HDAC/Top-IN-1
HDAC/Top-IN-1 is an orally active and pan HDAC/Top dual inhibitor with IC50s of 0.036 μM, 0.14 μM, 0.059 μM, 0.089 μM and 9.8 μM for HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8. HDAC/Top-IN-1 efficiently induces apoptosis with S cell-cycle arrest in HEL cells. HDAC/Top-IN-1 has exhibits excellent in vivo antitumor efficacy[1].
Product Specifications
CAS Number
2411379-14-9
UNSPSC
12352005
Target
HDAC; Topoisomerase
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/hdac-top-in-1.html
Solubility
10 mM in DMSO
Smiles
O=C1C2=C(N(C3N1CCC4=C3NC5=CC=C(OCC6=CC=C(C=C6)/C=C/C(NO)=O)C=C45)C)C=CC(F)=C2
Molecular Formula
C29H25FN4O4
Molecular Weight
512.53
References & Citations
[1]Wu S, Huang Y, Wang T, et al. Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. J Med Chem. 2022;65 (6) :4818-4831.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
HDAC1; HDAC2; HDAC3; HDAC6; HDAC8
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