Sulfaphenazole

Catalog No.S3673 Batch:S367302

Technical Data

Formula	C₁₅H₁₄N₄O₂S
Molecular Weight	314.36	CAS No.	526-08-9
Solubility (25°C)*	In vitro	DMSO	63 mg/mL (200.4 mM)
		Ethanol	20 mg/mL (63.62 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Sulfaphenazole (Depocid, Depotsulfonamide, Plisulfan, Raziosulfa) is an inhibitor of CYP2C9 with Ki value of 0.3 μM and demonstrates at least 100-fold selectivity over other CYP450 isoforms (Ki values of 63 and 29 μM for CYP2C8 and CYP2C18, respectively, and no activity at CYP1A1, CYP1A2, CYP3A4, CYP2C19).

Targets

CYP2C9 ^[1]
(Cell-free assay)

0.3 μM(Ki)

In vitro

Cystamine is a transglutaminase (TGase) inhibitor. In addition to TGase inhibition, cystamine is able to replenish glutathione and to inhibit caspase activity. The inhibitory capacity of cystamine in vitro is largely affected by the extent of the reduced form of the molecule. Nonetheless, cystamine inhibits in situ TGase activity decidedly stronger than cysteamine^[1].

In vivo

Treatment with cystamine results in prolonged survival and decreased abnormal movements in a murine model of HD（Huntington's disease）. Cystamine does not cross the blood brain barrier^[1]. Cystamine treatment normalizes transglutaminase and GGEL levels in R6/2 mice. cystamine has significant efficacy in improving the neurological and neuropathological phenotype observed in the R6/2 transgenic model of HD and strongly suggests that Tgase plays a role in HD^[2].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines DU145 cells Concentrations 50, 100, 150, 200 μM Incubation Time -- Method The cells (2×10⁶) are labeled with BP at 1 mM or amine compounds (0 to 1.0 mM) in serum-free medium for 1h prior to harvesting. After washing twice with PBS, the cells are suspended in PBS containing protease inhibitors and sonicated (2 s pulse/2 s pause×5, 20% amplitude). The homogenate is centrifuged for 10 min at 20,000g at 4℃. The cell extract(0.2 mg/ml, 50 μl/well) is coated in the wells of a 96-well microtiter plate for 12 h at 4℃. The wells are then overcoated with 5% BSA in PBS for 1 h at room temperature. After washing three times with PBST, BP incorporated into the cellular proteins is assessed as performed in microtiter plate assays.
Animal Study:^{^[2]}	Animal Models wild-type (Wt) and R6/2 mice Dosages 112, 225, and 400 mg/kg Administration i.p.

Cell Assay:^{^[1]}

Cell lines
DU145 cells
Concentrations
50, 100, 150, 200 μM
Incubation Time
--
Method
The cells (2×10⁶) are labeled with BP at 1 mM or amine compounds (0 to 1.0 mM) in serum-free medium for 1h prior to harvesting. After washing twice with PBS, the cells are suspended in PBS containing protease inhibitors and sonicated (2 s pulse/2 s pause×5, 20% amplitude). The homogenate is centrifuged for 10 min at 20,000g at 4℃. The cell extract(0.2 mg/ml, 50 μl/well) is coated in the wells of a 96-well microtiter plate for 12 h at 4℃. The wells are then overcoated with 5% BSA in PBS for 1 h at room temperature. After washing three times with PBST, BP incorporated into the cellular proteins is assessed as performed in microtiter plate assays.

Animal Study:^{^[2]}

Animal Models
wild-type (Wt) and R6/2 mice
Dosages
112, 225, and 400 mg/kg
Administration
i.p.

References

Selleck's Sulfaphenazole has been cited by 3 publications

Die Optimierung einer Multiplex-Färbung für verschiedene Metastasen des Melanoms [ UNIVERSITY OF APPLIED SCIENCES, 2023, ]	PubMed: none
Potential herb-drug interaction risk of thymoquinone and phenytoin [ Chem Biol Interact, 2022, 353:109801]	PubMed: 34998822
Potential food-drug interaction risk of thymoquinone with warfarin [ Chem Biol Interact, 2022, 365:110070]	PubMed: 35921950

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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