JAK/STAT Signaling

NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist with anti-cancer and anti-proliferative properties.

ENMD-119 (ENMD 1198) (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-119 (ENMD 1198) is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.

ZD-4190 is a potent, orally available inhibitor of the vascular endothelial cell growth factor receptor 2 (VEGFR2) and of epidermal growth factor receptor (EGFR) signalling, used for the treatment of cancer.

BGB-102 (JNJ-26483327) is a potent multi-kinase inhibitor against EGFR, HER2, and HER4 with IC50s of 9.6 nM, 18 nM and 40.3 nM, respectively.

EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation EGFR inhibitor.

GNE-955 is a potent and orally active pan Pim kinase inhibitor with Kis of 0.018, 0.11, 0.08 nM for Pim1, Pim2, Pim3, respectively.

JAK1-IN-4 is a potent and selective JAK1 inhibitor, with IC50s of 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively. JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50, 227 nM).

JAK3-IN-7 is a potent and selective JAK3 inhibitor extracted from patent WO2011013785A1, has an IC50 of <0.01 μM.

A STAT3 inhibitor

A STAT3 inhibitor

Dihydroisotanshinone I is a phenanthrenequinone derivative isolated from the roots of Salvia trijuga , with antioxidant effects.

A highly potent EGFR inhibitor

M-110 is a highly selective, ATP-competitive inhibitor of PIM kinases with a preference for PIM-3 (IC50=47 nM). M-110 inhibits PIM-1 and PIM-2 with similar IC50s of 2.5 μM. M-110 inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 μM.

Pertuzumab (Anti-Human HER2, Humanized Antibody), the first of a new class of agents designated as HER dimerisation inhibitors, is a humanised IgG1 monoclonal antibody (mAb) that sterically binds domain II of the erbB2 receptor.

Trastuzumab is a fully humanized monoclonal antibody directed at HER2 which binds the external domain of the receptor and exerts its action via a combination of antibody-dependent cytotoxicity, reduced shedding of the extracellular domain, inhibition of dimerization and possibly receptor downregulation.

Cetuximab is a chimeric monoclonal antibody generated from fusion of the variable region of the murine anti-EGFR monoclonal antibody M225 and the human IgG1 constant region.

CMD178 is a lead peptide that consistently reduced the expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα signaling and inhibits Treg cell development.

Protosappanin A (PTA), an immunosuppressive ingredient and major biphenyl compound isolated from Caesalpinia sappan L, suppresses JAK2/STAT3-dependent inflammation pathway through down-regulating the phosphorylation of JAK2 and STAT3.

An ErbB3 inhibitor

(1S,3R,5R)-PIM447 (dihydrochloride) an PIM inhibitor extracted from patent US 20100056576 A1, compound example 72, has IC50 values of 0.095 μM for Pim1, 0.522 μM for Pim2 and 0.369 μM for Pim3.

(3R,4S)-Tofacitinib is an less active enantiomer of Tofacitinib.

(3S,4R)-Tofacitinib is an less active enantiomer of Tofacitinib.

(3S,4S)-Tofacitinib is the less active S-enantiomer of Tofacitinib.