JAK/STAT Signaling

Dacomitinib (PF-00299804) drate is an orally active, irreversible pan-ErbB inhibitor.

HTH-01-091 TFA is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM.

HJ-PI01 (10-Acetylphenoxazine) is an orally active Pim-2 inhibitor.

SJF-1528 hemidrate is the hemidrate form of SJF-1528.

Depatuxizumab mafodotin is an antibody-drug conjugate (ADC) that specifically targets the epidermal growth factor receptor (EGFR).

(Rac)-JBJ-04-125-02 acetate is the racemate of JBJ-04-125-02.

limertinib (ASK120067) diTFA is a potent and orally active inhibitor of EGFRT790M (IC50: 0.3 nM) with selectivity over EGFRWT (IC50: 6.0 nM).

Danvatirsen sodium is an antisense oligonucleotide targeting STAT3 with potential antitumor activity.

SIAIS164018 drochloride is a PROTAC-based ALK and EGFR degrader, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively.

SJ1008030 (compound 8) formic is a JAK2 PROTAC which selectively degrades JAK2.

MS9449 is a potent PROTAC EGFR degrader with Kds of 17 nM and 10 nM for EGFR WT and EGFR L858R, respectively.

JAK-IN-21 (Example 4) is a selective and potent JAK inhibitor with IC50s of 1.73, 2.04, 109 and 62.9 nM against JAK1, JAK2, J2V617F and TYK2, respectively.

AK-2292 is a potent and selective STAT5 PROTAC degrader, with a DC50 of 0.10 μM.

LL-K8-22 is a potent, selective and durable CDK8-cyclin C dual degrader, with DC50 values of 2.52 and 2.64 μM, respectively.

Multi-target kinase inhibitor 2 (compound 5K) is a multi-targeted kinase inhibitor, and exhibits activity against EGFR, Her2, VEGFR2, and CDK2 enzymes, with IC50 values ranging from 40 to 204 nM.

EGFR T790M/L858R-IN-2 is a potent and selective EGFRT790M/L858R inhibitor with IC50 values of 3.5, 1290 nM for EGFRT790M/L858R, EGFR WT, respectively.

STAT3-IN-13 (compound 6f) is a potent STAT3 inhibitor.

DHFR-IN-4 is a potent didrofolate reductase (DHFR) inhibitor with an IC50 value of 123 nM.

STAT3-SH2 domain inhibitor 1 is a potent Src Homology 2 (SH2) Domain of STAT3 (STAT3-SH2 domain) inhibitor with a Kd value of 1.57 μM.

SJ988497 is a PROTAC JAK2 degrader.

HX103 is an epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitor (TKI)-based fluorogenic probe.

Larotinib is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with an IC50 of 0.6 nM.

EGFR/HER2-IN-9 (Compound 1) is an EGFR and HER2 inhibitor with IC50s of 3.2, 8.3 and 14 nM against EGFR, EGFR T790M and HER2, respectively.

W1131 TFA is a potent STAT3 inhibitor that induces ferroptosis.