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MS147

CAT: 0804-HY-160924-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-160924-01Size:1 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
MS147 is a VHL-based PROTAC degrader of PRC1 (Polycomb Repressive Complex 1). The dissociation constants (Kd) of MS147 for EED (Embryonic Ectoderm Development) and VHL (Von Hippel-Lindau) are 3.0 μM and 450 nM, respectively. MS147 specifically binds to the EED protein through its EED-binding moiety; EED is a core component of PRC2 (Polycomb Repressive Complex 2) and interacts with the core components of PRC1, BMI1 (B-lymphoma Mo-MLV insertion region 1 homolog) and RING1B (Ring Finger Protein 1B). By this binding, MS147 is able to recruit BMI1 and RING1B near to VHL. Through the degradation of BMI1 and RING1B, MS147 reduces the level of H2AK119ub (histone H2A lysine 119 ubiquitination), affecting the proliferation of cancer cells. (Blue: VHL ligand , Black: linker ; Pink: PRC1 ligand (HY-158771) ).
UNSPSC
12352005
Target
E1/E2/E3 Enzyme; PROTACs
Type
Reference compound
Related Pathways
Metabolic Enzyme/Protease; PROTAC
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/ms147.html
Purity
98.31
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
O=C([C@H]1N(C([C@@H](NC(CCCCCCNC(CCCCN2CCN(C3=CC=C(C4=CN=C(NCC5=CC=CO5)N6C4=NN=C6)C=C3)CC2)=O)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC7=CC=C(C8=C(C)N=CS8)C=C7
Molecular Formula
C54H70N12O6S
Molecular Weight
1015.28
References & Citations
[1]Park K S, et al. Targeted degradation of PRC1 components, BMI1 and RING1B, via a novel protein complex degrader strategy[J]. Advanced Science, 2023, 10 (10) : 2205573.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported

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