MS645|MS-645;MS 645

Cas No.:
Chemical Name:	(S)-N,N'-(decane-1,10-diyl)bis(2-((6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f] [1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamide)
Synonyms:	MS-645;MS 645
SMILES:	C(NC(=O)C[C@H]1N=C(C2=CC=C(Cl)C=C2)C2C(C)=C(C)SC=2N2C(C)=NN=C21)CCCCCCCCCNC(=O)C[C@H]1N=C(C2=CC=C(Cl)C=C2)C2C(C)=C(C)SC=2N2C(C)=NN=C21
Formula:	C₄₈H₅₄Cl₂N₁₀O₂S₂
M.Wt:	938.048
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

MS645 (MS-645) is a novel, bivalent bromodomain (BRD) inhibitor with Ki of 18.4 nM for tandem BD1-BD2 (BRD4 BD1/BD2 ), shows12- to 28-fold gain in affinity for binding to the tandem BD1-BD2 over the single BD1 or BD2; shows comparable potency to the tandem BD1-BD2 of BRD2 and BRD3 as to that of BRD4; inhibits the transcription of BRD4 target gene IL-6 in MDA-MB-231 cells with 70% inhibition at 20 nM, much higher than 20-30% inhibition by JQ1 and MS417; potently inhibits cell growth of a panel TNBC with IC50 of 4-20 nM, blocks BRD4 binding to transcription enhancer/mediator proteins MED1 and YY1 with potency superior to monovalent BET inhibitors Reference: JQ1.C Ren, G Zhang, F Han, S Fu, Y Cao, F Zhang, Q Zhang, J Meslamani, Proceedings of the National Academy of Sciences 115 (31), 7949-7954

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC10190	TPOP146	TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4.
DC11041	QCA276	QCA276 is a novel potent BET proteins inhibitor with IC50/Ki of 10/.3 nM, QCA276 is the BET ligand for PROTAC QCA570.
DC12248	PROTAC BET degrader-2	PROTAC BET degrader-2 is a highly potent degrader of Bromodomain and Extra-Terminal (BET) proteins with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression.
DC11063	MS645	MS645 (MS-645) is a novel, bivalent bromodomain (BRD) inhibitor with Ki of 18.4 nM for tandem BD1-BD2 (BRD4 BD1/BD2 ), shows12- to 28-fold gain in affinity for binding to the tandem BD1-BD2 over the single BD1 or BD2.
DC12313	GNE-371	GNE-371 is a potent and selective chemical probe for the second bromodomains of human transcription-initiation-factor TFIID subunit 1 and transcription-initiation-factor TFIID subunit 1-like, with an IC50 of 10 nM for TAF1(2).
DC9934	GNE-272	GNE-272 is a in Vivo Probe for the Bromodomains of CBP/EP300.
DC8556	BET-BAY 002	BET-BAY 002 is a potent BET inhibitor; shows efficacy in a multiple myeloma model.
DC11042	BET inhibitor CF53	BET inhibitor CF53 is a highly potent, orally active inhibitor of bromodomain and extra-terminal (BET) with Ki of <1 nM (BRD4 BD1).
DC7854	BAZ2-ICR	BAZ2-ICR is a selective BAZ2 bromodomain inhibitor (Kd values are 109 and 170 nM for BAZ2A and BAZ2B respectively).
DC11568	HJB-97	A potent BET bromodomian inhibitor with IC50 of 3-7 nM for BRD2/3/4 BD1 and BD2..