BG-45

SKU: orb1223630

Description

A potent and selective HDAC3 inhibitor with IC50 of 289 nM; shows selectivity over HDAC1 and HDAC2; downregulates phosphorylation (Tyr705 and Ser727) of STAT3 and triggers hyperacetylation of STAT3 in MM cells; significantly enhances bortezomib-induced cytotoxicity; exhibits significant tumor growth inhibition in vivo in a murine xenograft model of human MM.

Key Properties

• CAS Number: 926259-99-6
• MW: 214.2233
• Purity: >98% (HPLC)
• Formula: C₁₁H₁₀N₄O
• SMILES: O=C(C1=NC=CN=C1)NC2=CC=CC=C2N
• Target: HDAC
• Solubility: DMSO: ≥ 48 mg/mL

Bioactivity

• In Vivo:
  BG45 (15-50 mg/kg; i.p.; 5 days a week for 3 weeks; CB17 SCID mice with MM. 1S xenograft model) inhibits human multiple myeloma (MM) cells growth and enhances bortezomib (HY-10227) induced cytotoxicity In vivo. Animal model: CB17 SCID mice (48-54 days old) with MM. 1S xenograft model. Dosage: 15 and 50 mg/kg. Administration: Intraperitoneal injection; 5 days a week for 3 weeks. Result: Inhibited MM tumor growth in a dose-dependent fashion. Enhanced either single agent activity in combination with bortezomib (HY-10227).
• In Vitro:
  BG45 (1.875-30 μM; 48 and 72 h) targets multiple myeloma (MM) cells and inhibits cell growth in a dose-dependent manner. BG45 (15 μM; 0-48 h; MM.1S cells) induces apoptosis via caspase-3/PARP cleavage. BG45 (10 and 20 μM; 12 h; MM.1S cells) induces acetylation of histone H2A, H3, and H4 in a dose-dependent manner. BG45 (10 and 20 μM; 10 h; MM.1S cells) induces multiple myeloma (MM) cells toxicity is associated with hyperacetylation of histones and STAT3 and downregulation of p-STAT3.Cell Viability Assay Cell line: MM.1S, RPMI8226, U266, OPM1, and H929 cells Concentration: 1.875, 3.75, 7.5, 15, and 30 μM Incubation time: 48 and 72 hours. Result: Inhibited multiple myeloma (MM) cells growth in a dose-dependent manner. Western blot analysis. Cell line: MM.1S cells Concentration: 15 μM. Incubation time: 0, 6, 12, 24, and 48 hours. Result: Induced caspase-dependent apoptosis in multiple myeloma (MM) cells. Western blot analysis. Cell line: MM.1S cells Concentration: 10 and 20 μM. Incubation time: 12 hours. Result: Increased acetylation of histone in a dose-dependent manner. Western blot analysis. Cell line: MM.1S cells Concentration: 10 and 20 μM. Incubation time: 10 hours. Result: Downregulated p-STAT3 in a dose-dependent manner. Increased acetylation of STAT3 in MM.1S cells.

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

BG45

Quick Database Links

Gene Symbol

HDAC