WT-161

Modify Date: 2024-02-28 09:03:04

WT-161 Structure
WT-161 structure
Common Name WT-161
CAS Number 1206731-57-8 Molecular Weight 458.552
Density 1.2±0.1 g/cm3 Boiling Point N/A
Molecular Formula C27H30N4O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of WT-161


WT-161 is a potent and selective HDAC6 inhibitor with an IC50 of 0.40 nM.

 Names

Name WT-161
Synonym More Synonyms

 WT-161 Biological Activity

Description WT-161 is a potent and selective HDAC6 inhibitor with an IC50 of 0.40 nM.
Related Catalog
Target

HDAC6:0.4 nM (IC50)

HDAC1:8.35 nM (IC50)

HDAC2:15.4 nM (IC50)

HDAC3:51.6 nM (IC50)

HDAC8:1430 nM (IC50)

In Vitro WT161 selectively inhibits HDAC6 and dramatically increases levels of acetylated α-tubulin (Ac-α-tubulin) with little effect on global lysine acetylation. WT161 induces significant toxicity in all multiple myeloma cell lines tested, with IC50s between 1.5 and 4.7 µM . WT161 in combination with bortezomib triggers significant accumulation of polyubiquitinated proteins and cell stress, followed by caspase activation and apoptosis. More importantly, this combination treatment is effective in bortezomib-resistant cells and in the presence of bone marrow stromal cells, which have been shown to mediate multiple myeloma cell drug resistance[1].
In Vivo WT161 shows toxicity at 100 mg/kg i.p., but WT161 is well tolerated at 50 mg/kg i.p.. Bortezomib combined with WT161 demonstrates a significant antitumor effect[1].
Cell Assay MM.1S cells are treated with increasing concentrations of WT161 (0-10 μM) for 48 hours. Cell viability is determined using the MTT assay[1].
Animal Admin Mice: Mice tumor xenograft are assigned into cohorts receiving vehicle (control), BTZ (0.5 mg/kg, i.v.), WT161 (50 mg/kg, i.p.), or BTZ+WT161. WT161 is administered for five consecutive days each week, and BTZ is given on a twice-weekly schedule. Caliper measurements of the longest perpendicular tumor diameters are performed on alternate days to estimate the tumor volume[1].
References

[1]. Hideshima T, et al. Discovery of selective small-molecule HDAC6 inhibitor for overcoming proteasome inhibitor resistance in multiple myeloma. Proc Natl Acad Sci U S A. 2016 Nov 15;113(46):13162-13167.

 Chemical & Physical Properties

Density 1.2±0.1 g/cm3
Molecular Formula C27H30N4O3
Molecular Weight 458.552
Exact Mass 458.231781
LogP 5.34
Index of Refraction 1.594
Storage condition -20℃

 Synonyms

Octanoic acid, 8-(hydroxyamino)-8-oxo-, 2-[(1E)-[4-(diphenylamino)phenyl]methylene]hydrazide
8-{(2E)-2-[4-(Diphenylamino)benzylidene]hydrazino}-N-hydroxy-8-oxooctanamide
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