| Identification | Back Directory | [Name]
INDEX NAME NOT YET ASSIGNED | [CAS]
2375432-47-4 | [Synonyms]
N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-6-((1-(19-((4R)-4-hydroxy-2-((1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)carbamoyl)pyrrolidine-1-carbonyl)-20,20-dimethyl-17-oxo-3,6,9,12,15-pentaoxa-18-azahenicosanoyl)azetidin-3-yl)amino)pyrimidine-4-carboxamide | [Molecular Formula]
C55H76N10O12S | [MOL File]
2375432-47-4.mol | [Molecular Weight]
1101.33 |
| Chemical Properties | Back Directory | [Boiling point ]
1254.3±65.0 °C(Predicted) | [density ]
1.295±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (90.80 mM; Need ultrasonic) | [form ]
Solid | [pka]
12.41±0.46(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
MS4322 (YS43-22) is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 ))[1]. | [Biological Activity]
MS4322 (YS43-22) is a first-in-class PRMT5 degrader and a valuable chemical tool (PROTAC) for exploring the PRMT5 functions in health and disease. | [in vivo]
MS4322 (150 mg/kg, i.p., single dose, male Swiss albino mice) results in good exposure levels in plasma and reaches the highest plasma concentration (14 μM) 2 hours after administration. After 12 hours, the concentration of MS4322 is still above 100 nM. In addition, MS4322 is well tolerated in treated mice. [1].
| [IC 50]
VHL; Cereblon; MDM2; SMYD2; SMYD3; EHMT1/GLP/KMT1D; SETD7/KMT7; PRMT4; PRMT8; EZH1; SETDB1/KMT2G; SETD8/KMT5A; PRMT5; EZH2; SUV39H2/KMT1B; SETD2/KMT3A; PRMT1; PRMT6; DOT1L; EHMT2/G9a/KMT1C; NSD2; PRMT3; PRMT7 | [References]
[1]. Shen Y, et al. Discovery of First-in-Class Protein Arginine Methyltransferase 5 (PRMT5) Degraders. J Med Chem. 2020 Sep 10;63(17):9977-9989. |
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| Company Name: |
R&D Systems, Inc
|
| Tel: |
18003437475 18003437475 |
| Website: |
www.rndsystems.com |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|