RasGRP3 ligand 96 |CAS 2229068-13-5|DC Chemicals

Cas No.:	2229068-13-5
Chemical Name:	(E)-(2-(Hydroxymethyl)-4-((1-methyl-1H-indol-3-yl)methylene)-5-oxotetrahydrofuran-2-yl)methyl pivalate
SMILES:	C(OCC(CO)1C/C(=C\C2C3=C(N(C)C=2)C=CC=C3)/C(=O)O1)(=O)C(C)(C)C
Formula:	C₂₁H₂₅NO₅
M.Wt:	371.433
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

RasGRP3 ligand 96 is a potent, selective ligand of Ras guanine-releasing protein 3 (RasGRP3) with Ki of 1.75 nM, showed 73-fold and 45-fold selectivity relative to PKCα and PKCε for in vitro binding activity resepctively; induces Ras activation, a downstream response to RasGRP stimulation, with 8-29 fold selectivity relative to PKCδ S299 phosphorylation in intact cells.

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2018-0101

Cat. No.	Product name	Field of application
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DC70371	DW0254	DW0254 (DW-0254,DW 0254) is a small molecules capable of inhibiting RAS-related C3 botulinum toxin substrate (RAC) small GTPase activation in ALL cell lines, directly binds to the hydrophobic pocket of PDE6D (Kd=436 nM, ITC), a RAS chaperone protein.DW0254 demonstrated dose-dependent RAC inhibition, arrest of proliferation and induced apoptosis in human leukemic cell lines (RS4;11 IC50=1.5-1.8 uM), also showed promising anti-leukemic activity in RAS-mutated cells (CCRF-CEM NRAS G12D, IC50=3.3-4.2 uM).DW0254 disrupted the interaction between PDE6D and RAS, disturbing RAS subcellular localization.DW0254 demonstrated anti-leukemic activity, decreased tumor progression in a murine xenograft model.
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