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
Frequently Asked Questions
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