Voderdeucitinib (Compoudn I) is a TYK2 inhibitor with an anti-inflammatory activity. Voderdeucitinib can be used for inflammatory and autoimmune disease research, such as rheumatoid arthritis (RA), multiple sclerosis and intestinal bowel disease (IBD).

Butyzamide (GMP) is Butyzamide) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Butyzamide is an orally active activator of Mpl, a thrombopoietin (TPO) receptor. Butyzamide increases the phosphorylation level of JAK2, STAT3, STAT5 and MAPK. Butyzamide increases the level of platelets in mouse xenotransplantation assay.

WP-1034 is a JAK-STAT inhibitor with proapoptotic and antileukemic activity in acute myeloid leukemia (AML). WP-1034 blocks activation of Stat 3 and 5. WP-1034 induces cell cycle arrest and triggers apoptosis. WP-1034 can be used for AML research.

YZ-35 is a STAT3 inhibitor, with a Ki value of 0.38 μM. YZ-35 binds directly to STAT3 with high affinity, exhibiting a dissociation constant (Kd) of 190 nM. YZ-35 directly attenuates the dual phosphorylation of STAT3 (Tyr705 and Ser727). YZ-35 suppresses colony formation, cellular migration, and induces apoptosis in breast cancer cell lines (BCSC). YZ-35 selectively suppresses BCSC self-renewal. YZ-35 inhibits tumor growth in the BCSC xenograft models. YZ-35 can be used for the study of breast cancer.

(Rac)-TUL01101 (Compound I) is a selective JAK kinase inhibitor. (Rac)-TUL01101 can be used in the research of various diseases such as rheumatoid arthritis, atopic dermatitis, and alopecia areata.

Quecitinib (QY201) is an orally active JAK1/TYK2 dual inhibitor. Quecitinib is also a substrate of cytochrome P450 3A and is mainly metabolized to mono-oxide and glucuronidation products. Quecitinib has favorable pharmacokinetic properties as well as safety. Quecitinib can be used in the research of atopic dermatitis and other autoimmune diseases.

Modzatinib (ITK kinase-IN-1) (compound I) is an inhibitor targeting ITK kinase (IC50=8 nM, Jurkat cells) and can be used to study inflammatory diseases. Modzatinib has an IC50 of 23 nM for JAK3 in hPBMC cells (based on IL-2/pSTAT5 levels), wihout inhibitory effect against JAK2.

Socrodeucitinib (Compound Example 58) is an orally active and selective tyrosine kinase 2 (TYK2) inhibitor with an IC50 value of 1.41 nM. Socrodeucitinib exerts anti-inflammatory activity by inhibiting TYK2-mediated cytokine signaling pathways and reducing the secretion of inflammatory factors. Socrodeucitinib is promising for research of autoimmune diseases such as psoriasis and inflammatory diseases.

DEL1187-126-28-16 is a JAK3 inhibitor with IC50s of 10 and 0.97 nM against JAK3 WT in 0 and 60 min. DEL1187-126-28-16 has no activity at all towards the C909S mutant, JAK1, JAK2, and TYK2. DEL1187-126-28-16 can be used for the study of immune-mediated diseases.

KB-15 is a STAT3 inhibitor. KB-15 exhibits potent anti-proliferative activity against AGS gastric cancer cells (IC50 = 0.29 μM) and BGC-823 gastric cancer cells (IC50 = 0.65 μM). KB-15 exerts anti-tumor effects by inhibiting STAT3 phosphorylation, downregulating HO-1 expression, and promoting intracellular ROS accumulation. KB-15 induces G0/G1 phase cell cycle arrest and apoptosis, as well as suppresses colony formation and migration of gastric cancer cells. KB-15 demonstrates excellent anti-tumor efficacy in BGC-823 subcutaneous xenograft model. KB-15 can be used for the study of gastric cancer.

Soficitinib (Compound 20) is a selective inhibitor targeting tyrosine kinase 2 (TYK2) and Janus kinase 2 (JAK2) with an IC50 values of 0.5 nM and 1.2 nM, respectively. Soficitinib is promising for research of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis) and inflammatory diseases.

DEL1187-126-5-80 is a JAK3 inhibitor with IC50s of 52 and 7.9 nM against JAK3 WT in 0 and 60 min. DEL1187-126-5-80 has no activity at all towards the C909S mutant, JAK1, JAK2, and TYK2. DEL1187-126-5-80 can be used for the study of immune-mediated diseases.

STAT3 inhibitor N4 is a small molecule capable of inhibiting the STAT3 SH2 domain with IC50 of 0.57 uM, SPR KD of 1.04 uM, inhibits STAT3 dimerization and transcription in vitro and suppresses pancreatic cancer in vivo.N4 suppresses STAT3 activation in pancreatic cancer cells, suppresses pancreatic cancer cell growth, migration, and induces apoptosis.N4 (20 mg/kg, i.p.) suppresses pancreatic cancer growth, exhibits potent anti-metastatic activity in a pancreatic cancer liver metastasis mouse model, and prolongs survival of tumor-bearing mice.

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.