stat1

JAK-STAT-IN-1 is a specific JAK-STAT inhibitor indicated for the study of autoimmune diseases.

Nifuroxazide (Diarlidan) is an orally available and cell-permeable nitrofuran-based antidiarrheal agent. It has the inhibitory effect against the activation of cellular STAT1/3/5 transcription.

3-Hydroxykynurenamine, also known as 3-Hydroxy-L-kynurenamine or 3-HKA, is a biogenic amine produced via an alternative pathway of tryptophan metabolism. In vitro, 3-HKA has an anti-inflammatory profile by inhibiting the IFN-γ mediated STAT1/NF-κΒ pathway in both mouse and human dendritic cells (DCs) with a consequent decrease in the release of pro-inflammatory chemokines and cytokines, most notably TNF, IL-6, and IL12p70. 3-HKA has protective effects in an experimental mouse model of psoriasis by decreasing skin thickness, erythema, scaling and fissuring, reducing TNF, IL-1β, IFN-γ, and IL-17 production, and inhibiting generation of effector CD8+ T cells. Similarly, in a mouse model of nephrotoxic nephritis, besides reducing inflammatory cytokines, 3-HKA improves proteinuria and serum urea nitrogen, overall ameliorating immune-mediated glomerulonephritis and renal dysfunction.This compound is unstable in powder form and other related salt forms are recommended.

Fludarabine (Fludarabinum) is a fluorinated purine analog, an inhibitor of nucleic acid synthesis and an inhibitor of STAT1 activation. Fludarabine has antitumor activity and can be used for the treatment of leukemia and lymphoma.

S3I-201 (S3I-201) is a selective Stat3 inhibitor (IC50: 86±33 μM) and low effect towards STAT1 5.

Ethyl Caffeate (ETHYL 3,4-DIHYDROXYCINNAMATE) suppressed the differentiation of naive CD4+ T cells into Th1 in vitro. Furthermore, Ethyl Caffeate intensely blocked the transcriptional expression in interferon-γ-related signaling, including IFN-γ, T-bet, STAT1, and STAT4.

Cryptotanshinone (Cryptotanshinon), a STAT3 inhibitor (IC50: 4.6 μM) in a cell-free assay, strongly inhibits phosphorylation of STAT3 Tyr705, with a little effect on STAT3 Ser727, but no inhibition for STAT1 nor STAT5.

2-NP is a STAT1 enhancer.

Abrocitinib (PF-04965842) (PF-04965842) is a potent, specific and orally-active JAK1 inhibitor (IC50s: 29/803 nM for JAK1/2).

CAY10763 is a dual inhibitor of indolamine 2,3-dioxygenase 1 (IDO1; IC50= 46 nM) and STAT3 activation.1It binds to STAT3 (Kd= 530 nM) and selectively reduces the levels of STAT3 phosphorylated at the tyrosine in position 705 (STAT3Y705) over phosphorylated STAT3S727, STAT1, and STAT5 in SKOV3 cells when used at a concentration of 500 nM. It also inhibits STAT3 nuclear translocation in SKOV3 cells. CAY10763 is cytotoxic to HCT116, SKOV3, A549, and HepG2 cancer cells (IC50s = 37, 28, 33, and 12 nM, respectively). It reduces tumor growth in B16/F10 mouse melanoma and HepG2 mouse xenograft models when administered at doses of 100 and 10 mg/kg, respectively. 1.Huang, R., Jing, X., Huang, X., et al.Bifunctional naphthoquinone aromatic amide-oxime derivatives exert combined immunotherapeutic and antitumor effects through simultaneous targeting of indoleamine-2,3-dioxygenase and signal transducer and activator of transcription 3J. Med. Chem.63(4)1544-1563(2020)

C188 is a cell-permeable naphthol compound and a STAT3 inhibitor. C188 inhibits IL-6-stimulated STAT3 Tyr705 phosphorylation and nuclear translocation in HepG2 cells by targeting STAT3 SH2 domain peptide-binding pocket, while exhibiting little effect agai

6'-Sialyllactose Sodium Salt (6'-N-Acetylneuraminyl-D-lactose sodium salt), an oligosaccharide present in breast milk, is protective against LPS-induced ALI and attenuates LPS-induced lung injury by inhibiting the STAT1 and NF-κB signaling pathways. Diquat dibromide

LL-K8-22 is a potent, selective, and durable dual degrader of CDK8-cyclin C, demonstrating DC50 values of 2.52 and 2.64 μM, respectively. This compound effectively suppresses STAT1 Ser 727 phosphorylation and inhibits carcinogenic transcriptional programs driven by E2F and MYC. LL-K8-22 is specifically utilized in research for triple-negative breast cancer (TNBC) [1].

5,15-Diphenylporphyrin (5,15-DPP) is a selective STAT3-SH2 antagonist with IC50 values of 0.28 μM for STAT3 and 10 μM for STAT1 [1].

CDK8-IN-13 is a CDK8 inhibitor (IC50: 51.9 nM) with potent, selective and oral activity. CDK8-IN-13 induces apoptosis and reduces the expression of p-STAT1 S727 and p-STAT5 S726. CDK8-IN-13 exhibits anti-tumour activity.

BRD0476 is a suppressor of pancreatic β-cell apoptosis. BRD0476 inhibits interferon-gamma (IFN-γ)-induced Janus kinase 2 (JAK2) and signal transducer and activation of transcription 1 (STAT1) signaling to promote β-cell survival. BRD0476 inhibits JAK-STAT

Poloxipan is a potent and pan-specific PLK1 inhibitor. In vitro, Poloxipan has IC50 3.2 uM (Plk1); 1.7 uM (Plk2); and 3 uM (Plk3). Poloxipan showed minor inhibition over FHA dommain of Chk2, S2 domian of STAT1, STAT5b, Lck, etc.

Sophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects.

Interferon alfa, a type I interferon, activates new genes, displaying strong antiviral and antiproliferative effects on target cells. It signals through receptor-mediated activation of Stat1 and Stat2, which heterodimerize into a STAT complex binding with the DNA-binding protein IRF-9 (p48) to form ISGF-3 (IFN-stimulated gene factor 3). This complex further activates driver genes to fulfill its antiviral role [1].

Jaceosidin has anti-oxidative activity. Jaceosidin has anti-inflammatory activity, also a microglial inhibitor with anti-neuroinflammation activity. aceosidin has anticancer activity, modulates the ERK/ATM/Chk1/2 pathway, leading to inactivation of the Cd

ML115 is a potent and selective activator of transcription 3 (STAT3), with abn EC50 of 2.0 nM, and is inactive against the related STAT1 and NFκB anti-targets.

Caerulomycin A (Caerulomycin) (Cerulomycin; Caerulomycin) is an antifungal compound. Which induces generation of T cells, enhances TGF-β-Smad3 protein signaling via suppressing interferon-γ-induced STAT1 signaling. Antifungal and antibiotic activity, and used in autoimmune diseases.

Lupinalbin A as the most potent estrogen receptor α- and aryl hydrocarbon receptor agonist in Eriosema laurentii de Wild. (Leguminosae). It exerts anti-inflammatory effects via the inhibition of pro-inflammatory cytokines and blocking of IFN-β/STAT1 pathw

STAT3-IN-9, a potent inhibitor of STAT3 activation at Tyr705, exhibits no impact on the phosphorylation of STAT1 at Tyr 701. Additionally, this compound efficiently induces apoptosis and cell cycle arrest specifically at the G2 M phase [1].

Erasin, a formidable antagonist to Erlotinib resistance, selectively inhibits STAT3 with an IC50 of 9.7 μM, and STAT1 with an IC50 of 24 μM. It effectively induces apoptosis in cancer cells [1].