SecinH3 is a selective cytohesin inhibitor for hCyh2, hCyh1, mCyh3, hCyh3, drosophila steppke, and yGea2-S7 with IC50 of 2.4 μM, 5.4 μM, 5.4 μM, 5.6 μM, 5.6 μM, and 65 μM respectively.
SecinH3 is a selective cytohesin inhibitor for hCyh2, hCyh1, mCyh3, hCyh3, drosophila steppke, and yGea2-S7 with IC50 of 2.4 μM, 5.4 μM, 5.4 μM, 5.6 μM, 5.6 μM, and 65 μM respectively. SecinH3 almost completely blocks the insulin-dependent transcriptional repression of IGFBP1 with an IC50 of 2.2 μM. Insulin-stimulated translocation of ARF6 to the plasma membrane is also inhibited by SecinH3. SecinH3-treated mice show increased expression of gluconeogenic genes, reduced expression of glycolytic, fatty acid and ketone body metabolism genes in the liver, reduced liver glycogen stores, and a compensatory increase in plasma insulin[3]. SecinH3, a cytohesin inhibitor, has neuroprotective effects against mutant SOD1 toxicity. SecinH3 was demonstrated to successfully attenuate the TDP-43 (transactivating response region DNA binding protein 43) Q331K-induced neuronal toxicity by suppressing ER (endoplasmic reticulum) stress-mediated apoptosis and enhancing the autophagic flux[4]. SecinH3 can significantly inhibit the cytohesins and then relieve the lung injury induced by the sepsis of rats[5]. Treating mice bearing H460 xenografts with SecinH3 showed the antiproliferative and pro-apoptotic effect of SecinH3 in vivo[6].
To investigate the effect of SecinH3 on platelet dense granule secretion and aggregation, results showed that SecinH3 significantly enhanced ATP secretion from dense granules and platelet aggregation.
J Thromb Haemost. 2014 May;12(5):726-35
Mouse neutrophils
20 µM
20 minutes
Impairs polarization of RPH3A, RAB21, and PIP5K1C90
J Immunol. 2020 Feb 15;204(4):1012-1021
INS 832/13 cells
50 µM
30 min
Inhibited glucose-induced Arf6 activation and insulin secretion
Biochem Pharmacol. 2011 Apr 15;81(8):1016-27
HCT116 cells
10, 20, 40 µM
48 hours
Inhibited cell migration
PLoS One. 2014 Mar 11;9(3):e90997
Mouse preadipocyte 3T3-L1 cells
10 µM
6 and 10 hours
SecinH3 markedly inhibits migration of 3T3-L1 cells
J Biol Chem. 2010 Jul 30;285(31):24270-81
SecinH3 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
H460 xenograft model
Intraperitoneal injection
2.5 mM
Once daily for 9 days
SecinH3 significantly retarded the growth of H460 xenografts and increased tumor cell apoptosis
PLoS One. 2012;7(7):e41179
Nude mice
HT29 tumor xenograft model
Intraperitoneal injection
2.5 mM
Once daily for 14 days
Inhibited tumor growth
PLoS One. 2014 Mar 11;9(3):e90997
NOD/SCID mice
Subcutaneous tumor model
Intraperitoneal injection
50 mg/kg
Once daily for 12 days
SecinH3 inhibits AML growth and infiltration
Acta Pharmacol Sin. 2024 Jan;45(1):180-192
Mice
OVA-induced allergic asthma model
Intranasal administration
50 nmol/head
Administered 1 day after the first OVA challenge, followed by OVA challenges on days 3 and 6
Evaluate the therapeutic effect of SecinH3 on allergic asthma
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