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Abexinostat

Abexinostat (CRA 024781) is a novel pan-HDAC inhibitor mostly targeting HDAC1 with Ki of 7 nM. Abexinostat also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2) hydrolase activity with an EC50 below 10 nM[1][4].

Product Specifications

CAS Number

[783355-60-2]

Product Name Alternative

CRA 024781; PCI-24781

UNSPSC

12352005

Hazard Statement

H302, H312, H332

Target

HDAC

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/PCI-24781.html

Purity

99.00

Solubility

DMSO : 3.33 mg/mL (ultrasonic)

Smiles

O=C(NCCOC1=CC=C(C=C1)C(NO)=O)C2=C(C3=CC=CC=C3O2)CN(C)C

Molecular Formula

C21H23N3O5

Molecular Weight

397.42

Precautions

H302, H312, H332

References & Citations

[1]Buggy JJ, et al. CRA-024781: a novel synthetic inhibitor of histone deacetylase enzymes with antitumor activity in vitro and in vivo. Mol Cancer Ther, 2006, 5 (5), 1309-1317.|[2]Adimoolam S, et al. HDAC inhibitor PCI-24781 decreases RAD51 expression and inhibits homologous recombination. Proc Natl Acad Sci U S A, 2007, 104 (49), 19482-19487.|[3]Lopez G, et al. Combining PCI-24781, a novel histone deacetylase inhibitor, with chemotherapy for the treatment of soft tissue sarcoma. Clin Cancer Res, 2009, 15 (10), 3472-3483.|[4]Lechner S, et al. Target deconvolution of HDAC pharmacopoeia reveals MBLAC2 as common off-target. Nat Chem Biol. 2022 Aug;18 (8) :812-820.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 3

Isoform

HDAC1; HDAC10; HDAC2; HDAC3; HDAC6; HDAC8

Available Sizes

Curated Selection

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