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MS177 is an effective and fast-acting EZH2 degrader. MS177 is a PROTAC that consists of a CRBN ligand, linker, and a potent enzymatic EZH2 inhibitor C24 (C24 IC50): 12 nM). MS177 effectively depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes. MS177 induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest.
| Molecular Weight | 914.02 |
| Formula | C48H55N11O8 |
| CAS Number | 2225938-86-1 |
| Form | Solid |
| Solubility (25°C) | DMSO 125 mg/mL (ultrasonic) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PROTAC Products |
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| GDC-2992
GDC-2992 is an orally active androgen receptor (AR) degrader. GDC-2992 degrads AR with a DC50 value of 2.7 nM and inhibits proliferation with an IC50 valude of 9.7 nM in VCaPcells. |
| Setidegrasib
Setidegrasib is a PROTAC KRAS degrader (DC50: 37 nM). Setidegrasib induces the degradation of G12D-mutation KRAS protein. Setidegrasib has antitumor effect. |
| PROTAC HK2 Degrader-1
PROTAC HK2 Degrader-1 is a PROTAC consisting of Lonidamine as a target protein Hexokinase 2 (HK2) inhibitor and Thalidomide as a CRBN ligand-linked PROTAC. PROTAC HK2 Degrader-1 selectively inhibits the proliferation of breast cancer cells by forming a ternary complex through the ubiquitin-proteasome system to degrade Hexokinase 2 (HK2) protein leading to mitochondrial damage and cell death. |
| ZXH-4-130 TFA
ZXH-4-130 TFA is a highly potent and selective degrader of CRBN. ZXH-4-130 is a CRBN-VHL compound (hetero-PROTAC). |
| MS4322
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. |
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