K-7174

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

转录因子 GATA 结合蛋白 2 (GATA2) 的选择性小分子抑制剂。

A selctive small molecule inhibitor of the transcription factor GATA-binding protein 2 (GATA2); suppresses the expression of AR, including ARVs, in 22Rv1 cells, exertes potent anticancer activity against GATA2+/AR+ PC cell lines in vitro; induces transcriptional repression of class I histone deacetylases (HDAC1, -2, and -3) via caspase-8-dependent degradation of Sp1; significantly decreases HAMP expression, also upregulates CEBPB.

K-7174 (10 μM; 1 h) inhibits the adhesion by VCAM-1 and its ligand.K-7174 (1-30 μM; 1 h) dose-dependently suppresses the VCAM-1 expression with an IC50 value of 14 μM.K-7174 (1-30 μM; 1 h) dose-dependently suppresses the induction of VCAM-1 mRNA by TNFα with an IC50 value of 9 μM.K-7174 (10-20 μM; 24 h) dose-dependently rescues Epo production by Hep3B cells.K-7174 (2.5-30 μM; 24 h) inhibits the binding activity of GATA.K-7174 (0-25 μM; 72 h) inhibits MM cells growth and induces cell apoptosis.Cell Viability Assay Cell Line:KMS12-BM, U266, and RPMI8226 cell lines Concentration:0-25 μM Incubation Time:72 h Result:Inhibited MM cells growth.Apoptosis Analysis Cell Line:KMS12-BM, U266, and RPMI8226 cell lines Concentration:10 μM Incubation Time:48 h Result:Significantly increased apoptosis of MM cells with the increasing percentage of annexin-V-positive cells.

K-7174 (30 mg/kg; i.p. once daily for 9 days) reverses the decreasing of hemoglobin concentrations and reticulocyte counts by IL-1β or TNF-α.K-7174 (75 mg/kg; i.p. once daily for 14 days) inhibits the tumor growth in vivo.K-7174 (50 mg/kg; p.o. once daily for 14 days) inhibits the tumor growth in vivo and shows a better effect than intraperitoneal injection. Animal Model:ICR mice with IL-β or TNF-α injection Dosage:30 mg/kg Administration:Intraperitoneal injection; 30 mg/kg once daily for 9 days Result:Increased erythropoietin (Epo) production, reticulocyte counts, and hemoglobin (Hb) concentrations Animal Model:NOD/SCID mice with murine xenograft Dosage:75 mg/kg Administration:Intraperitoneal injection; once daily for 14 days Result:Significantly decreased tumor volume, but showed a significant body weight reduction after 10 days. Animal Model:NOD/SCID mice with murine xenograft Dosage:50 mg/kg Administration:Oral gavage; once daily for 14 days Result:Showed an anti-myeloma activity. Proved oral administration is more effective than intraperitoneal injection.

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Nuclear Receptor/Transcription Factor

GATA Binding Protein

GATA Binding Protein

Inflammation/Immunology

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191089-59-5

568.744

C33H48N2O6

>98% (HPLC)

10 mM in DMSO

COC1=CC(=CC(=C1OC)OC)C=CCCCN2CCCN(CC2)CCCC=CC3=CC(=C(C(=C3)OC)OC)OC

1H-1,4-Diazepine, hexahydro-1,4-bis[(4E)-5-(3,4,5-trimethoxyphenyl)-4-penten-1-yl]-

(-20℃)

With Ice Pack

≥ 2 years