eIF4A3-IN-1q|

Cas No.:	2132392-89-1
Chemical Name:	(S)-5-(4-(5-bromopicolinoyl)-3-(4-chlorophenyl)piperazine-1-carbonyl)-1-phenyl-3-(trifluoromethyl)pyridin-2(1H)-one
SMILES:	C(=O)1N(C2=CC=CC=C2)C=C(C(N2CCN(C(=O)C3=NC=C(Br)C=C3)[C@H](C3=CC=C(Cl)C=C3)C2)=O)C=C1C(F)(F)F
Formula:	C₂₉H₂₁BrClF₃N₄O₃
M.Wt:	645.861
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

A potent, subtype-selective, orally available eIF4A3 inhibitor with IC50 of 0.14 uM; displays no activity against eIF4A1, eIF4A2, BRR2 and DHX29 (IC50>100 uM); upregulates SC35 1.6 kb mRNA expression by 8-fold at 3 uM and 20-fold at 10 uM, potently inhibit cell growth in HCT-116 cells (GI50=1.18 uM) ; shows antitumor efficacy and promising PK profiles in vivo, without severe body weight loss.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC47660	eIF4A3-IN-4	eIF4A3-IN-4 is a novel eIF4A inhibitor with an IC50 value of 8.6 μM.
DC45877	ATPγS tetralithium salt	ATPγS (tetralithium salt) is a substrate for the nucleotide hydrolysis and RNA unwinding activities of eukaryotic translation initiation factor eIF4A.
DC44088	rel-Zotatifin	rel-Zotatifin is the racemic isomer of Zotatifin, acts as an eIF4A inhibitor with activity less than Zotatifin. Zotatifin (eFT226) is a potent, selective, and well-tolerated eIF4A inhibitor. Zotatifin promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5’-UTRs (IC50=2 nM) and interferes with the assembly of the eIF4F initiation complex.
DC41130	(Z)-4EGI-1	(Z)-4EGI-1 is the Z-isomer of 4EGI-1 and is an inhibitor of eIF4E/eIF4G interaction and of translation initiation. (Z)-4EGI-1 effectively binds to eIF4E with an IC50 of 43.5 μM and a Kd value of 8.74 μM. (Z)-4EGI-1 has anticancer activity.
DC40949	CR-1-31-B	CR-1-31-B is a potent eIF4A RNA helicase inhibitor. CR-1-31-B blocks MUC1-C translation in response to growth factor stimulation in breast cancer cells.
DC40155	Zotatifin	Zotatifin (eFT226) is a potent, selective, and well-tolerated eIF4A inhibitor. Zotatifin promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5’-UTRs (IC50=2 nM) and interferes with the assembly of the eIF4F initiation complex. Zotatifin shows robust antiviral effects, it effectively reduces viral infectivity by inhibiting SARS-CoV-2 NP protein biogenesis (IC90=37 nM). Zotatifin induces cell apoptosis.
DC39087	GCN2iB	GCN2iB is an ATP-competitive serine/threonine-protein kinase general control nonderepressible 2 (GCN2) inhibitor with IC50 of 2.4 nM.
DC28590	CMLD012073	CMLD012073 is an amidino-rocaglates and is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. CMLD012073 against NIH/3T3 cells with an IC50 of 10 nM. CMLD012073 inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase (eIF4A).
DC28589	CMLD012072	CMLD012072 is an amidino-rocaglates and is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. CMLD012072 can induce RNA clamping of eIF4A1 and eIF4A2 and possess potent anti-neoplastic activity.
DC28588	CMLD012612	CMLD012612 is an amidino-rocaglate containing a hydroxamate group and is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. CMLD012612 inhibits cell translation and is cytotoxic to NIH/3T3 cells with an IC50 value of 2 nM. CMLD012612 inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase (eIF4A) and possesses potent anti-neoplastic activity.