| Bioactivity | Chst15-IN-1 is a potent reversible covalent Chst15 inhibitor. Chst15-IN-1 effectively inhibits chondroitin sulfate-E (CS-E) sulfation levels and other closely related glycosaminoglycans (GAG) sulfotransferases. Chst15-IN-1, as a selective sulfotransferase inhibitor, can diminish the inhibitory effects of chondroitin sulfate proteoglycans (CSPGs), and can be used for the stimulation of neuronal repair[1]. | |||||||||
| Target | Chst15 | |||||||||
| Invitro | Chst15-IN-1 (25 μM; 24 hours; Neu7 astrocytes) is selective for sulfotransferases over the myriad of reactive cysteine-containing proteins. Chst15-IN-1 (10 and 25 μM; Neu7 astrocytes) shows a significant dose dependent decrease in cell-surface CS-E expression[1]. | |||||||||
| In Vivo | Chst15-IN-1 (3.0 mg/kg; i.v.) has a moderate clearance of 21 mL/min/kg, moderate volume of distribution of 0.97 L/kg, and short terminal half-life of 1.6 hours[1]. Animal Model: | |||||||||
| Name | Chst15-IN-1 | |||||||||
| CAS | 2158198-77-5 | |||||||||
| Formula | C17H11BrCl2N2O3 | |||||||||
| Molar Mass | 442.09 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Cheung ST, et al. Discovery of a Small-Molecule Modulator of Glycosaminoglycan Sulfation. ACS Chem Biol. 2017;12(12):3126-3133. |
Chst15-IN-1
CAS: 2158198-77-5 F: C17H11BrCl2N2O3 W: 442.09
Chst15-IN-1 is a potent reversible covalent Chst15 inhibitor. Chst15-IN-1 effectively inhibits chondroitin sulfate-E (CS
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