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Safety Information

SML3880

Sigma-Aldrich

CST626

new

≥98% (HPLC)

Synonym(s):

(2S,4S)-1-((S)-2-Cyclohexyl-2-((S)-2-(methylamino)-propanamido)acetyl)-4-(3-((5-(((S)-1-((2S,4R)-4-hydroxy-2-(((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-5-oxopentyl)oxy)phenoxy)-N-((R)-1,2,3,4-tetrahydronaphthalen-1-yl)pyrrolidine-2-carboxamide, IAP-VHL hetero-PROTAC 9

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About This Item

Empirical Formula (Hill Notation):
C61H82N8O9S
Molecular Weight:
1103.42
UNSPSC Code:
12352200

Quality Level

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

Biochem/physiol Actions

BIR domain-targeting degrader of inhibitor of apoptosis proteins (IAPs) cIAP1/2 and XIAP.



CST626 is a degrader of cellular inhibitor of apoptosis (IAP) proteins (cIAP1/cIAP2/XIAP DC50 post 16h = 2.4/6.2/0.7 nM with >99% degradation observed post 3h treatment at 100 nM; MM1S cells) that effectively reduces the viability of hematological cancer cultures, including MM (IC50 post 96h = 8.5 nM/NCI-H929, 1.14µM/JJN3, 2.54 µM/RPMI-8826), AML (IC50 post 96h = 2.1 nM/MOLM13, 420 nM/K562, 1.17 µM/HEL) and DLBCL (IC50 post 96h = 1.6 nM/SUDHL6, 460 nM/DB, 1.69 µM/SUDHL4). CST626 is composed of a von Hippel-Lindau (VHL) ligand VH032 derivative linked to a monovalent Smac (DIABLO) AVPI motif-based IAP BIR domain-targeting ligand.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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Yuen Lam Dora Ng et al.
Journal of medicinal chemistry, 66(7), 4703-4733 (2023-03-31)
Proteolysis targeting chimeras (PROTACs) represent a new pharmacological modality to inactivate disease-causing proteins. PROTACs operate via recruiting E3 ubiquitin ligases, which enable the transfer of ubiquitin tags onto their target proteins, leading to proteasomal degradation. However, several E3 ligases are

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