| Bioactivity | MS1943 is a first-in-class, orally bioavailable EZH2 selective degrader, with an IC50 of 120 nM. MS1943 significantly reduces EZH2 protein levels in numerous triple-negative breast cancer (TNBC) and other cancer and noncancerous cell lines. MS1943 effectively blocks proliferation of multiple TNBC and other cancer cell lines[1]. | ||||||||||||
| Invitro | MS1943 (0.625-5 μM; 3 days) inhibits cell growth with an GI50 of 2.2 µM[1].MS1943 (0.625-5 μM; 4 days) induces cell death in MDA-MB-468 cells. MS1943 effectively reduces EZH2 levels in BT549, HCC70 and MDA-MB-231 TNBC cells, as well as KARPAS-422 and SUDHL8 lymphoma cells and PNT2 non-cancerous prostate cells[1].MS1943 (1.25-5.0 μM; 2 days) inhibits EZH2 and SUZ12 protein levels in a concentration- and timedependent manner, without affecting EED protein levels, whereas the H3K27me3 mark was also suppressed[1]. Cell Viability Assay[1] Cell Line: | ||||||||||||
| Name | MS1943 | ||||||||||||
| CAS | 2225938-17-8 | ||||||||||||
| Formula | C42H54N8O3 | ||||||||||||
| Molar Mass | 718.93 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|