An HDAC6 inhibitor (IC50 = 2.6 nM); selective for HDAC6 over HDAC1-3

ACY-241 – 5 mg

Brand:
Cayman
CAS:
1316215-12-9
Storage:
-20
UN-No:
Non-Hazardous - /

ACY-241 is an inhibitor of histone deacetylase 6 (HDAC6; IC50 = 2.6 nM).{47143} It is selective for HDAC6 over HDAC1-3, HDAC7, and HDAC9 (IC50s = 35, 45, 46, 7,300, and 137 nM, respectively), as well as HDAC4, HDAC5, and HDAC9 (IC50 = >20,000 nM for all). It reduces proliferation of A2780, TOV-21G, and MDA-MB-231 cells when used at a concentration of 3 µM and completely inhibits it and induces apoptosis at a concentration of 10 µM. ACY-241, when used in combination with paclitaxel (Item No. 10461), inhibits proliferation in MiaPaCa-2, TOV-21G, and T47D cells. It also reduces tumor growth in a MiaPaCa-2 mouse xenograft model when administered at a dose of 50 mg/kg in combination with paclitaxel. ACY-241, in combination with the somatostatin receptor agonist pasireotide (Item No. 24092), reduces hepatorenal cystogenesis in a rat model of polycystic liver disease.{47144}  

 

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SKU: 26173 - 5 mg Category:

Description

An HDAC6 inhibitor (IC50 = 2.6 nM); selective for HDAC6 over HDAC1-3, HDAC7, and HDAC9 (IC50s = 35, 45, 46, 7,300, and 137 nM, respectively), as well as HDAC4, HDAC5, and HDAC9 (IC50 = >20,000 nM for all); reduces proliferation of A2780, TOV-21G, and MDA-MB-231 cells at 3 µM and completely inhibits it and induces apoptosis at 10 µM; inhibits proliferation in MiaPaCa-2, TOV-21G, and T47D cells when used in combination with paclitaxel; reduces tumor growth in a MiaPaCa-2 mouse xenograft model at 50 mg/kg when used in combination with paclitaxel; reduces hepatorenal cystogenesis in a rat model of polycystic liver disease when used in combination with pasireotide

Formal name: 2-[(2-chlorophenyl)phenylamino]-N-[7-(hydroxyamino)-7-oxoheptyl]-5-pyrimidinecarboxamide

Synonyms:  Citarinostat

Molecular weight: 468

CAS: 1316215-12-9

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Deacetylases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Epigenetics, Transcription, & Translation|Erasers|Histone Deacetylation

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