MS1943
MS1943 is an orally active, PROTAC-based, selective degrader of EZH2 that effectively reduces EZH2 levels in cells. MS1943 has anticancer activity and exhibits cytotoxic effects in a variety of TNBC cells while sparing normal cells. In addition, MS1943 maintains high potency (IC50=120 nM) in inhibiting EZH2 methyltransferase activity and is highly selective for EZH2. (Structure Note: RED, EZH2 ligand (HY-148458) ; Blue, Hyt (HY-W001578) ) [1].
Product Specifications
CAS Number
[2225938-17-8]
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Apoptosis; Histone Methyltransferase; PROTACs
Type
Reference compound
Related Pathways
Apoptosis; Epigenetics; PROTAC
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/ms1943.html
Purity
98.92
Solubility
DMSO : 125 mg/mL (ultrasonic)
Smiles
CC(C)N(N=C1)C2=C1C(C(NCC3=C(C)C=C(C)NC3=O)=O)=CC(C4=CC=C(N=C4)N(CC5)CCN5CCNC(CC67C[C@H]8C[C@H](C[C@H](C8)C7)C6)=O)=C2
Molecular Formula
C42H54N8O3
Molecular Weight
718.93
Precautions
H302, H315, H319, H335
References & Citations
[1]Ma A, et al. Discovery of a first-in-class EZH2 selective degrader[J]. Nature chemical biology, 2020, 16 (2) : 214-222.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
EZH2
Available Sizes
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