SML2952
Tasisulam
≥98% (HPLC)
Synonym(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
Empirical Formula (Hill Notation):
C11H6BrCl2NO3S2
CAS Number:
Molecular Weight:
415.11
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
SMILES string
[S](=O)(=O)(NC(=O)c2c(cc(cc2)Cl)Cl)c1[s]c(cc1)Br
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)
InChI key
WWONFUQGBVOKOF-UHFFFAOYSA-N
Biochem/physiol Actions
RNA binding motif protein 39 (RBM39; CAPERα, HCC1) degradation-inducing SPLAM (SPLicing inhibitor sulfonAMide).
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.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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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
Global Trade Item Number
| SKU | GTIN |
|---|---|
| SML2952-25MG | 04065265102230 |
| SML2952-5MG | 04065265102247 |