MS147 | BMI1 and RING1B PROTAC | Probechem Biochemicals

Chemical Structure : MS147

MS147 (MS 147, MS-147)

Catalog No.: PC-49622Not For Human Use, Lab Use Only.

MS147 (MS 147) is the first degrader of PRC1 core components, BMI1 and RING1B, comprises an EED small-molecule binder (EED226, Cat. PC-42321) linked to a ligand of the E3 ligase von Hippel-Lindau (VHL), degrades BMI1/RING1B in an EED-, VHL-, ubiquitination-, and time-dependent manner.

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Biological Activity

MS147 (MS 147) is the first degrader of PRC1 core components, BMI1 and RING1B, comprises an EED small-molecule binder (EED226, Cat. PC-42321) linked to a ligand of the E3 ligase von Hippel-Lindau (VHL), degrades BMI1/RING1B in an EED-, VHL-, ubiquitination-, and time-dependent manner.

MS147 preferentially degrades BMI1/RING1B over polycomb repressive complex 2 (PRC2) core components.

MS147 shows binding affinities for VHL with Kd of 450 nM, and binds to EED with Kd of 3.0 uM in ITC assays.

MS147 selectively degrades BMI1 and RING1B over PRC2 core components and is selective for EED over 20 methyltransferases and 12 epigenetic reader domains, selectively reduces H2AK119ub (mediated by PRC1) over H3K27me3 (mediated by PRC2).

MS147 exhibits antiproliferative activities in multiple cancer cell lines, effectively suppresses the proliferation in K562 (GI50 = 3.8 uM), MDA‐MB‐231 (GI50 = 4.5 uM) and NCI‐H1299 (GI50 = 6.8 uM) cells in a concentration‐dependent manner.
MS147 is a useful chemical tool to further investigate the roles of PRC1 in cancer.

Physicochemical Properties

M.Wt	1015.29
Formula	C54H70N12O6S
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(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

References

1. Kwang-Su Park, et al. Adv Sci (Weinh). 2023 Feb 3;e2205573.

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MS147 (MS 147, MS-147)

Biological Activity

Physicochemical Properties

References

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