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Cuspin-1 Sale

(Synonyms: Chemical Upregulator of SMN Protein-1) 目录号 : GC43332

An upregulator of SMN protein

Cuspin-1 Chemical Structure

Cas No.:337932-29-3

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5mg
¥770.00
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10mg
¥1,318.00
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25mg
¥2,895.00
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50mg
¥5,396.00
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产品描述

The Survival of Motor Neurons (SMN) protein participates in RNA splicing. Decreases in SMN, typically a consequence of defects in the smn1 gene, result in the death of motor neurons and lead to the neurodegenerative disease, spinal muscular atrophy (SMA). Cuspin-1 is a small molecule upregulator of SMN that has been shown in vitro to increase levels of SMN in SMA patient fibroblasts by 50% at 18 µM. Its mechanism of action is thought to involve increased phosphorylation of ERK to initiate Ras-Raf-MEK signaling, which results in an increased rate of SMN translation.

Chemical Properties

Cas No. 337932-29-3 SDF
别名 Chemical Upregulator of SMN Protein-1
Canonical SMILES CC1=CC=C(C(C2=CC(Br)=CN=C2)=O)C=C1
分子式 C13H10BrNO 分子量 276.1
溶解度 DMF: 25 mg/mL,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 16 mg/mL,Ethanol: 1 mg/mL 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 3.6219 mL 18.1094 mL 36.2188 mL
5 mM 0.7244 mL 3.6219 mL 7.2438 mL
10 mM 0.3622 mL 1.8109 mL 3.6219 mL
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Research Update

Small molecule screen reveals regulation of survival motor neuron protein abundance by Ras proteins

ACS Chem Biol 2013 May 17;8(5):914-22.PMID:23496866DOI:PMC3665055

Small molecule modulators of protein activity have proven invaluable in the study of protein function and regulation. While inhibitors of protein activity are relatively common, small molecules that can increase protein abundance are rare. Small molecule protein upregulators with targeted activities would be of value in the study of the mechanisms underlying loss-of-function diseases. We developed a high-throughput screening approach to identify small molecule upregulators of the Survival of Motor Neuron protein (SMN), whose decreased levels cause the neurodegenerative disease spinal muscular atrophy (SMA). We screened 69,189 compounds for SMN upregulators and performed mechanistic studies on the most active compound, a bromobenzophenone analogue designated Cuspin-1. Mechanistic studies of Cuspin-1 revealed that increasing Ras signaling upregulates SMN protein abundance via an increase in translation rate. These findings suggest that controlled modulation of the Ras signaling pathway may benefit patients with SMA.