QL-1200186 is a potent, highly selective allosteric inhibitor of tyrosine kinase 2 (TYK2) with IC50 of 0.06 nM, targets pseudokinase regulatory domain (Janus homology 2, JH2) of the TYK2 protein.

MMT3-72 is a gastrointestinal locally-activating Janus kinase (JAK) inhibitor, readily converted to MMT3-72-M2 in the colon contents (JAK1 IC50=10.8 nM, JAK2 IC50=26.3 nM and TYK2 IC50=91.6 nM).

CPL409116 (CPL 409116) is a potent, competitive, dual JAK and ROCK inhibitor with IC50 of 0.95/5.36//0.87/110.6/106.7 nM for JAK1/JAK2/JAK3/ROCK1/ROCK2, respectively.

AZD0449 (AZD-0449) is a potent and highly selective JAK1 inhibitor with IC50 of 2.4 nM, displays >50-fold selectivity over TYK2 and JAK2, and no inhibition against JAK3.

ABT-317 (ABT317) is a potent, selective JAK1 inhibitor, inhibits IL-6-stimulated pSTAT3 (TF-1 cells, IC50=16 nM) and IL-2-stimulated pSTAT5 (T-blasts, IC50=30 nM).

ABBV-712 is a potent, selective inhibitor of tyrosine kinase 2 (TYK2) with EC50 of 0.01 uM, binds and stabilizes the pseudokinase (JH2) domain of TYK2.

AZD1208 is orally available, small molecule inhibitor of PIM kinases with potential antineoplastic activity.

BTZ043 is a inhibitor of decaprenyl-phosphoribose-epimerase (DprE1), It can display nanomolar bactericidal activity against Mycobacterium tuberculosis in vitro.

Colivelin is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin has the potential for the treatment of alzheimer's disease and ischemic brain injury

Fosifidancitinib is a potent and selective inhibitor of JAK kinases 1/3. Fociatinib is used in studies of allergies, asthma and autoimmune diseases.

VVD-118313 (compound 5a) is a potent, selective JAK1 inhibitor. VVD-118313 targets an isoform-restricted allosteric cysteine to block JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer.

FLLK31 is a potent and selective inhibitor of the STAT3 signaling pathway.

Delgocitinib (JTE-052, LEO 124249) is a potent, selective, orally active, pan-JAK inhibitor with IC50 of 2.8, 2.6, 13 and 58 nM for JAK1,2,3 and Tyk2, respectively.

NDI034858 is a TYK2 inhibitor, target TYK2 JH2 domain with binding constant Kd of <200 pM.

BMS-986202 (BMS 986202) is potent, selective Tyk2 inhibitor that binds to Tyk2 JH2 domain with IC50 of 0.19 nM, Ki of 0.02 nM, >10,000-fold over 273 kinases and pseudokinases; BMS-986202 demonstrated cellular activity (IL-23 IC50=12 nM) in IL-23 stimulated reporter assay (in Kit225 T cells). BMS-986202 also binds Jak1 JH2 with an IC50 of 7.8 nM, but this enzymatic binding did not lead to any functional activities, as BMS-986202 displayed an activity (IC50) of greater than 12.5 μM in the IL-2 stimulated Jak1/3-dependent cellular assay. BMS-986202 showed in vivo efficacy in mouse models of IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus.

YLT-11 is a novel and specific PLK4 inhibitor with IC50 of 22 nM and Kd of 5.2 nM.

Nimucitinib is a Janus kinase (JAK) inhibitor.

Pumecitinib is a Janus kinase (JAK) inhibitor with anti-inflammatory activity.

Z3(NSC 42834), a novel 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.

XL019 is an orally bioavailable inhibitor of Janus-associated kinase 2 (JAK2) with potential antineoplastic activity.

WHI-P258 is a negative control for JAK3 inhibitors.

WHI-P154 is a potent JAK3 inhibitor with IC50 of 1.8 μM, no activity against JAK1 or JAK2, also inhibits EGFR, Src, Abl, VEGFR and MAPK, prevents Stat3, but not Stat5 phosphorylation.

Upadacitinib (ABT-494) is a potent and selective Janus kinase (JAK) 1 inhibitor being developed for the treatment of several autoimmune disorders with an IC50 of 43 nM.

Tofacitinib is a novel inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent versus JAK2 and JAK1. Phase 3.

Tofacitinib is a novel inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent versus JAK2 and JAK1. Phase 3.

TG-101348 (SAR302503) is a selective inhibitor of JAK2 with IC50 of 3 nM, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3, TG-101348 also inhibit BRD4 with IC50 of 340 nM.

TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM, ~30-fold selective for JAK2 than JAK3, sensitive to JAK2V617F and MPLW515L/K mutations; TG101209 inhibit BRD4 activity with IC50 of 130 nM.

TCS PIM-1 1 is a potent and selective ATP-competitive Pim-1 kianse inhibitor with IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2(IC50s >20,000 nM).

S-Ruxolitinib is the chirality of INCB018424, which is the first potent, 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. Phase 3.

Stat5 Inhibitor is a cell permeable nonpetidic nicotinoyl hydrazone which suppresses Stat5 via binding to the SH2 domain.