WDR5-0103, WDR5 Inhibitor


Catalog No. size PriceQuantity
M60233-2S 2 mg solid $89
M60233-10S 10mg solid $352

Description

WDR5-0103 is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with Kd of 450 nM. It has no effect on a panel of seven other methyltransferases, including SETD7. It binds in the WDR5 peptide-binding pocket and inhibits the catalytic activity of the MLL core complex in vitro. WDR5-0103 is a good chemical probe to demonstrate inhibition of an important protein-protein interaction and form the basis for further development of inhibitors of WDR5-dependent enzymes implicated in MLL-rearranged leukaemias or other cancers.

Product information

CAS Number: 890190-22-4

Molecular Weight: 383.44

Formula: C21H25N3O4

Chemical Name: methyl 3-(3-methoxybenzamido)-4-(4-methylpiperazin-1-yl)benzoate

Smiles: CN1CCN(CC1)C1=CC=C(C=C1NC(=O)C1=CC(=CC=C1)OC)C(=O)OC

InChiKey: ZPLBXOVTSNRBFB-UHFFFAOYSA-N

InChi: InChI=1S/C21H25N3O4/c1-23-9-11-24(12-10-23)19-8-7-16(21(26)28-3)14-18(19)22-20(25)15-5-4-6-17(13-15)27-2/h4-8,13-14H,9-12H2,1-3H3,(H,22,25)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Shelf Life: ≥360 days 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:

WDR5-0103 was used at 10 µM final concentration in various in vitro assays.

References:

  1. Senisterra G, et al. Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5. (2013) Biochem J. 449(1):151-9.

Products are for research use only. Not for human use.

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