2. Epigenetics
  3. Epigenetic Reader Domain
  4. IACS-9571

IACS-9571 is a potent and selective inhibitor of TRIM24 and BRPF1, with IC50 of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (IACS-9571 hydrochloride) usually boasts enhanced water solubility and stability.

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IACS-9571 Chemical Structure

IACS-9571 Chemical Structure

CAS No. : 1800477-30-8

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IACS-9571 Related Antibodies

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Description

IACS-9571 is a potent and selective inhibitor of TRIM24 and BRPF1, with IC50 of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively.

IC50 & Target

IC50: 8 nM (TRIM24)[1]
Kd: 31 nM (TRIM24), 14 nM (BRPF1)[1]
Cellular Effect
Cell Line Type Value Description References
CWR22R IC50
10.82 μM
Compound: IACS-9571
Antiproliferative activity against human 22Rv1 cells measured after 96 hrs by Cell Titer-Glo assay
Antiproliferative activity against human 22Rv1 cells measured after 96 hrs by Cell Titer-Glo assay
[PMID: 35385803]
HeLa EC50
0.05 μM
Compound: 8i; IACS-9571
Inhibition of Flag-tagged TRIM24-PHD/bromodomain (unknown origin) expressed in human HeLa cells for 2 hrs by AlphaLisa assay
Inhibition of Flag-tagged TRIM24-PHD/bromodomain (unknown origin) expressed in human HeLa cells for 2 hrs by AlphaLisa assay
[PMID: 26061247]
LNCaP IC50
12.15 μM
Compound: IACS-9571
Antiproliferative activity against human LNCaP cells measured after 96 hrs by Cell Titer-Glo assay
Antiproliferative activity against human LNCaP cells measured after 96 hrs by Cell Titer-Glo assay
[PMID: 35385803]
LNCaP C4-2B IC50
13.63 μM
Compound: IACS-9571
Antiproliferative activity against human LNCaP C4-2B cells measured after 96 hrs by Cell Titer-Glo assay
Antiproliferative activity against human LNCaP C4-2B cells measured after 96 hrs by Cell Titer-Glo assay
[PMID: 35385803]
In Vitro

IACS-9571 shows excellent cellular potency with EC50 of 50 nM. IACS-9571 (1 μM) has potent activities against a panel of 32 bromodomains. IACS-9571 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 does not interact with the BET sub-family of bromodomains, displaying greater than 7,700-fold selectivity versus BRD4(1, 2) relative to TRIM24[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

IACS-9571 Related Antibodies
Molecular Weight

642.76

Formula

C32H42N4O8S
CAS No.
SMILES

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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IACS-9571 Related Classifications

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This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

IACS-95711800477-30-8ASIS-P040IACS9571IACS 9571Epigenetic Reader DomainInhibitorinhibitorinhibit

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