K-7174 dihydrochloride

SKU: orb1941061

Description

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.(In Vitro):K-7174 dihydrochloride (10 μM; 1 h) inhibits the adhesion by VCAM-1 and its ligand.K-7174 dihydrochloride (1-30 μM; 1 h) dose-dependently suppresses the VCAM-1 expression with an IC50 value of 14 μM.K-7174 dihydrochloride (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 dihydrochloride (10-20 μM; 24 h) dose-dependently rescues Epo production by Hep3B cells.K-7174 dihydrochloride (2.5-30 μM; 24 h) inhibits the binding activity of GATA.K-7174 dihydrochloride (0-25 μM; 72 h) inhibits MM cells growth and induces cell apoptosis.(In Vivo):K-7174 dihydrochloride (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 dihydrochloride (75 mg/kg; i.p. once daily for 14 days) inhibits the tumor growth in vivo.K-7174 dihydrochloride (50 mg/kg; p.o. once daily for 14 days) inhibits the tumor growth in vivo and shows a better effect than intraperitoneal injection.

Images & Validation

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Key Properties

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CAS Number	191089-60-8
MW	641.6659
Purity	>98% (HPLC)
Formula	C₃₃H₅₀Cl₂N₂O₆
SMILES	COC1=CC(=CC(=C1OC)OC)C=CCCCN2CCCN(CC2)CCCC=CC3=CC(=C(C(=C3)OC)OC)OC.Cl.Cl
Target	GATA Binding Protein
Solubility	H2O: 15 mg/mL

Bioactivity

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In Vivo

K-7174 dihydrochloride (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 dihydrochloride (75 mg/kg; i.p. once daily for 14 days) inhibits the tumor growth In vivo. K-7174 dihydrochloride (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. Porved oral administration is more effective than intraperitoneal injection.

In Vitro

K-7174 dihydrochloride (10 μM; 1 h) inhibits the adhesion by VCAM-1 and its ligand. K-7174 dihydrochloride (1-30 μM; 1 h) dose-dependently suppresses the VCAM-1 expression with an IC50 value of 14 μM. K-7174 dihydrochloride (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 dihydrochloride (10-20 μM; 24 h) dose-dependently rescues Epo production by Hep3B cells. K-7174 dihydrochloride (2.5-30 μM; 24 h) inhibits the binding activity of GATA. K-7174 dihydrochloride (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.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

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Gene Symbol

GATA Binding Protein

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