CBL0137 hydrochloride

SKU: orb1302919

Description

CBL0137 hydrochloride (Curaxin-137 hydrochloride) is a FACT complex inhibitor that activates p53 and suppresses NF-κB, demonstrating potent anticancer activity in vitro and in vivo. It synergizes with chemotherapeutics like cisplatin, showing efficacy in preclinical models of small cell lung cancer (SCLC) and other malignancies.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1197397-89-9
• MW: 372.88
• Purity: 99.86%
• Formula: C₂₁H₂₅ClN₂O₂
• SMILES: Cl.CC(C)NCCn1c2ccc(cc2c2cc(ccc12)C(C)=O)C(C)=O
• Target: MDM-2/p53,NF-κB,p53
• Solubility: DMSO:36 mg/mL (96.55 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:25 mg/mL (67.05 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.36 mM)

Bioactivity

• Target IC50:
  NF-κB:0.47 μM(EC50)|p53:0.37 μM(EC50)|FACT:
• In Vivo:
  METHODS: ApoE−/− mice were treated with CBL0137 hydrochloride (Curaxin-137 hydrochloride) (1 mg/kg, oral, for three weeks) to observe the effects of CBL0137 hydrochloride (Curaxin-137 hydrochloride) on the atherosclerosis mouse model and perform Western blot experiments. RESULTSCBL0137 hydrochloride (Curaxin-137 hydrochloride) can reduce the formation of atherosclerotic plaques in partially ligated carotid arteries;CBL0137 hydrochloride (Curaxin-137 hydrochloride) treatment downregulated the protein levels of p-YAP (Y357) and p-Src (Y416) in these arteries, as well as the inflammatory genes MCP-1 and VCAM-1.
• In Vitro:
  METHODS: HUVECs and HAECs cell treated with CBL0137 hydrochloride (Curaxin-137 hydrochloride) (0, 1, 3, 10 μM, 24 h) were tested for cell viability using the CCK-8 assay kit. RESULTS CBL0137 hydrochloride (Curaxin-137 hydrochloride) above 1 μM reduced the survival rate of HUVECs and HAECs.
• Cell Research:
  Effects of CBLC137 (2 μM for 24 hours) on cell cycle in tumor (HT1080, RCC45, MiaPaca) and normal cells (Wi38, NKE-hTERT) are examined using FACS analysis of propidium iodide-stained cells.
• Animal Research:
  Animal Models: xenograft mouse models of cancer. Formulation: water. Dosages: 30 mg/kg. Administration: p.o.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Curaxin 137, Curaxin 137 hydrochloride, Curaxin137, Curaxin-137, Curaxin-137 hydrochloride, CBL-0137, CBLC 137, CBL-C 137 Hydrochloride, CBLC137, CBL-C137, CBLC-137, CBLC137 hydrochloride, CBL-C137 hydrochloride, CBL-C-137 Hydrochloride, CBL 0137, CBL 0137 Hydrochloride, NF-κB, NFκB, NFkB, NF-kB, p53, FACT, MDM-2/p53

Compound Identifiers

PubChem CID

44519123