InS3-54A18

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

InS3-54A18 是 inS3-54 的活性类似物，靶向 STAT3 的 DBD，在 STAT3 依赖性荧光素酶报告基因测定中，IC50 为 8.8 uM。

InS3-54A18 is an active analog of inS3-54 targeting the DBD of STAT3 with IC50 of 8.8 uM in STAT3-dependent luciferase reporter assay, with increased specificity and pharmacological properties; not only binds directly to the DBD and inhibits the DNA-binding activity of STAT3 both in vitro and in situ but also effectively inhibits the constitutive and IL-6-stimulated expression of STAT3 downstream target genes; InS3-54A18 is completely soluble in an oral formulation and effectively inhibits lung xenograft tumor growth and metastasis with little adverse effect on animals.

inS3-54A18 (5?μM) reduces wound healing to 64% and 76% for A549 and MDA-MB-231 cells, respectively. inS3-54A18 at 10?μM further reduces the healing to 47% and 39%, respectively. inS3-54A18 inhibits the expression of STAT3 downstream target genes and the binding of STAT3 to its endogenous target sequences. inS3-54A18 does not affect the constitutive or IL-6-induced STAT3 activation (Tyr705 phosphorylation) but represses STAT3 target gene (survivin) expression.

inS3-54A18 (200?mg/kg, p.o.) inhibits tumor growth, metastasis and expression of STAT3 target genes in a mouse xenograft model of A549 cells.

inS3-54-A18 | inS3-54A18 | inS3-54 A18 | inS354-A18

JAK/STAT Signaling

STAT

STAT

Cancer

——

328998-53-4

373.836

C23H16ClNO2

>98% (HPLC)

DMSO : ≥ 150 mg/mL 401.25 mM

O=C1N(C2=CC=C(O)C=C2)C(C3=CC=CC=C3)=C/C1=C/C4=CC=C(Cl)C=C4

3-(4-chlorobenzylidene)-1-(4-hydroxyphenyl)-5-phenyl-1,3-dihydro-2H-pyrrol-2-one

(-20℃)

With Ice Pack

≥ 2 years