2816059-41-1

2816059-41-1 structure

Name: STAT3-SH2 domain inhibitor 1
Chemical Name: STAT3-SH2 domain inhibitor 1
CAS Number: 2816059-41-1
Molecular Formula: C₂₈H₂₈BF₅N₂O₅S
Molecular Weight: 610.40
Catalog: Signaling Pathways Apoptosis Apoptosis
Create Date: 2022-11-06 11:44:21
Modify Date: 2024-01-09 20:31:02
STAT3-SH2 domain inhibitor 1 is a potent Src Homology 2 (SH2) Domain of STAT3 (STAT3-SH2 domain) inhibitor with a Kd value of 1.57 μM. STAT3-SH2 domain inhibitor 1 inhibits STAT3 signaling transduction and transcriptional activation. STAT3-SH2 domain inhibitor 1 induces apoptosis in gastric cancer cells. STAT3-SH2 domain inhibitor 1 can be used in research of cancer[1].

Name	STAT3-SH2 domain inhibitor 1

Description	STAT3-SH2 domain inhibitor 1 is a potent Src Homology 2 (SH2) Domain of STAT3 (STAT3-SH2 domain) inhibitor with a Kd value of 1.57 μM. STAT3-SH2 domain inhibitor 1 inhibits STAT3 signaling transduction and transcriptional activation. STAT3-SH2 domain inhibitor 1 induces apoptosis in gastric cancer cells. STAT3-SH2 domain inhibitor 1 can be used in research of cancer[1].
Related Catalog	Signaling Pathways >> Stem Cell/Wnt >> STAT Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer Signaling Pathways >> JAK/STAT Signaling >> STAT
In Vitro	STAT3-SH2 domain inhibitor 1 (compound 7; 1-5 μM; 24 h; AGS and MGC-803 cell lines) strongly and selectively inhibits the STAT3 signaling pathway[1]. STAT3-SH2 domain inhibitor 1 (0-10 μM; 72 h) has antiproliferative activity with IC50 values of 1.54 and 4.73 μM for AGS and MGC-803 cells, respectively[1]. STAT3-SH2 domain inhibitor 1 (1 and 3 μM; 72 h; AGS and MGC-803 cell lines) induces apoptosis effects in gastric cancer cells[1]. Cell Viability Assay[1] Cell Line: AGS and MGC-803 cell lines Concentration: 0-10 μM Incubation Time: 72 hours Result: Suppressed cancer cell proliferation and growth. Apoptosis Analysis[1] Cell Line: AGS and MGC-803 cell lines Concentration: 1 and 3 μM Incubation Time: 72 hours Result: Induced apoptosis in AGS cells in a concentration-dependent manner, resulting in apoptotic percentages of 13.0 and 26.7% at 1 and 3 μM, respectively. Induced apoptosis of MGC-803 cells in a dose-dependent way, leading to apoptotic percentage of 11.2% at 5 μM. Western Blot Analysis[1] Cell Line: AGS and MGC-803 cell lines Concentration: 1 and 3 μM Incubation Time: 24 hours Result: Inhibited STAT3 phosphorylation at Tyr705 in a dose-dependent manner. Western Blot Analysis[1] Cell Line: HEK-293T cells Concentration: 1, 3, and 5 μM Incubation Time: 24 hours Result: Disrupted STAT3 dimerization in HEK-293T cells.
In Vivo	STAT3-SH2 domain inhibitor 1 (compound 7; 5 and 15 mg/kg; i.p.; daily, for 20 d) exhibits superior antitumor activity in BALB/c male nude mice with gastric tumor xenografts[1]. Animal Model: BALB/c male nude mice with gastric tumor xenografts[1] Dosage: 5 and 15 mg/kg Administration: Intraperitoneal injection; daily, for 20 days Result: Suppressed tumor growth in a dose-dependent manner, with tumor growth inhibition (TGI) of65.14% at 5 mg/kg and 79.13% at 15 mg/kg, respectively.
References	[1]. Deng L, et, al. Boronic Acid: A Novel Pharmacophore Targeting Src Homology 2 (SH2) Domain of STAT3. J Med Chem. 2022 Oct 13;65(19):13094-13111.

Molecular Formula	C₂₈H₂₈BF₅N₂O₅S
Molecular Weight	610.40

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