UF-010

SKU: orb1224758

Description

A potent and selective inhibitor of class I HDACs with IC50s of 0.5/0.1/0.06/1.5/9.1/15.3/44.5 uM for HDAC1/2/3/8/6/10/11 respectively; shows no effect on HDAC4/5/7/9(>100 uM); induces the accumulation of protein acetylation and inhibits proliferation of NCI-60 panel of cancer cell lines (mean GI50=2.94 uM); a competitive with a fast-on/slow-off HDAC-binding mechanism.

Key Properties

• CAS Number: 537672-41-6
• MW: 271.1536
• Purity: >98% (HPLC)
• Formula: C₁₁H₁₅BrN₂O
• SMILES: O=C(NNCCCC)C1=CC=C(Br)C=C1
• Target: HDAC
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Animal model: postoperative cognitive dysfunction (POCD) mice. Dosage: 15 mg/kg. Administration: Intraperitoneal injection (i.p.). Result: Weakened the infiltration of CD4+ T cells and NK cells in hippocampal tissues. Reduced inflammatory parameters in serum and hippocampal tissues, such as interleukin 6 (IL-6), C-reactive protein (CRP), and tumor necrosis factor alpha (TNF-α) levels. Activated the NF-κB/p65, JAK/STAT and TLR/MyD88 pathways. Animal model: 4T1-Luc tumor-bearing mouse model. Dosage: 15 mg/kg. Administration: Intraperitoneal injection (i.p.). Result: Inhibited the tumor growth rate percentage to 55.56, 38.36, 39.52% at days 7, 14, and 21.Induced high levels of ROS generation, causing apoptosis-mediated tumor cell death.
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• In Vitro:
  Cell Cytotoxicity Assay Cell line: B16F10 cells, MCF-7 cells, A549 cells, 4T1 cells, HEK-293 cells and HCEC cells. Concentration: 10 μM, 100 μM. Incubation time: 72 h. Result: Showed IC50 values of 2.41 μM for B16F10 cells, 20.81 μM for A549 cells, 17.93 μM for MCF-7 cells, 8.40 μM for 4T1 cells, 98.52 μM for HEK-293 cells, 95.4 μM for HCEC cells.
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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

UF010 | UF 010

Quick Database Links

Gene Symbol

HDAC