MM-102 trifluoroacetate|Histone Methyltransferase (HMTase) Inhitibor&Antagonist&Agonist|DC Chemicals

Cas No.:
Chemical Name:	(S)-N-(bis(4-fluorophenyl)methyl)-1-(2-(2-ethyl-2-isobutyramidobutanamido)-5-guanidinopentanamido)cyclopentanecarboxamide 2,2,2-trifluoroacetate
Formula:	C₃₇H₅₀F₅N₇O₆
M.Wt:	783.8282
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

A high-affinity, small-molecule peptidomimetic inhibitor of MLL1/WDR5 protein-protein interaction with Ki of 2.4 nM; effectively decreases the expression of HoxA9 and Meis-1; specifically inhibits cell growth and induces apoptosis in leukemia cells harboring MLL1 fusion proteins.

MSDS

TITLE	DOWNLOAD
MSDS_13366_DC31042

COA

LOT NO.	DOWNLOAD

Cat. No.	Product name	Field of application
DC73330	IHMT-337	IHMT-337 (IHMT337) is a potent, highly selective and irreversible EZH2 inhibitor, specifically inhibits the methylation at H3K27.
DC73322	DP308	DP308 is a novel and effective 53BP1 tandem Tudor domain (TTD) inhibitor, disrupts the binding between 53BP1 and H4K20me2 peptide with IC50 of 1.69 uM.
DC72779	RK-701	RK-701 is an highly selective and non-genotoxic inhibitor of G9a with IC50 value of 23-27 nM. RK-701 selectively up-regulates HbF, γ- Globin, BGLT3 expression, down-regulates H3K9me2 expression. RK-701 also has inhibition for BCL11A and ZBTB7A.
DC72540	MS8815	MS8815 is a selective enhancer of zeste homolog 2 (EZH2) PROTAC degrader. MS8815 has inhibition activity for EZH2 with an IC50 value of 8.6 nM. MS8815 can be used for the research of triple-negative breast cancer (TNBC).
DC71676	EZM0414	EZM0414 is a potent, selective, and orally bioavailable inhibitor of Histone-lysine N-methyltransferase SETD2.
DC70785	SKLB-03176	SKLB-03176 (SKLB03176) is a potent, selective, covalent EZH2 inhibitor with IC50 of 47 nM, covalently binds to the SAM pocket of EZH2.SKLB-03176 showed good inhibitory activity against mutations EZH2 Y641F, EZH2 Y641N, and EZH2A677G at 200 nM concentration.SKLB-03176 exhibited weak activity against other targets, such as 5 histone methyltransferases and more than 30 kinases, >50-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1 (IC50=2.45 uM).SKLB-03176 inhibited the activity of a variety of EZH2 mutants and significantly inhibited the expression of H3K27Me3 in cells.SKLB-03176 showed no cytotoxicity to normal cells.
DC70095	NSD1 inhibitor BT5	NSD1 inhibitor BT5 is a covalent, small molecule inhibitor of NSD1 histone methyltransferase with IC50 of 1.4 uM, shows no covalent binding to NSD2.
DC47616	EPZ-719	EPZ-719 is a novel and potent SETD2 inhibitor ( IC50 = 0.005 μM) with a high selectivity over other histone methyltransferases.
DC47614	EEDi-5273	EEDi-5273 is an exceptionally potent and orally efficacious embryonic ectoderm development (EED) inhibitor with IC50 of 0.2 nM and inhibits the KARPAS422 cell growth with IC50 of 1.2 nM. EEDi-5273 demonstrates an excellent PK and ADME profile, and its oral administration leads to complete and persistent tumor regression in the KARPAS422 xenograft model with no signs of toxicity.
DC47117	MRTX-1719	MRTX-1719 is a potent first-in-class selective inhibitor of the PRMT5/MTA complex, with an IC50 of less than 10 nM in PRMT5/MTA MTAPDEL SDMA cells.