Decernotinib(VX-509; VRT-831509) is a potent and selective Janus kinase 3 (JAK3) inhibitor with Ki of 2.5 nM; IC50 is 50-170 nM in cellular assays.

WR-S-462 is a STAT3 inhibitor. WR-S-462 effectively suppresses STAT3 phosphorylation and biological functions in vitro. WR-S-462 inhibits MDA-MB-231 cells with an IC50 of 0.03 μM. WR-S-462 displays a strong binding affinity towards the STAT3 protein with a Kd of 58 nM. WR-S-462 inhibits the nuclear translocation of p-STAT3, selectively inhibits the expression of p-STAT3Tyr705 and downstream target genes regulated by STAT3 in MDA-MB-231 cells such as Cyclin D1, Bcl-2, and Bcl-xl. WR-S-462 inhibits TNBC (triple-negative breast cancer) growth and metastasis.

NW16 is an orally active inhibitor for STAT3 with Kd of 11.0 μM. NW16 arrests the cell cycle at S phase, induces apoptosis in HCT116, and inhibits the proliferation of cancer cell HCT116, A549, and B16 with IC50s of 0.28, 1.22, and 9.86 μM, respectively. NW16 induces the production of ROS, inhibits the PI3K/AKT signaling pathway, and thus exhibits antitumor efficacy in mouse model.

VB1080 (compound 12) is a potent PIM inhibitor with IC50 values of 69.5, 4996, 9.88 µM for PIM1, PIM2, PIM3, respectively. VB1080 shows cytotoxicity. VB1080 shows anthelmintic activity.

Golidocitinib 1-hydroxy-2-naphthoate is a derivative of Golidocitinib, an oral, potent, selective inhibitor of Janus kinase 1 (JAK1) with an IC50 of 70 nM. It exhibits enhnaced antitumor activity and can be used for the treatment of cancer, including peripheral T cell lymphoma (PTCL).

(3R,4S)-Tofacitinib is a less active enantiomer of Tofacitinib and a first-in-class inhibitor of JAK3 with an IC50 of 1 nM. It is highly efficacious in treating rheumatoid arthritis (RA).

Milpecitinib (Compound 21a) is a potent, selective Janus tyrosine kinase (JAK) inhibitor with anti-inflammatory activity. Milpecitinib is promising for research of cancers and inflammatory disorders.

LNK01004 is a JAK inhibitor with strong inhibitory effects on JAK1 (IC50: 10 nM), JAK2 (IC50:＜0.51 nM) and TYK2 (IC50: 1.0 nM) . LNK01004 can simultaneously inhibit multiple cytokine-induced p-STAT signaling pathways. LNK01004 can be used in the research of diseases such as atopic dermatitis.

lirucitinib is a JAK inhibitor, and has antiinflammatory activity

JNN-5 is a potent and selective JAK2 inhibitor with an IC50 of 0.41 nM. JNN-5 shows strong antiproliferative activities in the TNBC cell lines (MDA-MB-468, MDA-MB-213, HCC70, MDA-MB-157).

iBFAR2, a BFAR inhibitor, restores the CD8+ TRM cell subset against solid tumors. iBFAR2 promotes JAK2-STAT1 association and STAT1 phosphorylation.

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. STAT3-SH2 domain inhibitor 1 inhibits STAT3 signaling transduction and transcriptional activation. STAT3-SH2 domain inhibitor 1 induces apoptosis in gastric cancer cells. STAT3-SH2 domain inhibitor 1 can be used in research of cancer.

Lepzacitinib is a Janus kinase inhibitor targeting to JAK 1/3. Lepzacitinib exhibits anti-inflammatory effect and inhibits atopic dermatitis and other skin diseases.

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.