Description
WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines.
Product information
CAS Number: 2408842-51-1
Molecular Weight: 514.59
Formula: C30H31FN4O3
Chemical Name: 2-[(3,5-dimethoxyphenyl)methyl]-5-(4-fluoro-2-methylphenyl)-7-[(2-imino-3-methyl-2,3-dihydro-1H-imidazol-1-yl)methyl]-1,2,3,4-tetrahydroisoquinolin-1-one
Smiles: CN1C=CN(CC2=CC3C(=O)N(CC4C=C(C=C(C=4)OC)OC)CCC=3C(=C2)C2=CC=C(F)C=C2C)C1=N
InChiKey: PKONCIPMLLIAIL-UHFFFAOYSA-N
InChi: InChI=1S/C30H31FN4O3/c1-19-11-22(31)5-6-25(19)27-14-21(18-35-10-9-33(2)30(35)32)15-28-26(27)7-8-34(29(28)36)17-20-12-23(37-3)16-24(13-20)38-4/h5-6,9-16,32H,7-8,17-18H2,1-4H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
WDR5-IN-1 (1 µM; 48 hours) shows an apparent decrease in G2M phase cells. WDR5-IN-1 (0.01-3 µM; 24-48 hours) increases p53 and p21 protein levels.WDR5-IN-1 shows anti-proliferative activity in MYC-driven cancers (CHP-134, Ramos, Raji, Daudi, SW620, SW480 cells), with GI50s ranging from 0.26-3.2 µM.
Products are for research use only. Not for human use.
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