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Sotrastaurin is a potent and specific inhibitor of protein kinase C (PKC) with Ki at subnanomolar to low nanomolar range for a variety of PKC isotypes while selective for >200 other kinases. Sotrastaurin is an immunosuppressant that blocks early T-lymphocyte (T-cell) activation via protein kinase C inhibition. Sotrastaurin combined with EVR showed higher efficacy failure rates and some improvement in renal allograft function compared to a CsA-based therapy. Sotrastaurin inhibits nuclear factor (NF)-κB, which directly promotes the transcription of forkhead box protein 3 (FoxP3), the key regulator for the development and function of regulatory T cells (Tregs). Sotrastaurin is a potent inhibitor of alloreactivity in vitro, while it did not affect Treg function in patients after kidney transplantation. Sotrastaurin prevented TCR/CD28-induced T-cell activation and pro-inflammatory cytokine production, but preserved a stable Treg phenotype as evidenced by maintenance of suppressive capacity, high Foxp3 and CD25 expression, and lack of IL-17A and IFNγ production.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| Animal models | male Wistar/F rats |
| Formulation | Saline |
| Dosages | 10 mg/kg and 30 mg/kg |
| Administration | Orally administrated |
| Molecular Weight | 438.48 |
| Formula | C25H22N6O2 |
| CAS Number | 425637-18-9 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PKC Products |
|---|
| Enzastaurin
Enzastaurin inhibits PKCβ, PKCα, PKCγ and PKCε with IC50's of 0.006, 0.039, 0.083 and 0.110 µM, respectively. |
| Go 6983
Go 6983 is a fast acting, lipid soluble, broad spectrum protein kinase C inhibitor. |
| Staurosporine
Staurosporine (AM-2282) is a potent ATP-competitive kinase inhibitor with IC50 of 0.7, 7, 8.5, 6, 20 nM for PKC, PKA,PKG, p60v-src tyrosine protein kinase, CaM kinase II, respectively. |
| Dequalinium Chloride
Dequalinium Chloride is a PKC inhibitor with IC50 of 7-18 μM, and also a selective blocker of apamin-sensitive K+ channels with IC50 of 1.1 μM. |
| K252a
K252a is an inhibitor of the BDNF receptor TrkB. K-252a inhibits protein kinase with IC50 values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca2+/calmodulin-dependent kinase type II, and phosphorylase kinase, respectively. K-252a is a potent inhibitor (IC50 of 3 nM) of the tyrosine protein kinase (TRK) activity of the NGF receptor gp140trk, the product of the trk protooncogene. |
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