Molecular Formula | C5H3N5O2S3 |
Molar Mass | 261.3 |
Density | 1.88±0.1 g/cm3(Predicted) |
Melting Point | 160 °C(dec.) |
Boling Point | 549.8±42.0 °C(Predicted) |
Appearance | Pale yellow solid |
pKa | 0.65±0.10(Predicted) |
Storage Condition | Store at RT |
In vitro study | SU3327 (compound 9) is able to inhibit TNF-α stimulated phosphorylation of c-Jun in HeLa cells (EC 50 = 6.23 μM). SU3327 (25 nM) pretreatment of human-derived cerebral microvascular endothelial cells (hCMEC/D3) effectively reduces LPS-induced polymorphonuclear leukocytes (PMN) rolling/adhesion to hCMEC/D3, prevents activation of AP-1, and significantly reduces expression of VCAM-1. |
In vivo study | SU3327 (Compound 9; 25 mg/kg; intraperitoneal injection; male BKS.Cg-+Lepr db /+Lepr db /OlaHsd db/db mice) treatment possesses the ability to restore insulin sensitivity in mice models of diabetes. SU3327 (Compound 9) has favorable microsomal and plasma stability (T 1/2 = 27 min). Animal Model: Male BKS.Cg-+Lepr db /+Lepr db /OlaHsd db/db mice (11-week-old ) injected with insulin Dosage: 25 mg/kg Administration: Intraperitoneal injection Result: Resulted in a statistically significant reduction in blood glucose levels. |
biological activity | SU3327 is an effective, selective and substrate competitive JNK inhibitor with IC50 of 0.7 μM. SU3327 also inhibited the protein interaction between JNK and JIP with IC50 value as 239 nM. SU3327 has low activity against p38α and Akt kinase. |
target | IC50: 0.7 μM (JNK); 239 nM (JNK-JIP interactions) |
in vitro study | SU3327 (compound 9) is able to inhibit TNF-α stimulated phosphorylation of c-Jun in HeLa cells (EC 50=6.23 μ m). SU3327 (25 nm) pretreatment of human-derived cerebral microvascular endothelial cells (hCMEC/D3) effectively reduces LPS-induced polymorphonuclear leukocytes (PMN) rolling/adhesion to hCMEC/D3, prevents activation of AP-1, and significantly reduces expression of VCAM-1. |
in vivo study | SU3327 (Compound 9; 25 mg/kg; intraperitoneal injection; male BKS.Cg- Lepr db / Lepr db /OlaHsd db/db mice) treatment possesses the ability to restore insulin sensitivity in mice models of diabetes. SU3327 (Compound 9) has favorable microsomal and plasma stability (T 1/2=27 min). Animal Model: male bks. cg-lepr db/lepr db/olahsd db/db mice (11-week-old ) injected with insulin Dosage: 25 mg/kg Administration: Intraperitoneal injection Result: Resulted in a statistically significant reduction in blood glucose levels. |
Animal Model: | Male BKS.Cg- Lepr db / Lepr db /OlaHsd db/db mice (11-week-old ) injected with insulin |
Dosage: | 25 mg/kg |
Administration: | Intraperitoneal injection |
Result: | Resulted in a statistically significant reduction in blood glucose levels. |