JAK/STAT Signaling

A STAT3 inhibitor

EGFR-kinase inhibitor. Also JAK2, JAK3 inhibitor

STAT3 inhibitor

CORM 2 is a carbon monoxide-releasing molecule that can liberate a controlled amount of CO in biological systems and has been developed as a carbon monoxide donor.

A STAT3 inhibitor

Fedratinib hydrochloride hydrate is an effective, selective, ATP competitive and orally active JAK2 inhibitor, and the IC 50 values for both JAK2 and JAK2V617F kinases are 3nM.

Angoline is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM. Angoline inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.

Angoline hydrochloride is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM. Angoline hydrochloride inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.

SC-43, a Sorafenib derivative, is a potent and orally active SHP-1 (PTPN6) agonist. SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis. SC-43 has anti-fibrotic and anticancer effects.

AS1810722 is an orally active and potent STAT6 inhibitor with an IC50 of 1.9 nM.

Ochromycinone ((Rac)-STA-21) is a natural antibiotic and a STAT3 inhibitor.

(E/Z)-AG490 ((E/Z)-Tyrphostin AG490) is a racemic compound of (E)-AG490 and (Z)-AG490 isomers. (E)-AG490 is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.

Stafib-1 is the first selective inhibitor of the STAT5b SH2 domain, with a Ki of 44 nM and an IC50 of 154 nM.

AC-4-130 is a potent STAT5 SH2 domain inhibitor. AC-4-130 directly binds to STAT5 and disrupts STAT5 activation, dimerization, nuclear translocation, and STAT5-dependent gene transcription. AC-4-130 induces cell cycle arrest and apoptosis in FLT3-ITD-driven leukemic cells. AC-4-130 has anti-cancer activity and can efficiently block pathological levels of STAT5 activity in acute myeloid leukemia (AML).

Stafia-1 is a potent STAT5a inhibitor (K i=10.9 μM, IC50=22.2 μM). Stafia-1 displays high selectivity over STAT5b and other STAT family members.

Stafia-1-dipivaloyloxymethyl ester (compound 27, 0-200 μM) decreases pSTAT5a expression significantly, and has no obvious inhibition on pSTAT5b.

Stafib-2 is a potent and selctive inhibitor of the transcription factor STAT5b, with an IC50 of 82 nM and 1.7 μM for STAT5b and STAT5a, respectively.

(S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitory activity against EGFR exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC50=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK.

(E/Z)-Zotiraciclib ((E/Z)-TG02) hydrochloride is a potent CDK2, JAK2, and FLT3 inhibitor.

BLU-945 is a potent, highly selective, reversible and orally active epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI).

Befotertinib (D-0316) is the third-generation EGFR tyrosine kinase inhibitor. Befotertinib can be used for the research of EGFR T790M-positive non-small cell lung cancer (NSCLC).

Disitamab vedotin is an antibody-drug conjugate (ADC) targeting HER2 protein that is comprised of hertuzumab coupling monomethyl auristatin E (MMAE) via a cleavable linker.

Ifidancitinib (ATI-50002) is a potent and selective inhibitor of JAK kinases 1/3.

BAY 2476568 is a potent and selective EGFR inhibitor, with IC50s of < 0.2 nM for wild-type EGFR and several mutations (EGFRR ex20insSVD, EGFRR ex20insASV, EGFRR ex20insNPG).