JAK/STAT Signaling

TP-3654 is a second-generation Pim kinase inhibitor with Ki values of 5 and 42 nM for Pim-1 and Pim-3, respectively.

Tyrphostin AG 528 is an inhibitor of EGFR and ErbB2 with IC50s of 4.9 and 2.1 uM, respectively.

Upadacitinib is a highly potent, orally administered, and reversible selective Janus kinase 1 (JAK1) inhibitor with an IC 50 value of 0.043μM .

PIM447 is novel pan-PIM kinase inhibitor, including Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase.

PF-06700841 P-Tosylate is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC 50 values of 17nM and 23nM, respectively.

Uzansertib (INCB053914) phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. PIM inhibitor 1 phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines.

A VHL-recruiting PROTAC

Brepocitinib (PF-06700841, PF-841) is a potent inhibitor of Tyk2 and Jak1 with IC50s of 23 nM, 17 nM, 77 nM for Tyk2, Jak1 and Jak2 respectively. It has appropriate in-family selectivity against JAK2 and JAK3.

CH7233163 is a noncovalent ATP-competitive inhibitor for EGFR-Del19/T790M/C797S.

Lapatinib (GW-572016) Ditosylate is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.

RO495 (CS-2667) is a potent inhibitor of Non-receptor tyrosine-protein kinase 2 (TYK2).

SC-1 (1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(4-(4-cyanophenoxy)phenyl)urea, STAT3-IN-7), a Sorafenib analogue and potently inhibits the phosphorylation of STAT3, induces cell apoptosis through SHP-1 dependent STAT3 inactivation.

TG-89 is an inhibitor of JAK2 with IC50 of 11.2 μM.

Propanamide is a potent and selective JAK inhibitor extracted from patent WO2012122452A1, Compound II, has the potential for the skin disorders (such as cutaneous lupus) treatment.

Tyk2-IN-4 (BMS-986165) (BMS-986165) is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain.

Delgocitinib (JTE-052) (JTE-052) is a specific JAK inhibitor with IC50s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.

TyK2-IN-2 (Compoud 18) is a potent and selective TYK2 inhibitor with IC50s of 7 nM, 0.1 μM and 0.05 μM for TYK2 JH2, IL-23 and IFNα, respectively.

Oclacitinib maleate (PF-03394197 maleate) (PF-03394197 maleate) is a novel JAK inhibitor.

Tesevatinib (XL-647) (XL-647; EXEL-7647; KD-019) is an orally available, multi-target tyrosine kinase inhibitor; inhibits EGFR, ErbB2, KDR, Flt4 and EphB4 kinase with IC50s of 0.3, 16, 1.5, 8.7, and 1.4 nM.

JAK inhibitor 1 is an inhibitor of JAK extracted from patent US20170121327A1, compound example 283.

JAK3-IN-6 is a potent, selective irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM.

JAK-IN-1 is a JAK1/2/3 inhibitor with IC50s of 0.26, 0.8 and 3.2 nM, respectively.

Abrocitinib (PF-04965842) is a orally active and selective Janus kinase (JAK) inhibitor with IC 50 values of 29nM and 803nM for JAK1 and JAK2, respectively.

BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 nM and 72 nM, respectively.