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SML2952

Sigma-Aldrich

Tasisulam

≥98% (HPLC)

Synonyme(s) :

LY 573636, LY-573636, LY573636, N-(2,4-Dichlorobenzoyl)-5-bromothiophene-2-sulfonamide, N-(5-Bromothiophen-2-ylsulfonyl)-2,4-dichlorobenzamide, N-[(5-Bromo-2-thienyl)sulfonyl]-2,4-dichlorobenzamide

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About This Item

Formule empirique (notation de Hill):
C11H6BrCl2NO3S2
Numéro CAS:
519055-62-0
Poids moléculaire :
415.11
Numéro MDL:
MFCD11973637
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Pureté

≥98% (HPLC)

Forme

powder

Couleur

white to beige

Solubilité

DMSO: 2 mg/mL, clear

Température de stockage

2-8°C

InChI

1S/C11H6BrCl2NO3S2/c12-9-3-4-10(19-9)20(17,18)15-11(16)7-2-1-6(13)5-8(7)14/h1-5H,(H,15,16)

Clé InChI

WWONFUQGBVOKOF-UHFFFAOYSA-N

Actions biochimiques/physiologiques

Tasisulam (LY573636) is a SPLAM (SPLicing inhibitor sulfonAMide) that bridges RNA binding motif protein 39 (RBM39; CAPERα, HCC1) and DCAF15 for interaction, thereby promoting (CUL4-DDB1-DDA1-DCAF15) E3 ubiquitin ligase complex-mediated RBM39 ubiquitination and subsequent proteasomal degradation. Tasisulam exerts selective toxicity in parental HCT116 cancer cultures (IC50 = 6.5 μM), but not those harboring non-CUL4-DCAF15-associating RBM39 G268V mutant even at a high concentration of 50 μM.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

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Ting Han et al.
Science (New York, N.Y.), 356(6336) (2017-03-18)
Indisulam is an aryl sulfonamide drug with selective anticancer activity. Its mechanism of action and the basis for its selectivity have so far been unknown. Here we show that indisulam promotes the recruitment of RBM39 (RNA binding motif protein 39)
Tyler B Faust et al.
Nature chemical biology, 16(1), 7-14 (2019-11-07)
The investigational drugs E7820, indisulam and tasisulam (aryl-sulfonamides) promote the degradation of the splicing factor RBM39 in a proteasome-dependent mechanism. While the activity critically depends on the cullin RING ligase substrate receptor DCAF15, the molecular details remain elusive. Here we
Timothy Meier et al.
Molecular cancer therapeutics, 10(11), 2168-2178 (2011-09-10)
LY573636-sodium (tasisulam) is a small molecule antitumor agent with a novel mechanism of action currently being investigated in a variety of human cancers. In vitro, tasisulam induced apoptosis via the intrinsic pathway, resulting in cytochrome c release and caspase-dependent cell
Talin Haritunians et al.
Oncology reports, 20(5), 1237-1242 (2008-10-25)
LY573636-sodium is a promising anti-tumor agent, which causes growth arrest and apoptosis of a variety of human solid tumors in vitro and in vivo. Moreover, studies have shown that the compound is selectively toxic towards tumor cells over their normal
Everett J Perkins et al.
European journal of drug metabolism and pharmacokinetics, 43(3), 355-367 (2017-11-10)
Cytochrome P450 2C9 (CYP2C9) is involved in the biotransformation of many commonly used drugs, and significant drug interactions have been reported for CYP2C9 substrates. Previously published physiologically based pharmacokinetic (PBPK) models of tolbutamide are based on an assumption that its metabolic
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