JAK/STAT Signaling

Epidermal growth factor (EGF) is an effective epidermal growth factor that stimulates the proliferation of skin cells and is used for wound healing applications.

Fidasimtamab (IBI-315; BH2950) is a recombinant human IgG1 bispecific antibody that can simultaneously target, bind and inhibit HER2 and PD-1 and their downstream signaling pathways, connecting PD-1 expressing T cells with HER2-expressing tumor cells. Fidasimtamab has potential immune-suppressive and anti-tumor activity.

GS-829845 is the main active metabolite of Filgotinib. It is a JAK1 inhibitor, but its potency is about 10 times lower than that of the parent compound and it has a longer half-life.

IST5-002 is an effective inhibitor of Stat5a/b, selectively inhibiting the transcriptional activity of Stat5a/b with IC50 values of 1.5 μM (Stat5a) and 3.5 μM (Stat5b). IST5-002 induces apoptosis and death in prostate cancer cells and chronic myeloid leukemia (CML) cells. IST5-002 can be used for research on prostate cancer and CML.

JAK2/FLT3-IN-1 is an orally effective dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3 respectively. It has anti-cancer activity.

JAK-IN-25 (compound 19) is an effective JAK inhibitor with IC50 values of 6 nM, 21 nM, 8 nM, and 1051 nM for TYK2, JAK1, JAK2, and JAK3 respectively. It inhibits human whole blood IL-12 (HEB IL-12) with an IC50 value of 28 nM. JAK-IN-25 has potential for use in cancer research.

Laprituximab (J2898A) is a humanized IgG1 antibody against EGFR that can be used to synthesize ADC IMGN289.

Larotinib mesylate hydrate is an effective, broad-spectrum, orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target, with an IC50 of 0.6 nM.

LLL12 is a specific small molecule inhibitor of signal transducer and activator of transcription 3 (STAT3) that inhibits STAT3 phosphorylation.

Lumretuzumab (Anti-Human ERBB3 Recombinant Antibody) is a humanized monoclonal antibody that targets HER3 (ERBB3) and can be used for cancer research.

Matuzumab (EMD 72000) is a humanized monoclonal antibody that can block EGFR activation and downstream signaling, inhibiting tumor growth.

NSC-370284 is a selective inhibitor of both 10-11 translocation 1 (TET1) and 5-hydroxymethylcytosine (5hmC). It significantly inhibits TET1 expression levels by targeting STAT3/5.

NSC689857 is an effective inhibitor of EGFR and SCFSKP2, with an IC50 of 36 μM against Skp2-Cks1. NSC689857 can inhibit phosphorylation of p27 (IC50=30 μM). NSC689857 exhibits varying activity in different types of cancer, with higher resistance activity against leukemia cell lines compared to other cancer cells.

OSM-SMI-10B is a derivative of OSM-SMI-10. Co-incubation of OSM-SMI-10B with Oncostatin M (OSM) significantly reduces STAT3 phosphorylation induced by OSM in cancer cells.

Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody targeting ERBB3. Patritumab has synergistic effects with Cetuximab and can effectively inhibit the phosphorylation of EGFR, HER2, HER3, ERK and AKT. Patritumab also induces apoptosis and inhibits the growth of pancreatic, non-small cell lung cancer and colorectal cancer xenograft tumors.

Petosemtamab (MCLA 158) is a monoclonal antibody (mAb) that targets both EGFR (Kd: 0.22 nM) and LGR5 (Kd: 0.86 nM). Petosemtamab blocks EGFR signaling and receptor degradation in LGR5+ cancer cells. It can be used for research on solid tumors such as head and neck squamous cell carcinoma (HNSCC), metastatic colorectal cancer (CRC), etc.

Ponezumab (PF-04360365) is a humanized monoclonal antibody against amyloid beta protein of the IgG2 class. Ponezumab can reduce Aβ levels in the central nervous system and improve performance in various learning and memory models in mice. Ponezumab can be used for research on Alzheimer's disease.

Pumecitinib is a JAK inhibitor with anti-inflammatory activity.

(R,R)-VVD-118313 is an isomer of VVD-118313. VVD-118313 is a selective JAK1 inhibitor that can block JAK1-dependent phosphorylation and cytokine signaling. VVD-118313 can be used for cancer research.

Ruserontinib (SKLB1028) is an orally active inhibitor of EGFR, FLT3, and Abl kinases with an IC50 value of 55 nM against human FLT3. It has anti-tumor activity.

Salviolone is a natural diterpenoid derivative that can combat melanoma cells. Salviolone exhibits multifunctional effects on melanoma by blocking cell cycle progression, STAT3 signaling, and the malignant phenotype of A375 melanoma cells.

STAT3-IN-11 (7a) is a selective inhibitor of STAT3 that can inhibit the phosphorylation of the pTyr705 site on STAT3. It can also inhibit downstream genes (Survivin and Mcl-1) without affecting upstream tyrosine kinases (Src and JAK2) and p-STAT1 expression. STAT3-IN-11 can induce apoptosis in cancer cells, making it a promising candidate for the discovery of STAT3 inhibitors and anti-tumor agents.

STAT3-IN-12 is an effective STAT3 signaling inhibitor that can suppress the activation of the IL-6-induced JAK/STAT3 signaling pathway. It can inhibit cancer cell growth and migration, induce apoptosis (cell death), and block cell cycle progression. STAT3-IN-12 can be used in cancer-related research such as hepatocellular carcinoma (HCC) and esophageal cancer.

W1131 is an effective STAT3 inhibitor that can induce ferroptosis. W1131 inhibits cancer progression in gastric cancer subcutaneous xenograft models, organoid models, and PDX models. W1131 effectively reduces chemoresistance of cancer cells to 5-FU. W1131 regulates cell cycle, DNA damage response, and oxidative phosphorylation pathways including the IL6-JAK-STAT3 pathway and ferroptosis pathway.