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IACS-9571 Hydrochloride (ASIS-P040 Hydrochloride) Catalog No.GC34437

Size Price Stock Qty
10mM*1mLinDMSO
$467.00
In stock
1mg
$107.00
In stock
5mg
$312.00
In stock
10mg
$580.00
In stock
50mg
$2,008.00
In stock
100mg
$2,945.00
In stock

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Sample solution is provided at 25 µL, 10mM.

IACS-9571 Hydrochloride (ASIS-P040 Hydrochloride) Dilution Calculator

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IACS-9571 Hydrochloride (ASIS-P040 Hydrochloride) Molarity Calculator

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Chemical Properties

Cas No. N/A SDF Download SDF
Synonyms N/A
Chemical Name N/A
Canonical SMILES [H]Cl.O=S(C1=CC=C(OC)C(OC)=C1)(NC2=C(OC3=CC(OCCC)=CC(OCCCCN(C)C)=C3)C=C(N4C)C(N(C)C4=O)=C2)=O
Formula C32H43ClN4O8S M.Wt 679.22
Solubility DMSO : 125 mg/mL (184.03 mM; Need ultrasonic and warming);H2O : 10 mg/mL (14.72 mM; Need ultrasonic) Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

IACS-9571 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.

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[1].

[1]. 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.