (Compound 16) is a PKM2 inhibitor. PKM2-IN-10 inhibits the proliferation of A549 and HCC1833 cell lines with IC50 of 3.36 μM and 9.20 μM, respectively. PKM2-IN-10 exhibits antitumor activity in human non-small cell lung cancer (NSCLC) and mouse lung adenocarcinoma models. PKM2-IN-10 can be used in lung cancer research .
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- HY-168300
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Reactive Oxygen Species (ROS)
Apoptosis
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Inflammation/Immunology
Cancer
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Antiangiogenic agent 7 (Compound 1) can induce cell apoptosis, increase Reactive Oxygen Species, and inhibit the intracellular enzyme thioredoxin reductase. Antiangiogenic agent 7 has anti-cancer activity, with an IC50 of 0.08-3.5 μM against cervical cancer cells HeLa, prostate cancer cells PC-3, and non-small cell lung cancer A549. Antiangiogenic agent 7 inhibits tumor growth in mouse xenograft models .
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- HY-18030B
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Anaplastic lymphoma kinase (ALK)
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Others
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CEP-28122 mesylate hydrochloride, a diaminopyrimidine derivative, is a potent, selective, and orally active ALK inhibitor with an IC50 value of 1.9 nM. CEP-28122 mesylate hydrochloride has antitumor activity in experimental models of ALK-positive human cancers. CEP-28122 mesylate hydrochloride has good pharmacodynamic and pharmacokinetic activity. CEP-28122 mesylate hydrochloride can be used for the study of ALK-positive anaplastic large-cell lymphoma (ALCL), non-small cell lung cancer (NSCLC), and neuroblastoma cells .
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- HY-114253
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EGFR
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Cancer
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ODS-2004436 is a small molecule radiotracer that uses positron emission tomography (PET) imaging to measure the activity of the epidermal growth factor receptor (EGFR) in tumors. ODS-2004436 labeled with the radioactive isotope fluorine-18 shows significantly higher uptake in the xenograft models of lung cancer with EGFR mutations compared to the wild-type models, and could be used to distinguish the mutation status. ODS-2004436 can be used to identify EGFR-positive tumors and predict their response to certain reagent treatments, especially for non-small cell lung cancer (NSCLC) .
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- HY-W110138
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DNA/RNA Synthesis
Cytochrome P450
ROCK
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Cancer
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Chloroxoquinoline is an anticancer agent. Chloroxoquinoline damages the DNA templates of cancer cells, inducing DNA breaks and cell death, and inhibits cell invasion via down-regulating Rho/Rho kinase signaling pathway. Chloroxoquinoline enhances the radiation sensitivity of Lewis lung cancer cells and xenograft tumors in tumor-bearing mouse models but decreases efficacy after long term exposure in rat models by auto-induction effects on CYP1A and CYP3A. Chloroxoquinoline has a broad-spectrum anticancer activity, such as non-small-cell lung carcinoma (NSCLC), breast cancer and gastric cancer .
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- HY-P99658A
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- HY-149695
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EGFR
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Cancer
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EGFR-IN-91 (compound 9) is an orally available EGFR inhibitor with blood-brain barrier penetrability. EGFR-IN-91 inhibits EGFR L858R/C797S and EGFR exon 19del/C797S, inducing tumor regression in xenograft (PDX) mouse models. EGFR-IN-91 has the potential to inhibit localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutants .
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- HY-12965B
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TAM Receptor
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Cancer
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(Z)-S49076 hydrochloride is an orally active inhibitor of MET and AXL that blocks the downstream signaling of these receptors both in vitro and in vivo, inhibiting the proliferation and migration of tumor cells and suppressing tumor growth in xenograft models. (Z)-S49076 hydrochloride is capable of overcoming the resistance to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) due to MET amplification in Erlotinib (HY-50896)-resistant cell lines both in vitro and in vivo. (Z)-S49076 hydrochloride can be used for research in non-small cell lung cancer (NSCLC) .
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- HY-107513
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mGluR
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Neurological Disease
Cancer
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BAY 36-7620 is a potent and noncompetitive antagonist of mGlu1 Receptor (IC50=0.16 μM) with inverse agonist activity. BAY 36-7620 inhibits tumor growth and prolongs the survival of mice with tumors by inhibiting mGlu1 receptor. BAY 36-7620 suppresses AKT phosphorylation in A549 tumors. BAY 36-762 has neuroprotective effect in acute subdural hematoma rat model.BAY 36-7620 is used in non-small cell lung cancer and breast cancer research .
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- HY-178451
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Apoptosis
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Cancer
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NQO1-responsive prodrug is a prodrug of Gemcitabine (dFdC) (HY-17026) with anti-cancer effect. NQO1-responsive prodrug remains stable in plasma and liver/intestinal S9 fractions, releasing dFdC in an NQO1-dependent manner. NQO1-responsive prodrug induces S-phase arrest and apoptosis. NQO1-responsive prodrug inhibits tumor growth in an A549 xenograft mouse model. NQO1-responsive prodrug can be used for breast and non-small cell lung cancer (NSCLC) research .
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- HY-176942
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ROS1-IN-3
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ROS Kinase
Trk Receptor
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Cancer
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YP0322 (ROS1-IN-3) is a potent orally active, selective, and CNS-penetrant ROS1 inhibitor. JYP0322 selectively inhibits human wild-type ROS1 and human ROS1 G2032R with IC50s of 0.37 and 0.3 nM, respectively, showing 6-130-fold selectivity over TRKA, TRKB, and TRKC. JYP0322 inhibits proliferation of ROS1 fusion-expressing cells, and inhibits tumor growth in mouse xenograft models. JYP0322 can be used for the research of non-small cell lung cancer (NSCLC) .
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- HY-164503
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NEP010
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EGFR
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Cancer
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Neptinib (NEP010) is an orally active derivative of Afatinib (HY-10261) that has stronger antitumor activity than Afatinib (HY-10261) by improving pharmacokinetics. Neptinib has a significant inhibitory effect on tumor growth in mouse non-small cell lung cancer models with different EGFR mutations. Neptinib has a certain inhibitory effect on the EGFR kinase family, with IC50 values ??of 0.24 nM, 7.25 nM, 0.46 nM and 1.79 nM for EGFR wt, EGFR L858R/T790M, EGFR L858R and EGFR T790M, respectively .
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- HY-P992163
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Fc Receptor (FcR)
C-type Lectin-like Receptors (CTLRs)
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Inflammation/Immunology
Cancer
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23ME-01473 is an anti-ULBP6/2/5 antibody with enhanced Fc effector function, with a Kd of 0.053 nmol/L against hULBP6, 0.23 nmol/L against hULBP2, and 1.92 nmol/L against hULBP5. 23ME-01473 restores anti-tumor immunity by activating NKG2D and FcγRIIIa. 23ME-01473 exerts anti-cancer activity in non-small cell lung cancer PDX models. 23ME-01473 can be used for the research of non-small cell lung cancer .
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- HY-158029
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PI3K
Apoptosis
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Cancer
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PI3Kα-IN-21 (compound 8) is a PI3Kα inhibitor, and its selectivity for PI3Kα is 10.41/16.99/37.53 times higher than PI3Kβ/γ/δ respectively (IC50: 96.89/568.24/397.48 nM ). PI3Kα-IN-21 inhibits cancer cell activity, proliferation, and migration, and induces mitochondrial apoptosis through the PI3K/Akt/mTOR pathway. PI3Kα-IN-21 exhibits in vivo antitumor potency in a mouse model of non-small cell lung cancer .
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- HY-171509
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Drug-Linker Conjugates for ADC
Apoptosis
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Cancer
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Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27), an agent-linker conjugate for ADC, consists the ADC linker Mal-N(Me)-C6-N(Me) and a potent ADC cytotoxin PNU-159682. Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27) selectively delivers the payload to CD46-expressing cells, where the linker is cleaved by cathepsin B to release PNU-159682, inducing DNA damage and apoptosis. Mal-N(Me)-C6-N(Me)-PNU-159682 shows durable tumor regression in xenograft (PDX) models of non-small cell lung cancer (NSCLC) and colorectal cancer (CRC) .
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- HY-172251
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FGFR
Apoptosis
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Cancer
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FGFR-IN-17 (Compound 12l) is an orally active irreversible inhibitor of FGFR, which has a strong inhibitory effect on FGFR and its mutants. FGFR-IN-17 can inhibit the proliferation and migration, and induce apoptosis of non-small cell lung cancer cells. FGFR-IN-17 has anti-tumor activity .
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- HY-179049
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EGFR
Microtubule/Tubulin
Akt
ERK
Autophagy
Atg8/LC3
p62
Ferroptosis
Reactive Oxygen Species (ROS)
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Cancer
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EGFR/tubulin-IN-1 (Compound 26) is a dual-target inhibitor of EGFR and tubulin. EGFR/tubulin-IN-1 significantly reduces the levels of p-EGFR, p-AKT, and p-ERK in cells, disrupting the microtubule structure of the cells. EGFR/tubulin-IN-1 significantly inhibits the proliferation of H1975 cells and significantly blocks the cells in the G2/M phase. EGFR/tubulin-IN-1 induces the expression of autophagy markers LC3B-II and Beclin-1, while down-regulating the expression of p62. EGFR/tubulin-IN-1 induces ferroptosis, with increased ROS content and depletion of glutathione (GSH). EGFR/tubulin-IN-1 inhibits epithelial-mesenchymal transition (EMT) and tumor metastasis. EGFR/tubulin-IN-1 has a significant tumor-suppressing effect in the H1975 transplanted tumor nude mouse model. EGFR/tubulin-IN-1 can be used for the study of non-small cell lung cancer .
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- HY-180430
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Drug Derivative
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Cancer
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Antitumor agent-208, a Bufalin (HY-N0877) analogue, is a potent and orally active antitumor agent. Antitumor agent-208 exhibits antiproliferative activity against tumor cell line (IC50 =0.30-1.09 nM). Antitumor agent-208 inhibits tumor growth in a MV-4-11 xenograft mouse model. Antitumor agent-208 can be used for cancer research, such as acute myeloid leukemia (AML) and non-small cell lung cancer (NSCLC) .
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- HY-182378
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Cancer
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Vps34-IN-5 is an orally active VPS34 inhibitor, 98% target inhibition, and an IC50 categorized as B. Vps34-IN-5 induces additive or synergistic anti-proliferative activity with EGFR inhibitors in cancer cells. Vps34-IN-5 is administered orally alone or with Erlotinib (HY-50896) in mouse xenograft models. Vps34-IN-5 can be used for the research of non-small cell lung cancer .
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- HY-180850
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PROTACs
Estrogen Receptor/ERR
Reactive Oxygen Species (ROS)
Apoptosis
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Cancer
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ERB-2 is a selective ERβ PROTAC degrader. ERB-2 removes the inhibitory effect of ERβ on ROS, leading to the accumulation of ROS, mitochondrial damage, and ultimately triggering cell apoptosis (apoptosis). ERB-2 significantly inhibits tumor growth in the nude mouse model of NCI-H1975OR tumors. ERB-2 can be used for the study of non-small cell lung cancer .
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- HY-181517
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Bacterial
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Infection
Cancer
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Antitumor agent-212 is a α-exo-methylene-selenolactone derivative with prominent selective antitumor activity. Antitumor agent-212 exhibits an MIC value of 128 μg/mL against Gram-positive bacteria. Antitumor agent-212 exhibits significant antitumor effects in the U87 human glioma xenograft model. Antitumor agent-212 can be used for the study of glioma, breast cancer and non-small cell lung cancer, and antibacterial study .
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- HY-165503
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Wnt
β-catenin
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Cancer
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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 .
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- HY-181065
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Epigenetic Reader Domain
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Cancer
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LS-170 is a YEATS2 YEATS domain inhibitor with an IC50 of 0.14 μM. LS-170 displays selectivity for the YEATS2 YEATS domain over other YEATS domain family members and other epigenetic 'reader' and 'eraser' proteins. LS-170 reduces chromatin occupancy of the Ada-two-A-containing (ATAC) complex, decreases ATAC-dependent histone acetylation levels, and downregulates expression of ATAC-governed genes. LS-170 suppresses tumor growth in a lung cancer mouse model. LS-170 can be used for the research of non-small cell lung cancer .
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- HY-183007
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PROTACs
SWI/SNF Complex
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Cancer
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LJM133 is a SMARCA2/PBRM1/SMARCA4 PROTAC degrader with DC50 values of 3.5 nM, 7 nM, and 6.4 nM. LJM133 induces ternary complex formation with VHL E3 ligase to drive proteasome-mediated degradation of target proteins. LJM133 suppresses cell proliferation and exhibits significant antitumor efficacy in a SMARCA4 mutant cancer xenograft model. LJM133 can be used for the research of cancer, such as SMARCA4 mutant non-small cell lung cancer . (Pink: SMARCA2/PBRM1/SMARCA4 ligand (HY-182987); E3 ubiquitin ligase ligand-linker conjugate (HY-183619)).
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- HY-180200
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Ras
ERK
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Cancer
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RNK08954 is an orally active KRASG12D inhibitor with a Kd of 0.0395 nM. RNK08954 selectively binds the inactive GDP-bound KRASG12D form, suppresses downstream KRAS-mediated signaling pathways p-ERK1/2 experssion. RNK08954 inhibits KRASG12D-mutant cell proliferation, induces G0-G1 cell cycle arrest, and inhibits tumor growth in mouse xenograft models. RNK08954 can be used for the research of non-small cell lung cancer, pancreatic ductal adenocarcinoma .
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- HY-181420A
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Ras
Phosphatase
ERK
Apoptosis
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Cancer
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BBO-11818 is an orally active, highly selective (relative to NRAS and HRAS), non-covalent pan-KRAS inhibitor (IC50=28-120 nM). BBO-11818 specifically binds to the Switch-II/Helix 3 pocket, disrupts the KRAS:RAF1 interaction by inducing conformational changes, and blocks the MAPK signaling pathway. BBO-11818 exhibits significant anti-tumor activity, which not only inhibits cell proliferation and induces apoptosis, but also drives tumor regression in xenograft models. BBO-11818 produces synergistic effects when combined with Cetuximab (HY-P9905), anti-PD-1 antibody or PI3Kα inhibitor. BBO-11818 is used in the research of KRAS mutation-related malignancies such as pancreatic cancer, non-small cell lung cancer and colorectal cancer .
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- HY-186086
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Ras
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Cancer
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RM-041 is a selective, orally active KRAS G13C (ON) inhibitor that forms a covalent complex with KRAS G13C (ON) and Cyclophilin A. RM-041 blocks the binding of RAS effector proteins via steric hindrance, and then covalently binds to Cys-13 to form an irreversible inhibitory complex, thereby inhibiting the proliferation of KRAS G13C mutant cancer cells. RM-041 induces regression of KRAS G13C tumors in cellular and xenograft tumor models. RM-041 exerts a synergistic effect when combined with upstream node inhibitors (such as SHP2 inhibitors). RM-041 can be used for the research of non-small cell lung cancer .
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- HY-181777
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EGFR
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Cancer
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Mal-Pip-ValCit-PAB-AZ7550 is a prodrug of EGFR inhibitor. Mal-Pip-ValCit-PAB-AZ7550 selectively binds covalently to albumin via its maleimide moiety. Mal-Pip-ValCit-PAB-AZ7550 exhibits potent in vivo anticancer activity in non-small cell lung cancer xenograft models. Mal-Pip-ValCit-PAB-AZ7550 can be used in research related to non-small cell lung cancer .
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- HY-182914
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EGFR
Akt
Bcl-2 Family
Apoptosis
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Cancer
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NGI‑189 is a selective OST‑A inhibitor. NGI‑189 inhibits the STT3A catalytic subunit of the OST complex and reduces N‑glycosylation of target glycoproteins. NGI‑189 blocks oncogenic and bypass signaling, reduces phosphorylation of EGFR, AKT, p70S6K and S6RP, and induces cell cycle arrest and apoptosis. NGI‑189 markedly suppresses tumor growth and induces tumor regression in non‑small cell lung cancer (NSCLC) xenograft models. NGI‑189 can be used for the research of EGFR‑mutant non‑small cell lung cancer .
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- HY-P992146
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MYTX-011 Antibody; Q-397
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ADC Antibody
c-Met/HGFR
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Cancer
|
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Zevontabart (MYTX-011 Antibody; Q-397) is a pH-dependent anti-c-MET antibody. Zevontabart regulates the trafficking process of c-MET to reduce receptor recycling, and enhances its own endocytosis and accumulation in c-MET-expressing cells. Zevontabart induces cytotoxicity in solid tumor cells and exerts anti-tumor activity in a non-small cell lung cancer xenograft mouse model. Zevontabart can be used to synthesize ADC, such as: MYTX-011. Zevontabart can be used in studies related to non-small cell lung cancer, with its corresponding isotype control being Human IgG1 kappa, Isotype Control (HY-P99001) .
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- HY-183116
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Molecular Glues
Anaplastic lymphoma kinase (ALK)
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Cancer
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TRI-611 is a brain-penetrant, orally active molecular glue degrader targeting ALK. TRI-611 engages ALK via a distal degron, forms a ternary complex with CRBN, triggers ALK polyubiquitination and degradation, including TKI-resistant ALK fusion proteins. TRI-611 inhibits ALK downstream signaling pathways, induces anti-proliferative effects in ALK-positive cancer cells. TRI-611 induces regression of ALK-positive non-small cell lung cancer tumors in preclinical xenograft models. TRI-611 can be used for the research of ALK-positive non-small cell lung cancer, including TKI-refractory tumors and central nervous system metastases .
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- HY-153503
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Anaplastic lymphoma kinase (ALK)
Insulin Receptor
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Cancer
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ALK-IN-24 is an orally active ALK inhibitor with an IC50 value of 1.7 nM. ALK-IN-24 also inhibits insulin receptor kinase with an IC50 value of 6 nM. ALK-IN-24 suppresses the proliferation of lung adenocarcinoma cells. ALK-IN-24 inhibits ALK-driven tumor growth in xenograft mouse models. ALK-IN-24 can be used in research related to non-small cell lung cancer .
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- HY-179481
-
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Ferroptosis
Keap1-Nrf2
Glutathione Peroxidase
Reactive Oxygen Species (ROS)
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Cancer
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Ferroptosis inducer-13 is a 5′-prenylated chalcone derivative that effectively induces ferroptosis in human non-small cell lung cancer (NSCLC) cells by altering the activity of the Nrf2/xCT/GPX4 pathway. Ferroptosis inducer-13 exhibits potent anti-proliferative effects in vitro, and inhibits tumour growth in a NSCLC mouse model. Ferroptosis inducer-13 can be used for NSCLC research .
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- HY-180241
-
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Glutaminase
Reactive Oxygen Species (ROS)
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Cancer
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Glutaminase C-IN-3 is a potent allosteric inhibitor of Glutaminase C (GAC) with an EC50 of 116 nM. Glutaminase C-IN-3 regulates cellular metabolites and increases reactive oxygen species (ROS) production by blocking glutamine metabolism. Glutaminase C-IN-3 exhibits strong antitumor activity in an A549 xenograft mouse model. Glutaminase C-IN-3 can be used for the research of non-small cell lung cancer (NSCLC) .
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- HY-182336
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PROTACs
Dipeptidyl Peptidase
GLP Receptor
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Inflammation/Immunology
Cancer
|
|
DeDPP4 is a DPP-4 PROTAC degrader. DeDPP4 induces sustained elevation of glucagon-like peptide-1 (GLP-1), enhances glucose tolerance, causes persistent reduction of blood glucose, and achieves long-term blood glucose regulation in animal models of type 2 diabetes. DeDPP4 mediates dose-dependent DPP-4 depletion in cancer cells, and also targets and degrades DPP-4 in the liver and adipose tissues of animal models with type 2 diabetes. DeDPP4 can be used for the research of type 2 diabetes and non-small cell lung cancer .
|
-
- HY-183568
-
|
|
Methionine Adenosyltransferase (MAT)
|
Cancer
|
|
MAT2A-IN-26 is an orally active MAT2A inhibitor with a human IC50 of 17.53 nM. MAT2A-IN-26 inhibits the enzymatic activity of MAT2A, thereby reducing the levels of S-adenosylmethionine (SAM) and symmetric dimethylarginine (sDMA). MAT2A-IN-26 inhibits the proliferation of MTAP-deficient cancer cells and induces anti-tumor efficacy in xenograft models. MAT2A-IN-26 can be used in non-small cell lung cancer research .
|
-
- HY-183984
-
|
|
G-quadruplex
|
Cancer
|
|
G-quadruplex ligand 6 is a G-quadruplex ligand targeting the c-MYC promoter with anti-tumor activity. G-quadruplex ligand 6 forms a non-covalent complex with Pu22, a G-quadruplex model of the c-MYC promoter, with a microscopic dissociation constant Kd of 0.202 μM. G-quadruplex ligand 6 selectively inhibits tumor cell proliferation, blocks the binding of transcription factors by stabilizing the G-quadruplex in the c-MYC promoter, and thereby regulates the expression of proto-oncogenes. G-quadruplex ligand 6 can be used in the research of pancreatic cancer, non-small cell lung cancer, colorectal cancer, and triple-negative breast cancer .
|
-
- HY-P992323
-
|
|
VEGFR
Tie
ERK
|
Cardiovascular Disease
Cancer
|
|
BI-836880 is a humanized bispecific nanobody and a selective inhibitor of VEGF and ANG2, with a Kd of 16 pM for hANG2, an EC50 of 1.4 nM for VEGF165, and an EC50 of 2.3 nM for VEGF121. BI-836880 blocks ERK phosphorylation downstream of VEGF-A as well as TIE2 phosphorylation downstream of ANG2. BI-836880 does not inhibit ANG1-mediated TIE2 phosphorylation. BI-836880 exerts anti-angiogenic effects, reduces the number of immature endothelial vessels in tumor tissues, and inhibits tumor growth in preclinical models. BI-836880 can be used in the research of pancreatic cancer, non-small cell lung cancer, renal cell carcinoma, ovarian cancer, colon cancer, and Lewis lung cancer .
|
-
- HY-183120
-
|
|
FAK
EGFR
Apoptosis
|
Cancer
|
|
EGFR T790M/FAK-IN-2 is an orally active dual FAK and EGFR T790M kinase inhibitor, with an IC50 of 1.03 nM against FAK and an IC50 of 3.89 nM against EGFR T790M. EGFR T790M/FAK-IN-2 exerts antiproliferative effects in drug-resistant cancer cells overexpressing FAK, inducing apoptosis and cell cycle arrest. EGFR T790M/FAK-IN-2 exhibits antitumor activity in a pancreatic cancer xenograft mouse model. EGFR T790M/FAK-IN-2 can be used for the research of pancreatic cancer, breast cancer and non-small cell lung cancer .
|
-
- HY-P991954
-
|
|
Complement System
Syk
|
Inflammation/Immunology
Cancer
|
|
GT103 is a human-derived monoclonal antibody targeting complement factor H (CFH). GT103 binds to a conformationally distinct epitope of CFH on tumor cells. GT103 activates the classical complement pathway, induces complement-dependent cytotoxicity, and triggers antibody-dependent cellular phagocytosis (ADCP) of tumor cells. GT103 increases calreticulin translocation to tumor cell plasma membranes. GT103 mediates B-cell activation via Syk kinase phosphorylation. GT103 inhibits tumor growth and metastasis in animal models. GT103 can be used for the research of non-small cell lung cancer .
|
-
- HY-109061R
-
|
YH25448 (Standard); GNS-1480 (Standard)
|
Apoptosis
Akt
TRP Channel
EGFR
ERK
Reference Standards
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
Lazertinib (Standard) is the analytical standard of Lazertinib (HY-109061). This product is intended for research and analytical applications. Lazertinib (YH25448) is a potent, selective, CNS-penetrant, orally available and irreversible EGFR tyrosine Kinase inhibitor, exhibiting high selectivity for activating (EGFRm) and T790M resistance mutations. Lazertinib inhibits phosphorylation of EGFR, AKT and ERK, leading to apoptosis and suppression of tumor growth in mouse H1975-luc brain metastasis xenograft models. Lazertinib can be used in the study of non-small cell lung cancer .
|
-
- HY-109061BR
-
|
YH25448 mesylate (Standard); GNS-1480 mesylate (Standard)
|
Reference Standards
|
Cancer
|
|
Lazertinib mesylate (Standard) is the analytical standard of Lazertinib (mesylate) (HY-109061B). This product is intended for research and analytical applications. Lazertinib (YH25448) mesylate is a potent, selective, CNS-penetrant, orally available and irreversible EGFR tyrosine Kinase inhibitor, exhibiting high selectivity for activating (EGFRm) and T790M resistance mutations. Lazertinib mesylate inhibits phosphorylation of EGFR, AKT and ERK, leading to apoptosis and suppression of tumor growth in mouse H1975-luc brain metastasis xenograft models. Lazertinib mesylate can be used in the study of non-small cell lung cancer .
|
-
- HY-181954
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
ZW-49 is an orally active pan-EGFR inhibitor with IC50 values at 0.03-1.5 nM. ZW-49 inhibits all subgroups of EGFR mutations with selectivity over wild-type EGFR and other target families. ZW-49 blocks the ATP-binding pocket, occupies a conserved hydrophobic subpocket, avoids steric conflicts with PACC mutation P loops. ZW-49 inhibits cancer cells proliferation, induces G0/G1 phase cell-cycle arrest and apoptosis, and demonstrates anti-proliferative activity in xenograft mice models. ZW-49 can be used for the research of cancer, such as non-small cell lung cancer .
|
-
- HY-15947G
-
|
GDC-0994
|
ERK
c-Myc
Hexokinase
Lactate Dehydrogenase
|
Cancer
|
|
Ravoxertinib GMP is Ravoxertinib (HY-15947) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Ravoxertinib (GDC-0994) is an orally active ERK1/2 inhibitor. Ravoxertinib inhibits the ERK1/2 MAPK signaling pathway and reduces the expression levels of c-Myc, HK2 and LDHA. Ravoxertinib decreases mammosphere formation, and exerts additive and/or superadditive cytotoxicity when combined with Ipatasertib (HY-15186) in 3D tumor sphere models. Ravoxertinib can be used in research related to various cancers including breast cancer, melanoma, head and neck cancer, non-small cell lung cancer, ovarian cancer and Merkel cell carcinoma .
|
-
- HY-116636
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
KRCA-0377 is an orally active ALK inhibitor with an IC50 of 0.001 μM. KRCA-0377 also inhibits mutant ALK enzyme with IC50 values ≤0.01 μM. KRCA-0377 shows cytotoxicity against cancer cells and inhibits tumor growth in xenograft mice models. KRCA-0377 can be used for the research of ALK-positive non-small-cell lung cancer .
|
-
- HY-P992369
-
|
|
VISTA
|
Cancer
|
|
HMBD-002 is an Fc-independent, non-depleting IgG4 subclass antibody that targets VISTA and VSIG3. It is widely used in research related to various solid tumors, including colon cancer, triple-negative breast cancer, and non-small cell lung cancer. HMBD-002 blocks the interactions of VISTA with VSIG3 and LRIG1, relieves immunosuppression without depleting VISTA-positive cells, activates the cytotoxic program of CD8 + T cells, and drives the type I interferon signaling pathway. HMBD-002 reprograms tumor-associated macrophages to the M1 phenotype, reduces tumor infiltration of inhibitory myeloid cells, thereby significantly inhibiting tumor growth and improving survival. HMBD-002 is well tolerated in rodent and non-human primate animal models .
|
-
- HY-181687
-
|
|
HSP
CDK
|
Cancer
|
|
Hsp90-IN-46 is a Hsp90 inhibitor. Hsp90-IN-46 exhibits broad-spectrum antiproliferative activity against tumor cell lines. Hsp90-IN-46 inhibits breast cancer cell proliferation by reducing colony formation and downregulating the proliferation marker Ki-67. Hsp90-IN-46 inhibits Hsp90 and its ATPase activity, downregulates the downstream substrate oncoproteins HER2 and CDK4, and moderately induces the heat shock response. Hsp90-IN-46 shows significant antitumor activity in a mouse model of triple-negative breast cancer tumor xenografts. Hsp90-IN-46 can be used for research on various cancers including triple-negative breast cancer, leukemia, non-small cell lung cancer, colon cancer, ovarian cancer, renal cancer, prostate cancer .
|
-
- HY-181889
-
|
|
Ras
|
Cancer
|
|
KRAS G12C-IN-75 is an orally active, blood-brain barrier penetrant KRAS G12C inhibitor with an IC50 of 0.53 nM. KRAS G12C-IN-75 attenuates active transport mediated by P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP). KRAS G12C-IN-75 inhibits tumor growth, regulates the expression of downstream MAPK target genes DUSP6 and SPRY4, and exhibits dose-dependent KRAS G12C alkylation in KRAS G12C-positive xenograft models. KRAS G12C-IN-75 can be used for research related to non-small cell lung cancer .
|
-
- HY-181420
-
|
|
ERK
Apoptosis
Phosphatase
Ras
|
Cancer
|
|
(S,R,S)-BBO-11818 is an orally active, highly selective (relative to NRAS and HRAS), non-covalent pan-KRAS inhibitor (IC50=28-120 nM). (S,R,S)-BBO-11818 specifically binds to the Switch-II/Helix 3 pocket, disrupts the KRAS:RAF1 interaction by inducing conformational changes, and blocks the MAPK signaling pathway. (S,R,S)-BBO-11818 exhibits significant anti-tumor activity, which not only inhibits cell proliferation and induces apoptosis, but also drives tumor regression in xenograft models. (S,R,S)-BBO-11818 produces synergistic effects when combined with Cetuximab (HY-P9905), anti-PD-1 antibody or PI3Kα inhibitor. (S,R,S)-BBO-11818 is used in the research of KRAS mutation-related malignancies such as pancreatic cancer, non-small cell lung cancer and colorectal cancer .
|
-
- HY-183684
-
|
|
RET
VEGFR
PDGFR
Akt
ERK
|
Endocrinology
Cancer
|
|
RET-IN-33 is a moderately selective inhibitor of RET mutants. RET-IN-33 potently inhibits G810 mutants, with IC50 values of 4.43 nM (G810R), 3.28 nM (G810C) and 0.51 nM (G810S), respectively. RET-IN-33 also inhibits other RET mutants: V804M (IC50 0.73 nM), V804L (IC50 0.36 nM), Y806H (IC50 0.74 nM) and M918T (IC50 0.55 nM). RET-IN-33 also inhibits other kinases, with an IC50 of 1.50 nM against VEGFR2 and 1.60 nM against PDGFRα. RET-IN-33 blocks the autophosphorylation of RET mutants and the downstream SHC/AKT/ERK signaling pathway. RET-IN-33 selectively inhibits the proliferation of RET-driven cell models without affecting non-RET-dependent or normal cells. RET-IN-33 exhibits dose-dependent antitumor efficacy in RET-driven xenograft models. RET-IN-33 can be used for the research of medullary thyroid carcinoma, papillary thyroid carcinoma and non-small cell lung cancer .
|
-
- HY-172795
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-158 (compound 12e) is an orally active EGFR inhibitor with an IC50 of 0.22 nM for EGFR(Del19/T790M). EGFR-IN-158 inhibits phosphorylation and downstream signaling by binding to EGFR, thereby inhibiting the proliferation of tumor cell lines and promoting apoptosis .
|
-
- HY-N6871
-
|
|
Bacterial
IKK
Ferroptosis
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
Abietic acid, an orally active diterpene isolated from Colophony, displays significant anti-proliferative, anti-inflammatory, anti-obesity effect, bacteriostatic, cell cycle arresting and pro-apoptotic activities. Abietic acid inhibits lipoxygenase activity for allergy. Abietic acid enhances cell migration and tube formation in HUVECs. Abietic acid induces significant angiogenic potential, which is associated with upregulation of extracellular signal-regulated kinase (ERK) and p38 expression. Abietic acid attenuates sepsis-induced lung injury by inhibiting nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway to inhibit M1 macrophage polarization. Abietic acid exhibits a positive effect against liver injury by attenuating inflammation and ferroptosis. Abietic acid shows accelerated wound closure in a mouse model of cutaneous wounds. Abietic acid significantly reduces the proliferation and growth of NSCLC cells by IKKβ inhibition.Additionally, Abietic acid ameliorates psoriasis-like inflammation and modulates gut microbiota in mice. Abietic acid is promising for research in non-small-cell lung cancer (NSCLC), liver injury-related deseases and psoriasis .
|
-
- HY-180818
-
|
|
Anaplastic lymphoma kinase (ALK)
Apoptosis
|
Cancer
|
|
ALK-IN-33 (Compound 8q) is an orally active ALK inhibitor with an IC50 of 1.61 nM. ALK-IN-33 exhibits significant selective killing effect on ALK-positive cancer cells. ALK-IN-33 induces cell cycle arrest and apoptosis, effectively weakening the migration, invasion and long-term survival ability of cancer cells. ALK-IN-33 can be used for research on non-small cell lung cancer
|
-
- HY-N3980R
-
|
Champacol (Standard); Guaiac alcohol (Standard)
|
Reference Standards
Autophagy
RAD51
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Guaiol (Standard) is the analytical standard of Guaiol. This product is intended for research and analytical applications. Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
|
-
- HY-N3980
-
Guaiol
1 Publications Verification
Champacol; Guaiac alcohol
|
Autophagy
RAD51
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
|
-
- HY-P99275
-
|
AMG-888; U3-1287
|
EGFR
Akt
ERK
PARP
Survivin
|
Cancer
|
|
Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of EGFR, HER2, HER3, ERK, and AKT. Patritumab also induces cell apoptosis and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors .
|
-
- HY-N0164R
-
|
Matridin-15-one (Standard); Vegard (Standard); α-Matrine (Standard)
|
PINK1/Parkin
Reference Standards
Opioid Receptor
Autophagy
Mitophagy
Ferroptosis
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Matrine (Standard) is the analytical standard of Matrine. This product is intended for research and analytical applications. Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI) .
|
-
- HY-N0164
-
Matrine
Maximum Cited Publications
18 Publications Verification
Matridin-15-one; Vegard; α-Matrine
|
PINK1/Parkin
Opioid Receptor
Autophagy
Mitophagy
Ferroptosis
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI) .
|
-
- HY-183912
-
|
|
Topoisomerase
ADC Payload
|
Cancer
|
|
PY-4Car2 is a Camptothecin (HY-16560) derivative and a topoisomerase I inhibitor. PY-4Car2 functions as a warhead conjugated via a cleavable linker to the bispecific ADC TJ101. PY-4Car2 can be used as an ADC payload for the research of cancers .
|
-
- HY-185075
-
|
LY4050784
|
SWI/SNF Complex
|
Cancer
|
|
FHD-909 (LY4050784) is an orally active and selective SMARCA2 (BRM) ATPase inhibitor. FHD-909 potently inhibits purified BRM ATPase with an IC50 of 0.0025 μM and exhibits 35.69-fold selectivity for BRM over purified SMARCA4 (BRG1) ATPase. FHD-909 induces synthetic lethality, suppresses cell proliferation, modulates target gene expression, and achieves remarkable tumor growth inhibition and regression in SMARCA4-mutant cancer cells and xenograft models. FHD-909 can be used for the research of SMARCA4/BRG1-mutant cancers, advanced solid tumors, and BAF complex-related disorders .
|
-
- HY-P991995
-
|
OMTX705 antibody
|
ADC Antibody
FAP
|
Cancer
|
|
OMTX005 (OMTX705 antibody) is a humanized anti-FAP IgG1 monoclonal antibody that specifically binds to human (EC50: 0.33 nM)/mouse (EC50: 0.14 nM) FAP proteins and FAP-positive cells. OMTX005 exhibits no cytotoxicity when used alone and fails to induce an increase in caspase 3/7 activity in relevant cells. OMTX005 can be used to synthesize the ADC molecule OMTX705 for tumor research .
|
-
- HY-170428
-
|
|
Molecular Glues
Ras
Ligands for E3 Ligase
|
Cancer
|
|
IPS-06061 is an orally active molecular glue forming a ternary complex of CRBN-KRAS G12D-IPS06061, degrading KRAS G12D with a DC50 value lower than 500 nM. IPS-06061 shows a strong anti-tumor efficacy .
|
-
- HY-169061
-
|
|
Histone Methyltransferase
Aminotransferases (Transaminases)
Lactate Dehydrogenase
|
Cancer
|
|
WQQ-345 is an orally active BCAT1 inhibitor with an IC50 values of 10.8 mM. WQQ-345 reduces cellular α-KG levels, upregulating H3K27me3 expression, decreasing glycolytic enzyme expression, and impairing glycolysis activity. WQQ-345 reduces colony formation, suppresses growth of BCAT1-high TKI-resistant lung cancer cells. WQQ-345 exerts in vitro and in vivo antitumor activity. WQQ-345 can be used for the research of TKI-resistant non-small cell lung cancer and TKI-resistant lung cancer .
|
-
- HY-141598
-
|
DS-1062 (solution); Dato-DXd (solution)
|
TROP2
Antibody-Drug Conjugates (ADCs)
Topoisomerase
|
Cancer
|
|
Datopotamab deruxtecan (DS-1062) solution is a TROP2-targeted antibody-drug conjugate (ADC) with human TROP2 Kd of 0.74 nmol/L. Datopotamab deruxtecan solution consists of the antibody Datopotamab (HY-P99843) and the toxic molecule-linker conjugate Deruxtecan (HY-13631E). Datopotamab deruxtecan solution binds TROP2, triggers internalization and lysosomal trafficking and releases DXd topoisomerase I inhibitor payload. Datopotamab deruxtecan solution disrupts DNA function, induces DNA damage, apoptosis, and bystander killing of tumor microenvironment cells. Datopotamab deruxtecan solution can be used in research related to triple-negative breast cancer, gastric cancer, and non-small cell lung cancer .
|
-
- HY-183277
-
|
|
EGFR
p38 MAPK
Akt
Apoptosis
|
Cancer
|
|
EGFR-IN-209 (Compound 6g) is an orally active, selective EGFR Del19/T790M/C797S inhibitor with an IC50 of 0.056 μM. EGFR-IN-209 blocks the phosphorylation of EGFR and its downstream effector molecules (pMAPK, pAKT). EGFR-IN-209 induces Apoptosis. EGFR-IN-209 exhibits antitumor activity against Osimertinib (HY-15772)-resistant non-small cell lung cancer. EGFR-IN-209 can be used in research related to non-small cell lung cancer .
|
-
- HY-164548
-
|
|
HSP
Apoptosis
PI3K
Akt
NF-κB
|
Inflammation/Immunology
Cancer
|
|
WK88-1 is an apoptosis inducer and Hsp90 client protein inhibitor with antiproliferative and immunomodulatory activities. WK88-1 inhibits signaling pathways such as PI3K/Akt and NF-κB, and induces mitochondrial dysfunction and cell cycle arrest. WK88-1 effectively suppresses cancer cell migration and invasion, and reverses various EGFR mutations and resistance to Gefitinib (HY-50895). WK88-1 also regulates the differentiation of monocytes and dendritic cells, blocks the expression of multiple chemokines, inhibits immune cell migration and M1 marker transcription, and restores impaired endocytic activity. WK88-1 has been used in studies of breast cancer, non-small cell lung cancer with various EGFR mutations or Met amplification, and atherosclerosis and other related diseases .
|
-
- HY-173629
-
|
|
Ras
Apoptosis
|
Cancer
|
|
RMC-5127 is a small molecule inhibitor that binds to GTP-targeted KRAS G12V, with oral bioavailability and blood-brain barrier permeability. RMC-5127 inhibits the activities of the RAS and MAPK pathways, suppresses the proliferation of KRAS G12V-mutant cancer cells and induces their apoptosis. RMC-5127 can be used for the research of KRAS G12V-mutant non-small cell lung cancer, pancreatic ductal adenocarcinoma, colorectal cancer and intracranial KRAS G12V tumors .
|
-
- HY-181477
-
|
|
ERK
Apoptosis
Bcl-2 Family
Caspase
Reactive Oxygen Species (ROS)
|
Cancer
|
|
ERK5-IN-7 is an orally active ERK5 inhibitor with an IC50 of 403.4 nM. ERK5-IN-7 directly inhibits ERK5 kinase activity, and downregulates the phosphorylation level and total protein expression of ERK5. ERK5-IN-7 induces Apoptosis (upregulates Bax, downregulates Bcl-2, and induces Caspase-3 cleavage). ERK5-IN-7 induces ROS accumulation. ERK5-IN-7 exhibits anticancer effects against Lewis lung cancer .
|
-
- HY-124084
-
|
|
Stearoyl-CoA Desaturase (SCD)
|
Cancer
|
|
SW203668 is an irreversible stearoyl CoA desaturase (SCD) inhibitor with an IC50 of 54 nM. SW203668 covalently binds and inhibits SCD, depletes unsaturated fatty acids, and triggers cell death in sensitive cells. SW203668 requires demethylation by CYP4F11 to form its active SCD-inhibiting form; differential CYP4F11 expression drives selective cytotoxicity. SW203668 exerts cytotoxicity toward CYP4F11-expressing non-small cell lung cancer (NSCLC) cells and spares CYP4F11-lacking NSCLC cells. SW203668 inhibits tumor growth in immunodeficient mice bearing CYP4F11-expressing NSCLC xenografts and spares mouse skin sebocytes. SW203668 can be used for the research of non-small cell lung cancer .
|
-
- HY-181964
-
|
|
|
Cancer
|
|
KRAS G12C-IN-77 is an orally active and selective KRAS G12C covalent dual-state inhibitor that binds with high affinity to both GDP-bound (inactive state) and GTP-bound (active state) KRAS G12C (IC50 = 133 nM). KRAS G12C-IN-77 rapidly inhibits ERK1/2 phosphorylation, induces the formation of covalent adducts with endogenous KRAS G12C, suppresses the expression of MAPK pathway genes, and inhibits the proliferation of KRAS G12C-mutant cells. KRAS G12C-IN-77 is applicable to research related to KRAS G12C-mutant solid tumors, including pancreatic ductal adenocarcinoma and non-small cell lung cancer .
|
-
- HY-P99866
-
|
MEHD-7945A; RG 7597
|
EGFR
Akt
p38 MAPK
Apoptosis
|
Cancer
|
|
Duligotuzumab (MEHD-7945A; RG 7597) is a humanized IgG-κ monoclonal antibody targeting EGFR. Duligotuzumab blocks the binding of ligands to these two receptors, inhibits downstream HER/ErbB, AKT and MAPK signaling pathways, induces antibody-dependent cellular cytotoxicity, reduces the proliferation and migration abilities of cancer cells, promotes apoptosis, exerts radiosensitizing effects, and reverses EGFR resistance in cancer cells. Duligotuzumab can be used in tumor-related research .
|
-
- HY-158143
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
AZD3470 is an orally active MTA-cooperative PRMT5 inhibitor, selective for MTAP-deficient tumors. AZD3470 induces cell cycle G2/M phase alterations, DNA damage, apoptosis, and symmetric dimethylarginine reduction. AZD3470 alters alternative splicing, increases skipped exon events in DNA repair and cell cycle pathways, and inhibits cancer cell proliferation and tumor growth. AZD3470 can be used for the research of non-small cell lung cancer and MTAP-deleted solid tumors .
|
-
- HY-182624
-
|
|
Na+/H+ Exchanger (NHE)
Wnt
Apoptosis
|
Cancer
|
|
FJ9 is a NHERF1/PDZ inhibitor with human NHERF1 PDZ1 IC50 1540 μM, NHERF1 PDZ2 IC50 160 μM, and Frizzled-7-Dishevelled PDZ complex Ki 10 μM. FJ9 binds ligand-binding pockets of NHERF1 PDZ domains to block cognate ligand interactions, disrupts Frizzled-7-Dishevelled interactions, and down-regulates canonical Wnt signaling. FJ9 induces apoptosis in cancer cells with intact β-catenin signaling. FJ9 can be used for the research of non-small cell lung cancer, melanoma .
|
-
- HY-171821
-
|
SGN-PDL1V
|
Antibody-Drug Conjugates (ADCs)
PD-1/PD-L1
|
Cancer
|
|
PF-08046054 (SGN-PDL1V) is a PD-L1-directed Antibody-drug conjugate (ADC), which is comprised of an anti-PD-L1 antibody conjugated to VcMMAE (HY-15575). PF-08046054 is direct cytotoxicity to PD-L1-expressing tumor cells via the intracellular delivery of MMAE. PF-08046054 can be used for the study of solid tumors
|
-
- HY-185683
-
|
DB-1311; BNT324
|
Antibody-Drug Conjugates (ADCs)
Topoisomerase
CD276/B7-H3
|
Cancer
|
|
Elfetabart drozuntecan (DB-1311; BNT324) is an antibody-drug conjugate (ADC) targeting B7H3. Elfetabart drozuntecan conjugates a humanized anti-B7H3 IgG1 monoclonal antibody with a topoisomerase I inhibitor via a cleavable linker. Elfetabart drozuntecan exerts antitumor activity in solid tumors. Elfetabart drozuntecan can be used for the research of advanced/metastatic solid tumors .
|
-
- HY-114214
-
|
|
Drug Derivative
NF-κB
MMP
TNF Receptor
Interleukin Related
Cyclin G-associated Kinase (GAK)
CDK
PI3K
Akt
|
Inflammation/Immunology
Cancer
|
|
CKD-712 is an orally active multi-target tetrahydroisoquinoline derivatived and a potent inhibitor of the NF-κB pathway . CKD-712 selectively inhibits MMP-9 with no effect on MMP-2, downregulates the expression of TNF-α, IL-6, cyclin A, cyclin B, CDK-1 and other proteins, and activates the PI3K/Akt signaling pathway . CKD-712 blocks the activation and nuclear translocation of NF-κB, downregulates inflammatory factors and pro-tumor metastatic proteins, and induces G2/M phase arrest in tumor cells and thereby inhibits the invasion of cancer cells . CKD-712 can be used for the research of sepsis, myocardial ischemia-reperfusion injury and non-small cell lung cancer .
|
-
-
- HY-141598
-
|
DS-1062 (solution); Dato-DXd (solution)
|
蛍光色素
|
|
Datopotamab deruxtecan (DS-1062) solution is a TROP2-targeted antibody-drug conjugate (ADC) with human TROP2 Kd of 0.74 nmol/L. Datopotamab deruxtecan solution consists of the antibody Datopotamab (HY-P99843) and the toxic molecule-linker conjugate Deruxtecan (HY-13631E). Datopotamab deruxtecan solution binds TROP2, triggers internalization and lysosomal trafficking and releases DXd topoisomerase I inhibitor payload. Datopotamab deruxtecan solution disrupts DNA function, induces DNA damage, apoptosis, and bystander killing of tumor microenvironment cells. Datopotamab deruxtecan solution can be used in research related to triple-negative breast cancer, gastric cancer, and non-small cell lung cancer .
|
-
- HY-171821
-
|
SGN-PDL1V
|
蛍光色素
|
|
PF-08046054 (SGN-PDL1V) is a PD-L1-directed Antibody-drug conjugate (ADC), which is comprised of an anti-PD-L1 antibody conjugated to VcMMAE (HY-15575). PF-08046054 is direct cytotoxicity to PD-L1-expressing tumor cells via the intracellular delivery of MMAE. PF-08046054 can be used for the study of solid tumors
|
-
- HY-15947G
-
|
GDC-0994
|
蛍光色素
|
|
Ravoxertinib GMP is Ravoxertinib (HY-15947) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Ravoxertinib (GDC-0994) is an orally active ERK1/2 inhibitor. Ravoxertinib inhibits the ERK1/2 MAPK signaling pathway and reduces the expression levels of c-Myc, HK2 and LDHA. Ravoxertinib decreases mammosphere formation, and exerts additive and/or superadditive cytotoxicity when combined with Ipatasertib (HY-15186) in 3D tumor sphere models. Ravoxertinib can be used in research related to various cancers including breast cancer, melanoma, head and neck cancer, non-small cell lung cancer, ovarian cancer and Merkel cell carcinoma .
|
-
- HY-15947G
-
|
GDC-0994
|
生化学アッセイ試薬
|
|
Ravoxertinib GMP is Ravoxertinib (HY-15947) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Ravoxertinib (GDC-0994) is an orally active ERK1/2 inhibitor. Ravoxertinib inhibits the ERK1/2 MAPK signaling pathway and reduces the expression levels of c-Myc, HK2 and LDHA. Ravoxertinib decreases mammosphere formation, and exerts additive and/or superadditive cytotoxicity when combined with Ipatasertib (HY-15186) in 3D tumor sphere models. Ravoxertinib can be used in research related to various cancers including breast cancer, melanoma, head and neck cancer, non-small cell lung cancer, ovarian cancer and Merkel cell carcinoma .
|
-
- HY-156002
-
|
Paluratide
|
Ras
ERK
|
Cancer
|
|
LUNA18 is an orally-available cyclic peptide KRAS and ERK inhibitor. LUNA18 phosphorylates ERK and AKT and decreases cell proliferation in RAS-mutated cancer cells. LUNA18 exhibits RAS signal inhibition and potent anti-cancer activities through inhibiting interaction between RAS and guanine nucleotide exchange factors (GEFs) in a mouse xenograft model. LUNA18 shows significant cellular efficacy against cell lines with KRAS genetic alterations, such as colon cancer, stomach cancer, non-small cell lung cancer and pancreaticcancer .
|
| 製品番号 |
製品名 |
Target |
研究分野 |
Image |
-
- HY-P99275
-
|
AMG-888; U3-1287
|
EGFR
Akt
ERK
PARP
Survivin
|
Cancer
|
|
Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of EGFR, HER2, HER3, ERK, and AKT. Patritumab also induces cell apoptosis and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors .
|
-
(5)
-
- HY-P9964
-
|
11F8; IMC-11F8; LY3012211
|
EGFR
|
Cancer
|
|
Necitumumab (11F8; IMC-11F8; LY3012211) is a human IgG monoclonal antibody directed against EGFR. Necitumumab binds to the EGF binding site of EGFR, blocks ligand binding, neutralizes ligand-induced EGFR phosphorylation and downstream signaling, induces EGFR internalization and degradation, and mediates antibody-dependent cellular cytotoxicity (ADCC) in EGFR-expressing cells. Necitumumab enhances antitumour activity in combination with Gemcitabine (HY-17026) and Cisplatin (HY-17394) in murine non-small-cell lung cancer xenograft models. Necitumumab can be used in research on cancers such as non-small cell lung cancer and colorectal cancer .
|
-
(5)
-
- HY-P99866
-
|
MEHD-7945A; RG 7597
|
EGFR
Akt
p38 MAPK
Apoptosis
|
Cancer
|
|
Duligotuzumab (MEHD-7945A; RG 7597) is a humanized IgG-κ monoclonal antibody targeting EGFR. Duligotuzumab blocks the binding of ligands to these two receptors, inhibits downstream HER/ErbB, AKT and MAPK signaling pathways, induces antibody-dependent cellular cytotoxicity, reduces the proliferation and migration abilities of cancer cells, promotes apoptosis, exerts radiosensitizing effects, and reverses EGFR resistance in cancer cells. Duligotuzumab can be used in tumor-related research .
|
-
(5)
-
- HY-P991669
-
|
AML-01
|
Caspase
Apoptosis
|
Cancer
|
|
IGN523 is an anti-CD98 antibody (hCD98, KD = 0.55 nM). IGN523 induces antibody-dependent cell-mediated cytotoxicity (ADCC) activity, lysosomal membrane permeabilization, and inhibition of essential amino acid transport, ultimately leading to caspase-3 and caspase-7-mediated apoptosis of tumor cells. IGN523 inhibits tumor growth in multiple tumor xenograft models. IGN523 is useful in the research of non-small cell lung cancer (NSCLC), acute myeloid leukemia (AML), and other cancers. .
|
-
(5)
-
- HY-P99943
-
|
KN-046
|
PD-1/PD-L1
CTLA-4
|
Cancer
|
|
Erfonrilimab (KN-046) is a monoclonal antibody targeting PD-L1/CTLA-4. Erfonrilimab blocks the PD-L1 and CTLA-4 pathways, thereby regulating T cell function. Erfonrilimab enhances the secretion of IL-2 in superantigen-stimulated peripheral blood mononuclear cells. Erfonrilimab inhibits tumor growth in xenograft and double gene knock-in mouse models. Erfonrilimab can be used in research related to a variety of advanced solid tumors, including non-small cell lung cancer and nasopharyngeal carcinoma.
|
-
(5)
-
- HY-P990947
-
|
AZD9592 Antibody
|
ADC Antibody
EGFR
|
Cancer
|
|
Tilatamig (AZD9592 Antibody) is a human antibody of the Ig (G1-κ_G1-λ2) subtype that targets EGFR/MET. Tilatamig conjugates with the Top1 inhibitor AZ14170133 (HY-145399) to form the antibody-drug conjugate (ADC) Tilatamig samrotecan (HY-171124) (AZD9592). Tilatamig accurately targets NSCLC models including EGFR-mutant, EGFR-wildtype, and EGFR tyrosine kinase inhibitor-treated ones, and its activity correlates with high expression of EGFR, c-MET and SLFN11. Tilatamig is available for in vivo anti-tumor studies in patient-derived xenograft models of non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC) .
|
-
(5)
-
- HY-P99658A
-
-
(5)
-
- HY-P992163
-
|
|
Fc Receptor (FcR)
C-type Lectin-like Receptors (CTLRs)
|
Inflammation/Immunology
Cancer
|
|
23ME-01473 is an anti-ULBP6/2/5 antibody with enhanced Fc effector function, with a Kd of 0.053 nmol/L against hULBP6, 0.23 nmol/L against hULBP2, and 1.92 nmol/L against hULBP5. 23ME-01473 restores anti-tumor immunity by activating NKG2D and FcγRIIIa. 23ME-01473 exerts anti-cancer activity in non-small cell lung cancer PDX models. 23ME-01473 can be used for the research of non-small cell lung cancer .
|
-
(5)
-
- HY-P992146
-
|
MYTX-011 Antibody; Q-397
|
ADC Antibody
c-Met/HGFR
|
Cancer
|
|
Zevontabart (MYTX-011 Antibody; Q-397) is a pH-dependent anti-c-MET antibody. Zevontabart regulates the trafficking process of c-MET to reduce receptor recycling, and enhances its own endocytosis and accumulation in c-MET-expressing cells. Zevontabart induces cytotoxicity in solid tumor cells and exerts anti-tumor activity in a non-small cell lung cancer xenograft mouse model. Zevontabart can be used to synthesize ADC, such as: MYTX-011. Zevontabart can be used in studies related to non-small cell lung cancer, with its corresponding isotype control being Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
(5)
-
- HY-P992323
-
|
|
VEGFR
Tie
ERK
|
Cardiovascular Disease
Cancer
|
|
BI-836880 is a humanized bispecific nanobody and a selective inhibitor of VEGF and ANG2, with a Kd of 16 pM for hANG2, an EC50 of 1.4 nM for VEGF165, and an EC50 of 2.3 nM for VEGF121. BI-836880 blocks ERK phosphorylation downstream of VEGF-A as well as TIE2 phosphorylation downstream of ANG2. BI-836880 does not inhibit ANG1-mediated TIE2 phosphorylation. BI-836880 exerts anti-angiogenic effects, reduces the number of immature endothelial vessels in tumor tissues, and inhibits tumor growth in preclinical models. BI-836880 can be used in the research of pancreatic cancer, non-small cell lung cancer, renal cell carcinoma, ovarian cancer, colon cancer, and Lewis lung cancer .
|
-
(5)
-
- HY-P991954
-
|
|
Complement System
Syk
|
Inflammation/Immunology
Cancer
|
|
GT103 is a human-derived monoclonal antibody targeting complement factor H (CFH). GT103 binds to a conformationally distinct epitope of CFH on tumor cells. GT103 activates the classical complement pathway, induces complement-dependent cytotoxicity, and triggers antibody-dependent cellular phagocytosis (ADCP) of tumor cells. GT103 increases calreticulin translocation to tumor cell plasma membranes. GT103 mediates B-cell activation via Syk kinase phosphorylation. GT103 inhibits tumor growth and metastasis in animal models. GT103 can be used for the research of non-small cell lung cancer .
|
-
(5)
-
- HY-P992369
-
|
|
VISTA
|
Cancer
|
|
HMBD-002 is an Fc-independent, non-depleting IgG4 subclass antibody that targets VISTA and VSIG3. It is widely used in research related to various solid tumors, including colon cancer, triple-negative breast cancer, and non-small cell lung cancer. HMBD-002 blocks the interactions of VISTA with VSIG3 and LRIG1, relieves immunosuppression without depleting VISTA-positive cells, activates the cytotoxic program of CD8 + T cells, and drives the type I interferon signaling pathway. HMBD-002 reprograms tumor-associated macrophages to the M1 phenotype, reduces tumor infiltration of inhibitory myeloid cells, thereby significantly inhibiting tumor growth and improving survival. HMBD-002 is well tolerated in rodent and non-human primate animal models .
|
-
(5)
-
- HY-P991995
-
|
OMTX705 antibody
|
ADC Antibody
FAP
|
Cancer
|
|
OMTX005 (OMTX705 antibody) is a humanized anti-FAP IgG1 monoclonal antibody that specifically binds to human (EC50: 0.33 nM)/mouse (EC50: 0.14 nM) FAP proteins and FAP-positive cells. OMTX005 exhibits no cytotoxicity when used alone and fails to induce an increase in caspase 3/7 activity in relevant cells. OMTX005 can be used to synthesize the ADC molecule OMTX705 for tumor research .
|
-
(5)
| 製品番号 |
製品名 |
Category |
Target |
構造式 |
-
- HY-N0164
-
-
-
- HY-N6871
-
|
|
Infection
Colophony
Classification of Application Fields
Pinaceae
Ketones, Aldehydes, Acids
Metabolic Disease
Plants
Inflammation/Immunology
Disease Research Fields
|
Bacterial
IKK
Ferroptosis
|
Abietic acid, an orally active diterpene isolated from Colophony, displays significant anti-proliferative, anti-inflammatory, anti-obesity effect, bacteriostatic, cell cycle arresting and pro-apoptotic activities. Abietic acid inhibits lipoxygenase activity for allergy. Abietic acid enhances cell migration and tube formation in HUVECs. Abietic acid induces significant angiogenic potential, which is associated with upregulation of extracellular signal-regulated kinase (ERK) and p38 expression. Abietic acid attenuates sepsis-induced lung injury by inhibiting nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway to inhibit M1 macrophage polarization. Abietic acid exhibits a positive effect against liver injury by attenuating inflammation and ferroptosis. Abietic acid shows accelerated wound closure in a mouse model of cutaneous wounds. Abietic acid significantly reduces the proliferation and growth of NSCLC cells by IKKβ inhibition.Additionally, Abietic acid ameliorates psoriasis-like inflammation and modulates gut microbiota in mice. Abietic acid is promising for research in non-small-cell lung cancer (NSCLC), liver injury-related deseases and psoriasis .
|
-
-
- HY-N0600
-
-
-
- HY-N3980
-
Guaiol
1 Publications Verification
Champacol; Guaiac alcohol
|
Infection
Structural Classification
Classification of Application Fields
Terpenoids
Sesquiterpenes
Distemonanthus benthamianus Baill.
Plants
Compositae
Disease Research Fields
Source Classification
|
Autophagy
RAD51
|
|
Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
|
-
-
- HY-113418
-
-
-
- HY-121811
-
|
Lanceolatin C
|
Structural Classification
Pongamia pinnata (L.) Pierre
Leguminosae
Ketones, Aldehydes, Acids
Derris trifoliata Lour.
Plants
Source Classification
|
Glycosidase
Phosphatase
Interleukin Related
TNF Receptor
COX
Beclin1
GLUT
FAK
Akt
mTOR
p38 MAPK
Keap1-Nrf2
Apoptosis
Amyloid-β
Tau Protein
Autophagy
|
|
Pongamol (Lanceolatin C) is an orally active flavonoid with an IC50 of 75 μM and a Ki of 58 μM against PTPase-1B, and an IC50 of 103.5 μM against intestinal α-Glycosidase. Pongamol reduces the release of IL‑1β, TNF‑α, COX‑2 and iNOS in cells, reverses the nuclear translocation of NF‑κB, and upregulates the levels of Beclin 1 and LC3 Ⅱ/LC3 Ⅰ. Pongamol promotes glucose uptake by increasing the level of GLUT4 on the surface of skeletal muscle cells. Pongamol inhibits epithelial-mesenchymal transition by suppressing the FAK/Akt-mTOR signaling pathway. Pongamol inhibits neuronal cytotoxicity, suppresses cell apoptosis and extends the lifespan of Caenorhabditis elegans by activating the MAPKs/Nrf2 signaling pathway. Pongamol exerts hypoglycemic effects in diabetic mouse models. Pongamol exhibits antibacterial activity. Pongamol alleviates oxidative stress, neuroinflammation, Aβ deposition and excessive phosphorylation of Tau Protein, and restores autophagy function in Alzheimer's disease mouse models by inhibiting the Akt/mTOR signaling pathway. Pongamol is applicable to research related to Alzheimer's disease, type 2 diabetes, non-small cell lung cancer and postprandial hyperglycemia .
|
-
-
- HY-N7694
-
-
-
- HY-N2199
-
|
|
Structural Classification
Flavonoids
Classification of Application Fields
Phenols
Polyphenols
Selaginellaceae
Plants
Biflavones
Selaginella tamariscina (P. Beauv.) Spring
Disease Research Fields
Source Classification
Cancer
|
Apoptosis
Autophagy
PI3K
JNK
mTOR
p38 MAPK
CDK
MMP
TGF-beta/Smad
STAT
β-catenin
Reactive Oxygen Species (ROS)
Bcl-2 Family
Caspase
|
|
Sotetsuflavone is a flavonoid that can be isolated from Cycas revolute. Sotetsuflavone inhibits phosphorylation of PI3K, Akt, mTOR, JNK, and p38 MAPK; modulates expression of Cyclin D1, CDK4, Bcl-2, Bax, cleaved caspases 3/9, MMP-9, TGF-β, STAT3, and β-catenin. Sotetsuflavone induces G0/G1 cell cycle arrest, apoptosis, autophagy, and intracellular ROS elevation, inhibits cancer cell proliferation. Sotetsuflavone inhibits tumor growth in mouse tumor xenograft models. Sotetsuflavone can be used for the research of non-small cell lung cancer and Crohn’s disease .
|
-
-
- HY-N3980R
-
|
Champacol (Standard); Guaiac alcohol (Standard)
|
Structural Classification
天然物
Distemonanthus benthamianus Baill.
Plants
Compositae
Source Classification
|
Reference Standards
Autophagy
RAD51
|
|
Guaiol (Standard) is the analytical standard of Guaiol. This product is intended for research and analytical applications. Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
|
-
-
- HY-N0164R
-
-
-
- HY-180200
-
|
|
|
Alkynes
|
|
RNK08954 is an orally active KRASG12D inhibitor with a Kd of 0.0395 nM. RNK08954 selectively binds the inactive GDP-bound KRASG12D form, suppresses downstream KRAS-mediated signaling pathways p-ERK1/2 experssion. RNK08954 inhibits KRASG12D-mutant cell proliferation, induces G0-G1 cell cycle arrest, and inhibits tumor growth in mouse xenograft models. RNK08954 can be used for the research of non-small cell lung cancer, pancreatic ductal adenocarcinoma .
|
-
- HY-145729
-
|
AZD9150
|
|
Antisense Oligonucleotides
|
|
Danvatirsen (AZD9150) is an antisense oligonucleotide targeting STAT3. Danvatirsen reduces the viability and promotes apoptosis of leukemia cell lines. Danvatirsen inhibits the expression of endogenous STAT3 and its downstream target genes, and reduces the proliferation and tumorigenicity of neuroblastoma and lymphoma cells. Danvatirsen inhibited tumor growth in mouse models of neuroblastoma, lymphoma, and non-small cell lung cancer. Danvatirsen achieves STAT3 mRNA and protein depletion in a mouse model of epidermoid carcinoma. Danvatirsen can be used in research related to lymphoma, myelodysplastic syndrome, acute myeloid leukemia, neuroblastoma and non-small cell lung cancer .
|
-
- HY-145729A
-
|
AZD9150 sodium
|
|
Antisense Oligonucleotides
|
|
Danvatirsen sodium (AZD9150 sodium) is an antisense oligonucleotide targeting STAT3. Danvatirsen sodium reduces the viability and promotes apoptosis of leukemia cell lines. Danvatirsen sodium inhibits the expression of endogenous STAT3 and its downstream target genes, and reduces the proliferation and tumorigenicity of neuroblastoma and lymphoma cells. Danvatirsen sodium inhibited tumor growth in mouse models of neuroblastoma, lymphoma, and non-small cell lung cancer. Danvatirsen sodium achieves STAT3 mRNA and protein depletion in a mouse model of epidermoid carcinoma. Danvatirsen sodium can be used in research related to lymphoma, myelodysplastic syndrome, acute myeloid leukemia, neuroblastoma and non-small cell lung cancer .
|
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