Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S1155 S3I-201 <1 mg/mL 73 mg/mL <1 mg/mL
S1491 Fludarabine <1 mg/mL 57 mg/mL <1 mg/mL
S7024 Stattic <1 mg/mL 42 mg/mL <1 mg/mL
S3030 Niclosamide <1 mg/mL <1 mg/mL <1 mg/mL
S4182 Nifuroxazide <1 mg/mL 55 mg/mL <1 mg/mL
S8685 AS1517499 <1 mg/mL 79 mg/mL 36 mg/mL
S7337 SH-4-54 <1 mg/mL 100 mg/mL 50 mg/mL
S7977 Napabucasin <1 mg/mL 10 mg/mL <1 mg/mL
S2265 Artesunate <1 mg/mL 77 mg/mL 77 mg/mL
S7769 BP-1-102 <1 mg/mL 100 mg/mL <1 mg/mL
S2285 Cryptotanshinone <1 mg/mL 5 mg/mL 1 mg/mL
S7923 SH5-07 (SH-5-07) <1 mg/mL 100 mg/mL 100 mg/mL
S7951 Ochromycinone (STA-21) <1 mg/mL 21 mg/mL 2 mg/mL
S8561 HJC0152 <1 mg/mL 88 mg/mL <1 mg/mL
S8197 APTSTAT3-9R 98 mg/mL <1 mg/mL <1 mg/mL
S8605 C188-9 <1 mg/mL 94 mg/mL 6 mg/mL
S7501 HO-3867 <1 mg/mL 13 mg/mL 6 mg/mL

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations


S3I-201 shows potent inhibition of STAT3 DNA-binding activity with IC50 of 86 μM in cell-free assays, and low activity towards STAT1 and STAT5.



Fludarabine is a STAT1 activation inhibitor which causes a specific depletion of STAT1 protein (and mRNA) but not of other STATs. Also a DNA synthesis inhibitor in vascular smooth muscle cells.



Stattic, the first nonpeptidic small molecule, potently inhibits STAT3 activation and nuclear translocation with IC50 of 5.1 μM in cell-free assays, highly selectivity over STAT1.



Niclosamide can inhibit DNA replication and inhibit STAT3 with IC50 of 0.7 μM in a cell-free assay. Niclosamide selectively inhibited the phosphorylation of STAT3 and had no obvious inhibition against the activation of other homologues (e.g., STAT1 and STAT5).



Nifuroxazide is a cell-permeable and orally available nitrofuran-based antidiarrheal agent that effectively suppresses the activation of cellular STAT1/3/5 transcription activity with IC50 of 3 μM against IL-6-induced STAT3 activation in U3A cells.



AS1517499 is a novel and potent STAT6 inhibitor with an IC50 value of 21 nM.



SH-4-54 is a potent STAT inhibitor with KD of 300 nM and 464 nM for STAT3 and STAT5, respectively.



Napabucasin is an orally available Stat3 and cancer cell stemness inhibitor.



Artesunate is a part of the artemisinin group of agents with an IC50 of < 5 μM for small cell lung carcinoma cell line H69. It is a potential inhibitor of STAT-3 and exhibits selective cytotoxicity of cancer cells over normal cells in vitro; A potent inhibitor of EXP1.



BP-1-102 is a potent, orally bioavailable and selective STAT3 inhibitor, binds Stat3 with an affinity Kd of 504 nM and blocks Stat3-phospho-tyrosine (pTyr) peptide interactions and Stat3 activation at 4-6.8 μM.



Cryptotanshinone is a STAT3 inhibitor with IC50 of 4.6 μM in a cell-free assay, strongly inhibits phosphorylation of STAT3 Tyr705, with a small effect on STAT3 Ser727, but none against STAT1 nor STAT5.


SH5-07 (SH-5-07)

SH5-07 is a robust hydroxamic acid-based STAT3 inhibitor, which induce antitumor cell effects in vitro and antitumor response in vivo against human glioma and breast cancer models.


Ochromycinone (STA-21)

Ochromycinone (STA-21) is a selective STAT3 inhibitor.



HJC0152 is a signal transducer and activator of transcription 3 (STAT3) inhibitor with remarkably improved aqueous solubility.



APTSTAT3-9R is a specific STAT3-binding peptide with addition of a cell-penetrating motif. The treatment of APTSTAT3-9R in various types of cancer cells blocks STAT3 phosphorylation and reduces expression of STAT targets.



C188-9 is a potent inhibitor of STAT3 that binds to STAT3 with high affinity (KD=4.7±0.4 nM). C188-9 is well tolerated in mice, shows good oral bioavailability, and is concentrated in tumors.



HO-3867, an analog of curcumin, is a selective STAT3 inhibitor that inhibits its phosphorylation, transcription, and DNA binding without affecting the expression of other active STATs.

Tags: STAT inhibition | STAT signaling pathway | STAT pathway | STAT cancer | STAT signaling | STAT protein | STAT activation | JAK-STAT signaling pathway | STAT3 pathway | STAT3 cancer | STAT3 inhibition | STAT3 activation | STAT phosphorylation | STAT3 protein | STAT1 inhibition | STAT1 pathway | STAT1 activation | STAT1 protein | JAK-STAT mechanism | STAT3 inhibitors in clinical trials | STAT3 inhibitor in vivo | STAT inhibitor review