A potent inhibitor of HDAC6 (IC50 = 0.40 nM); selective for HDAC6 over HDAC3 (IC50 = 51.61 nM); induces α-tubulin acetylation

WT161 – 10 mg

Brand:
Cayman
CAS:
1206731-57-8
Storage:
-20
UN-No:
Non-Hazardous - /

WT161 is a potent inhibitor of HDAC6 with an IC50 value of 0.40 nM.{32615} It is selective for HDAC6 over HDAC3 (IC50 = 51.61 nM) and induces α-tubulin acetylation, an HDAC6-dependent process, with minimal effect on global lysine acetylation. WT161 inhibits growth of patient-derived multiple myeloma cell lines with IC50 values ranging from 1.5 to 4.7 μM. WT161 enhances the cytotoxicity of bortezomib (Item No. 10008822) and carfilzomib (Item No. 17554) against patient-derived multiple myeloma cells. It also decreases tumor size in a human MM.1S multiple myeloma mouse xenograft model when administered in combination with bortezomib at doses of 50 and 0.5 mg/kg, respectively.  

 

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Description

A potent inhibitor of HDAC6 (IC50 = 0.40 nM); selective for HDAC6 over HDAC3 (IC50 = 51.61 nM); induces α-tubulin acetylation, an HDAC6-dependent process, with minimal effect on global lysine acetylation; inhibits growth of patient-derived multiple myeloma cell lines (IC50s = 1.5-4.7 μM); enhances cytotoxicity of bortezomib and carfilzomib against patient-derived multiple myeloma cells; decreases tumor size in a human MM.1S multiple myeloma mouse xenograft model when administered in combination with bortezomib at doses of 50 and 0.5 mg/kg, respectively

Formal name: 8-(hydroxyamino)-8-oxo-octanoic acid, 2-[[4-(diphenylamino)phenyl]methylene]hydrazide

Synonyms: 

Molecular weight: 458.6

CAS: 1206731-57-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Deacetylases||Research Area

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