Signaling Pathway

STAT

STAT

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STAT is a family of cytoplasmic protein that regulates many aspects of growth, survival and differentiation in cells. The transcription factors of this family are activated by Janus kinase and dysregulation of this pathway is frequently observed in primary tumours and leads to increased angiogenesis, enhanced survival of tumours and immunosuppression. Gene knockout studies have provided evidence that STAT proteins are involved in the development and function of the immune system and play a role in maintaining immune tolerance and tumour surveillance. There are seven mammalian STAT family members that have been identified: STAT1, STAT2, STAT3, STAT4, STAT5 (STAT5A and STAT5B), and STAT6. STAT proteins were originally described as latent cytoplasmic transcription factors that require phosphorylation for nuclear retention. The unphosphorylated STAT proteins shuttle between cytosol and the nucleus waiting for its activation signal. Once the activated transcription factor reaches the nucleus, it binds to consensus DNA-recognition motif called gamma-activated sites (GAS) in the promoter region of cytokine-inducible genes and activates transcription of these genes.

STAT Inhibitors & Modulators (21)

Product Name Catalog No. Brief Description
AG-490

HY-12000

AG-490 (Tyrphostin AG 490) is an inhibitor of EGFR with IC50 of 0.1 μM, 135-fold more selective for EGFR versus ErbB2, also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.

Alantolactone

HY-N0038

Alantolactone(Alant camphor) is a sesquiterpene lactone; has potential activity against triple-negative breast cancer MDA-MB-231 cells by suppressing the signal transducer and activator of transcription 3 (STAT3) signaling pathway.

AS1517499

HY-100614

AS1517499 is a potent STAT6 inhibitor with IC50 of 21 nM.

BP-1-102

HY-100493

BP-1-102 is an orally available, small-molecule inhibitor of transcription factor Stat3.

Corylifol A

HY-N0897

Corylifol A is a phenolic compounds isolated from Psoralea corylifolia; inhibits IL-6-induced STAT3 activation and phosphorylation(IC50=0.8 uM).

Cryptotanshinone

HY-N0174

Cryptotanshinone(Tanshinone c) is a potent STAT3 inhibitor(IC50 =4.6 uM); inhibited STAT3 Tyr705 phosphorylation in DU145 prostate cancer cells.

Cucurbitacin I

HY-N1405

Cucurbitacin I is a naturally occurring triterpenoid derived from Cucurbitaceae family plants that exhibits a number of potentially useful pharmacological and biological activities.

HO-3867

HY-100453

HO-3867 a selective and potent inhibit STAT3 phosphorylation, transcription, and DNA binding without affecting the expression of other active STATs.

Homoharringtonine

HY-14944

Homoharringtonine(HHT) is a cytotoxic alkaloid from the evergreen tree.

Leflunomide

HY-B0083

Leflunomide(SU101; HWA486; RS-34821) is a disease-modifying antirheumatic drug, which is a pyrimidine synthesis inhibitor.

Mogrol

HY-N2312

Mogrol is a biometabolite of mogrosides, and acts via inhibition of the ERK1/2 and STAT3 pathways, or reducing CREB activation and activating AMPK signaling.

Napabucasin

HY-13919

Napabucasin is an orally-administered small molecule which can block cancer stem cell (CSC) self-renewal and induces cell death in CSCs as well as non-stem cancer cells.

Niclosamide

HY-B0497

Niclosamide(BAY2353) is used for the treatment of most tapeworm infections by inhibiting DNA replication.

Nifuroxazide

HY-B1436

Nifuroxazide is an inhibitor of STAT activation and signaling activity, is an oral nitrofuran antibiotic, used to treat colitis and diarrhea in humans and non-humans.

NSC 74859

HY-15146

NSC 74859(S3I-201) shows potent inhibition of STAT3 DNA-binding activity with IC50 of 86 μM, and low activity towards STAT1 and STAT5.

Oleanolic Acid

HY-N0156

Oleanolic acid (Caryophyllin) is a natural compound from plants with anti-tumor activities.

Scutellarin

HY-N0751

Scutellarin, an active flavone isolated from Scutellaria baicalensis, can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts.

SH-4-54

HY-16975

SH-4-54 is a most potent, small molecule, nonphosphorylated STAT3 inhibitor, strongly binds to STAT3 protein (KD = 300 nM), is selective for STAT3 over STAT1.

Stattic

HY-13818

Stattic is a potent inhibitor of STAT3, used for cancer treatment.

Teriflunomide

HY-15405

Teriflunomide (A77 1726), the active metabolite of an approved antirheumatic drug Leflunomide, is an emerging oral therapy for multiple sclerosis (MS).