WT-161

SKU: orb1226799

Description

A potent, selective, and bioavailable HDAC6 inhibitor with IC50 0.4 nM; displays >20-fold selectivity over HDAC1/2/3/8; selectively inhibits HDAC6 and dramatically increases levels of acetylated α-tubulin with little effect on global lysine acetylation in cells; reversibly and rapidly induces the accumulation of Ac-α-tubulin in MM cell lines, displays synergism with both BTZ and CFZ, caspase activation and apoptosis; demonstrates a significant antitumor effect in human MM cell xenograft mouse model combined with BTZ.

Key Properties

• CAS Number: 1206731-57-8
• MW: 458.55
• Purity: >98% (HPLC)
• Formula: C₂₇H₃₀N₄O₃
• SMILES: O=C(NO)CCCCCCC(N/N=C/C1=CC=C(N(C2=CC=CC=C2)C3=CC=CC=C3)C=C1)=O
• Target: HDAC
• Solubility: DMSO : ≥ 100 mg/mL 218.08 mM

Bioactivity

• 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.
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

WT 161 | WT161

Quick Database Links

Gene Symbol

HDAC