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MMRi62
Cat. No. IC23206
CAS. No. 352693-80-2
Key Features and Details
Category
Inhibitor&Activator
Purity
0.9958
Formula
C21H15Cl2N3O
Product Details
Product Name
MMRi62
CAS No.
352693-80-2
Molecular Weight
396.27
Formula
C21H15Cl2N3O
Appearance
Solid
Purity
0.9958
SMILES
OC1=C2N=CC=CC2=CC=C1C(C3=CC=CC(Cl)=C3Cl)NC4=NC=CC=C4
Product Overview
Description
MMRi62, a ferroptosis inducer targeting MDM2-MDM4 (negative regulators of tumor suppressor p53). MMRi62 shows a P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induce autophagy. MMRi62 inducesferroptosis, resulting in a increase of reactive oxygen and lysosomal degradation of ferritin heavy chain (FTH1). MMRi62 also leads to proteasomal degradation of mutant p53, also inhibits orthotopic xenograft PDAC mouse model in vivo with high frequency mutation characteristics of KRAS and TP53.12.
In Vitro Activity
MMRi62 inhibits proliferation, clonogenic, and spheroid growth of pancreatic ductal adenocarcinoma cell (PDAC) by induction of cell death. 1
MMRi62 (3 nM-100 μM;4 h) binds to RING–RINGheterodimers of MDM2 and MDM4 withthe Kd value of 1.39 μM.
MMRi62 (10 nM-1 μM;72 h) induces apoptosis and inhibits leukemic cells with IC50sof 0.34 µM (HL60) and 0.22 µM (HL60VR).
MMRi62 (5 μM and 10μM; 24 h) decreases MDM2B autoubiquitination, increasesMDM4 ubiquitination in a dose-dependent manner.
MMRi62 is an E3 ligase modifier capable ofswitching substrate preference from MDM2 to MDM4.
MMRi62 (5 μM; 24and 72 h) induces apoptosis in a p53-independent manner.
In Vivo Activity
MMRi62 shows anti-tumor activity in orthotopic xenograft PDAC mouse models, by inhibiting tumor growth in mice associated with downregulation of NCOA4 and mutant p53.
MMRi62 also completely abrogates metastasis of orthotopic tumors.
Storage & Handling
Storage
4 °C, protect from light
In solvent : -80 °C, 6 months; -20 °C, 1 month (protect from light)
Shipping
Room temperature in continental US; may vary elsewhere.
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