Description
IACS-9571 (ASIS-P040) hydrochloride is a potent and selective inhibitor of TRIM24 and BRPF1, with an IC50 of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively.
Product information
CAS Number: 2319611-93-1
Molecular Weight: 679.22
Formula: C32H43ClN4O8S
Synonym:
ASIS-P040 hydrochloride
Chemical Name: N-(6-{3-[4-(dimethylamino)butoxy]-5-propoxyphenoxy}-1,3-dimethyl-2-oxo-2,3-dihydro-1H-1,3-benzodiazol-5-yl)-3,4-dimethoxybenzene-1-sulfonamide; chlorohydrogen
Smiles: Cl.CN(C)CCCCOC1C=C(C=C(C=1)OC1C=C2C(=CC=1NS(=O)(=O)C1C=C(OC)C(=CC=1)OC)N(C)C(=O)N2C)OCCC
InChiKey: MOYQIQKWUIYJMN-UHFFFAOYSA-N
InChi: InChI=1S/C32H42N4O8S.ClH/c1-8-14-42-22-16-23(43-15-10-9-13-34(2)3)18-24(17-22)44-30-21-28-27(35(4)32(37)36(28)5)20-26(30)33-45(38,39)25-11-12-29(40-6)31(19-25)41-7;/h11-12,16-21,33H,8-10,13-15H2,1-7H3;1H
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 125 mg/mL (184.03 mM; Need ultrasonic and warming). H2O : 10 mg/mL (14.72 mM; Need ultrasonic).
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:
IACS-9571 Hydrochloride shows excellent cellular potency with EC50 of 50 nM. IACS-9571 Hydrochloride (1 μM) has potent activities against a panel of 32 bromodomains. IACS-9571 Hydrochloride is a selective dual TRIM24/BRPF1 inhibitor (Kd=1.3/2.1 nM) with 9- and 21-fold selectivity against BRPF2 and BRPF3, respectively. IACS-9571 Hydrochloride does not interact with the BET sub-family of bromodomains, displaying greater than 7700-fold selectivity versus BRD4 (1, 2) relative to TRIM24.
References:
- Palmer WS, et al. Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor. J Med Chem. 2016 Feb 25;59(4):1440-54.
Products are for research use only. Not for human use.
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