Sulfaphenazole

Catalog No.S3673 Synonyms: Depocid, Depotsulfonamide, Plisulfan, Raziosulfa

Sulfaphenazole Chemical Structure

Molecular Weight(MW): 314.36

Sulfaphenazole 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).

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Biological Activity

Description Sulfaphenazole 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

Cell Research:[1]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[2]
+ Expand
  • Animal Models: wild-type (Wt) and R6/2 mice
  • Formulation: PBS
  • Dosages: 112, 225, and 400 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 62 mg/mL (197.22 mM)
Ethanol 62 mg/mL (197.22 mM)
Water 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.

Chemical Information

Molecular Weight 314.36
Formula

C15H14N4O2S

CAS No. 526-08-9
Storage powder
in solvent
Synonyms Depocid, Depotsulfonamide, Plisulfan, Raziosulfa

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID