Itacitinib is an oral selective JAK1 tyrosine kinase inhibitor, which is potential for the treatment of rheumatoid arthritis, myelofibrosis, rheumatoid arthritis and plaque psoriasis.

WHI-P258 is a quinazoline compound that binds to the active site of JAK3 with an estimated Ki of 72 µM, but does not inhibit JAK3 and does not affect the thrombin-induced aggregation of platelets even at 100 μM[1][2].

Cerdulatinib HCl is a dual JAK/SYK inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. It also inhibits other kinases with IC50 less than 200 nM.

Abrocitinib is a potent and selective JAK1 inhibitor with IC50s of 29 and 803nM for JAK1 and JAK2, respectively.

(3R,4S)-Tofacitinib is an isomer of tofacitinib, an inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent against JAK2 and JAK1.

Solcitinib is a highly selective JAK1 inhibitor with IC50 value of 9.8 nM, with much less potency against JAK1 and JAK2 with IC50 values >100nM.

JANEX-1 is a cell-permeable, reversible, potent, ATP-competitive, and specific inhibitor of JAK3 (IC50 = 78 μM) and has no effect on JAK1, JAK2, or Zap/Syk or SRC tyrosine kinases.

Upadacitinib is a selective JAK1 inhibitor with an IC50 of 43 nM.

PF-06826647 is a selective TYK2 inhibitor It is being tested in moderate-to-severe psoriasis in a Phase II clinical trial.

Baricitinib Phosphate can selectively inhibit JAK1/2 inhibitor with IC50 values of 5.9 nM and 5.7 nM.

Potent, selective JAK3 inhibitor

Itacitinib adipate is a selective JAK1 inhibitor which has been tested for efficacy and safety in a phase II trial in myelofibrosis.

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

PF-06651600 is an orally active and selective JAK3 inhibitor with an IC50 of 33.1 nM.

AZD-4205 is a selective JAK1 inhibitor, with an IC50 of 73 nM, weakly inhibits JAK2, and shows little inhibition on JAK3 (IC50, >14.7, >30 μM, respectively).

NS-018 HCl is a highly selective JAK2 inhibitor.

NSC 42834, a specific inhibitor of Jak2, inhibits Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner but was not cytotoxic to cells at concentrations that inhibited kinase activity.

SC99 is a selective inhibitor of JAK2-STAT3 activation.

Ruxolitinib phosphate is a potent and selective JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, > 130-fold selectivity for JAK1/2 versus JAK3.