AZD4604 (AZD-4604) is a potent, selective Janus-associated kinase 1 (JAK1) inhibitor with anti-inflammatory effect.

PIM1-IN-2 is a highly effective and ATP-competitive inhibitor of Pim-1, demonstrating a Ki value of 91 nM. Unlike traditional inhibitors, it interacts with the ATP-binding kinase hinge region without relying on the formation of standard hydrogen bonds, showcasing a unique mechanism of action. This distinctive approach highlights its potential as a promising therapeutic agent.

Ilunocitinib (compound 27) is a JAK inhibitor (extracted from patent WO2009114512A1).

JAK1-IN-8, a potent JAK1 inhibitor (IC50<500 nM), compound 28, extracted from patent WO2016119700A1.

JAK-IN-14 is a potent and selective JAK1 inhibitor, with an IC50 of <5 μM. JAK-IN-14 is >8-fold more selective for JAK1 than JAK2 and JAK3 (Patent WO2016119700A1, compound 16).

PIM/AKK1-IN-1 is a potent multi-kinase inhibitor with Kd values of 35 nM/53 nM/75 nM/380 nM for Pim1/AKK1/MST2/LKB1 respectively; also inhibits MPSK1 and TNIK.

Filgotinib (GLPG0634) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib can effectively inhibit the activities of JAK1, JAK2, JAK3 and TYK2 with IC50 values of 10 nM, 28 nM, 810 nM and 116 nM, respectively. Filgotinib also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib can be used in the study of rheumatoid arthritis and inflammatory bowel disease.

Piperlongumine induces cell death and increases the level of reactive oxygen species (ROS) in cancer cells with both wild-type and normal p53.

Peficitinib(ASP015K,JNJ-54781532) is a novel potent JAK inhibitor, which demonstrated potent efficacy in adjuvant-induced arthritis model in rats.

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

AZ 960 is a novel ATP competitive JAK2 inhibitor with IC50 and Ki of <3 nM and 0.45 nM, 3-fold selectivity of AZ960 for JAK2 over JAK3.

(1S,3R,5R)-PIM447 (dihydrochloride) an PIM inhibitor extracted from patent US 20100056576 A1, compound example 72, has IC50 values of 0.095 μM for Pim1, 0.522 μM for Pim2 and 0.369 μM for Pim3.

CMD178 is a lead peptide that consistently reduced the expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα signaling. CMD178 also is an inhibitor of STAT5 and inhibit Treg cell development.

JP-11646 is a novel potent, selective, non-ATP competitive Pim2 inhibitor with IC50 of 0.5/1/24 nM for Pim2/3/1, respectively; shows less potency for other kinases in a kinase selectivity panel; exhibits 4-760-fold greater suppression of MM proliferation and viability than ATP-competitive PIM inhibitors; significant reduces tumor burden and increases median survival in xenogeneic myeloma murine models.

TD-1473 (Izencitinib, TD1473, JNJ 8398) is a potent, selective, oral gut-selective pan-JAK inhibitor with pKi of 10.0/10.0/8.8/9.5 for human recombinant JAK1, JAK2, JAK3 and TYK2.TD-1473 inhibited cytokine-induced phosphorylation of STAT1 in mouse primary colonic epithelial cells with pIC50 values for inhibition against IL-6, IFNα and IFNγ were 7.3, 6.8 and 7.0.TD-1473 demonstrated JAK inhibitory activity in ex vivo mouse colon and human IBD patient colonic tissue. TD-1473 (Izencitinib) is under development for the treatment of ulcerative colitis.

CEP33779(< 3 μM) inhibits phosphorylation of downstream target signal transducer and activator of transcription 5(pSTAT5) of JAK2 in a concentration dependent manner in HEL92 cells.

AS 602801(Bentamapimod) is a novel, orally active inhibitor of JNK.

WZ-2-033 is a potent, selective STAT3 inhibitor, binds to the SH2 domain of the STAT3 protein with KD of 7.4 uM, disrupts STAT3 dimerization and significantly inhibits STAT3 signaling.

WB737 is a potent and selective STAT3 inhibitor, directly binds to the STAT3 Src homology 2 (SH2) domain with KD value of 1.34 nM.

WB436B is a potent and highly selective small molecule inhibitor of STAT3, specifically targets the STAT3-SH2 domain with KD value of 94.3 nM.

W2014-S is a small molecule STAT3 inhibitor with binding Kd of 3.64 uM, disrupts STAT3 dimerization and selectively inhibits STAT3 signaling.

W1131 is a potent and selective STAT3 inhibitor with Kd of 7.55 uM in surface plasmon resonance (SPR) assays, inhibits STAT3 Tyr705 phosphorylation, triggers ferroptosis and possesses potent anti-tumor effects both in vitro and in vivo.

W1046 is a potent and selective STAT3 inhibitor, decreases the expression of VISTA at mRNA and protein level and inhibits proliferation and survival in AML cells.

TR120 (TR-120) is a potent small molecule STAT5 inhibitor, exhibits antiproliferative in K562 cells with IC50 of 0.12 uM, decreases STAT5 expression in imatinib-sensitive and imatinib-resistant BCR-ABL-expressing leukemia cells.

SF-1-088 is a small molecule STAT5-SH2 domain inhibitor with Ki of 8.3 uM (Stat5b), shows no affinity for Stat1 and Stat3 (Ki>25 uM).

ODZ10117 is a small molecule inhibitor of STAT3, effectively inhibits the level of tyrosine phosphorylated STAT3 in various cancer cell lines.

MNS1-MV is a novel pyrazole-based small molecular inhibitor of STAT3 pathway, potently inhibit IL-6-induced STAT3 phosphorylation at 10 μM in dBT114 cells.

MNS1-Leu is a novel pyrazole-based small molecular inhibitor of STAT3 pathway, potently inhibit IL-6-induced STAT3 phosphorylation at 10 μM in dBT114 cells.

MC0704 (MC-0704) is a novel synthetic STAT3 pathway inhibitor, exhibits potential antitumor activity in vitro and in vivo models in docetaxel-resistant TNBC cells.

LLL12B is a selective STAT3 inhibitor that suppresses Th17 development, specifically inhibits STAT3 and suppresses Th17 differentiation and expansion.