GNE-272|GNE272|Bromodomains CBP/EP300 probe

Cas No.:	1936428-93-1
Synonyms:	GNE272,GNE 272
SMILES:	CC(N1CCC2=C(C(NC3=C(F)C=C(C4=CN(C)N=C4)C=C3)=NN2[C@H]5CCOC5)C1)=O
Formula:	C₂₂H₂₅FN₆O₂
M.Wt:	424.2
Purity:	>98%
Sotrage:	4°C for 1 year, -20°C for more than 2 years

Description:

GNE-272 is a potent and selective in Vivo Probe for the Bromodomains of CBP/EP300 (CBP IC50 = 0.02 μM, EP300 IC50 = 0.03 μM, BRET IC50 = 0.41 μM, BRD4(1) C50 = 13 μM).GNE-272 showed a marked antiproliferative effect in hematologic cancer cell lines and modulates MYC expression in vivo that corresponds with antitumor activity in an AML tumor model. CBP has also been implicated in neurological disorders where a CBP bromodomain inhibitor has been shown to reduce expression of a regulator of G-protein signaling (RGS4).

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..