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. 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.
Cat. No. | Product Name | CAS No. | Information |
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H9252 |
SC-43 |
1400989-25-4 | SC-43 is a Sorafenib derivative, is a potent and orally active SHP-1 (PTPN6) agonist; SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis. SC-43 has anti-fibrotic and anticancer effects. |
H9251 |
Angoline hydrochloride |
1071676-04-4 | Angoline hydrochloride is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM; Angoline hydrochloride inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation. |
H9250 |
Angoline |
21080-31-9 | Angoline is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM; Angoline inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation. |
H9212 |
W2014-R |
2473028-69-0 | W2014-R is a novel STAT3 inhibitor,While surface plasmon resonance (SPR) analysis suggested that W2014-R may have similar affinities with STAT3 protein. W2014-R bind to wild-type STAT3, with KD of 3.39 μM respectively. |
H9211 |
W2014-S |
2473028-71-4 | W2014-S is a novel STAT3 inhibitor,While surface plasmon resonance (SPR) analysis suggested that W2014-S may have similar affinities with STAT3 protein. W2014-S bind to wild-type STAT3, with KD of 3.64 μM respectively;W2014-S regresses human non-small cell lung cancer xenografts and sensitizes EGFR-TKI acquired resistance.W2014-S showed stronger inhibition than W2014-R on cell proliferation and colony survival, especially in A549 cell line. |
H9163 |
Stafia-1 |
Stafia-1 is a potent STAT5a inhibitor (Ki=10.9 μM, IC50=22.2 μM). Stafia-1 displays high selectivity over STAT5b and other STAT family members. |
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H4277 |
XZH-5 |
1360562-98-6 | XZH-5 is a small moelcule that inhibits constitutive and interleukin-6-induced STAT3 phosphorylation, inhibits STAT3 DNA binding ability and downregulation of STAT3 downstream genes; inhibits downregulation of STAT3 downstream genes, such as Bcl-2, Bcl-xL, Cyclin D1 and Survivin, demonstrates blockade of STAT3 phosphorylation in human rhabdomyosarcoma cells with apoptosis and suppresses colony-forming ability and cell migration; blocks IL-6-induced STAT3 phosphorylation and nuclear translocation but not the stimulation of STAT1 phosphorylation by IFN-γ. |
H4276 |
UC-514321 |
299420-83-0 | UC-514321 is a more effective analog of NSC-370284 that directly binds to STAT3/5, significantly and selectively suppresses the viability of AML cells with high level of TET1 expression both in vitro and in vivo; shows no inhibitory effect on the viability of TET1-low AML (i.e., NB4) cells, function as TET1-transcription inhibitor in TET1-high AMLs and the anti-leukemic effects are TET1-dependent. |
H4275 |
STAT5b inhibitor 7 |
1818390-58-7 |
STAT5b inhibitor 7 (Capstafin prodrug) is the pivaloyloxymethyl ester prodrug of Capstafin, which is a potent, selective STAT5b inhibitor with Ki of 0.34 uM; inhibits STAT5b with selectivity over STAT5a in human tumor cells, inhibits cell viability and induces apoptosis in human tumor cells in a STAT5-dependent manner. |
H4274 |
STAT5-IN-1 |
285986-31-4 | A selective, small molecule inhibitor of the transcription factor STAT5 with IC50 of 47¡À17 uM in FP assays; shows little to no inhibition for STAT1, STAT3 and Lck ( |
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