SW2_110A is a selective chromobox 8 chromodomain (CBX8 ChD) inhibitor with a Kd of 800 nM. SW2_110A shows minimal 5-fold selectivity for CBX8 ChD over all other CBX paralogs in vitro.

Product information

Molecular Weight: 760.96

Formula: C42H60N6O7

Chemical Name: (2S)-2-[(2R,3S)-2-[(2S)-2-cyclopentyl-2-[(4-phenoxyphenyl)formamido]acetamido]-3-methylpentanamido]-6-(diethylamino)-N-[(1S)-2-hydroxy-1-[(prop-2-yn-1-yl)carbamoyl]ethyl]hexanamide

Smiles: C[C@@H](CC)[C@@H](NC(=O)[C@@H](NC(=O)C1=CC=C(C=C1)OC1=CC=CC=C1)C1CCCC1)C(=O)N[C@@H](CCCCN(CC)CC)C(=O)N[C@@H](CO)C(=O)NCC#C

InChiKey: HEDLPSLAOJYDMT-GUKRFWIHSA-N

InChi: InChI=1S/C42H60N6O7/c1-6-26-43-39(51)35(28-49)45-40(52)34(21-15-16-27-48(8-3)9-4)44-41(53)36(29(5)7-2)46-42(54)37(30-17-13-14-18-30)47-38(50)31-22-24-33(25-23-31)55-32-19-11-10-12-20-32/h1,10-12,19-20,22-25,29-30,34-37,49H,7-9,13-18,21,26-28H2,2-5H3,(H,43,51)(H,44,53)(H,45,52)(H,46,54)(H,47,50)/t29-,34-,35-,36+,37-/m0/s1

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : 125 mg/mL (164.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO).

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:

SW2_110A specifically inhibits the association of CBX8 with chromatin in cells and inhibits the proliferation of THP1 leukemia cells driven by the MLL-AF9 translocation (IC50 of 26 µM). In THP1 cells, SW2_110A treatment results in a significant decrease in the expression of MLL-AF9 target genes, including HOXA9.

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