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MS 147

Catalog #: 8077 Datasheet
Catalog # Availability Size / Price Qty
8077/2
MS 147 | Active Degraders
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Description: PRC1 Degrader (PROTAC®); degrades BMI1 and RING1B

Chemical Name: (2S,4R)-1-((S)-2-(7-(5-(4-(4-(5-((Furan-2-ylmethyl)amino)-[1,2,4]triazolo[4,3-c]pyrimidin-8-yl)phenyl)piperazin-1-yl)pentanamido)heptanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide hydrochloride

Purity: ≥97%

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Biological Activity Technical Data Additional Information Product Datasheets Calculators

Biological Activity

MS 147 is a polycomb repressive complex 1 (PRC1) Degrader (PROTAC®) (Kd values are 450 nM and 3 μM for VHL and EED, respectively). Comprises an EED binder (EED 226, Cat. No. 7762) joined by a linker to a VHL E3 ligase ligand. MS 147 preferentially degrades BMI1 and RING1B and reduces H2AK119ub in K562 cells. Inhibits proliferation in cancer cell lines that are insensitive to EZH2 knockout or EED/PRC2 Degraders.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Important Information

This product is sold as an HCl salt. The stoichiometry of the salt and hydration levels vary from batch to batch. It is sold in gross weight and the batch specific Molecular Weight is available on the Certificate of Analysis.

Technical Data

M. Wt
1015.29 (Free Base)
Formula:
C54H70N12O6S.xHCl
Solubility:
Soluble to 50 mg/ml in DMSO
Purity:
≥97%
Storage:
Store at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold under license from Icahn School of Medicine at Mount Sinai.

Product Datasheets

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