| Name | CBL0137 hydrochloride |
| Description | CBL0137 hydrochloride (Curaxin-137 hydrochloride) is an inhibitor of the histone chaperone FACT, which also activates p53 and inhibits NF-κB with EC50 values of 0.37 and 0.47 μM, respectively. CBL0137 hydrochloride functionally inactivates the complex that promotes chromatin transcription (FACT), thereby driving effects on p53 and NF-κB and promoting cancer cell death, and when used in combination with cisplatin, CBL0137 hydrochloride has potent anticancer activity against SCLC. |
| 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. |
| Kinase Assay | MiaPaca2 and BxPC-3 cells are treated with CBL0137 hydrochloride for 4 or 24 h. Cells are harvested in 1× Cell Culture Lysis Reagent containing protease and phosphatase inhibitors. Lysates 5 to 20 μg are separated on SDS-PAGE gels and transferred to PVDF membranes. Blots are probed with antibodies specific for SSRP1, SPT16, RRM1, and RRM2. |
| Animal Research | Animal Models: xenograft mouse models of cancer. Formulation: water. Dosages: 30 mg/kg. Administration: p.o. |
| 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. [1] |
| 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. [1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | Ethanol : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.36 mM), Sonication is recommended.
H2O : 25 mg/mL (67.05 mM), Sonication is recommended.
DMSO : 36 mg/mL (96.55 mM), Sonication is recommended.
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| Keywords | p53 | NF-κB | NFκB | NF-kB | NFkB | MDM-2/p53 | FACT | Curaxin-137 | Curaxin137 | Curaxin 137 | CBL-C-137 Hydrochloride | CBLC-137 | CBL-C137 | CBLC137 | CBL-C 137 Hydrochloride | CBLC 137 | CBL-0137 | CBL 0137 Hydrochloride | CBL 0137 |
| Inhibitors Related | Undecane | Flubendazole | Sodium propionate | Ethyl palmitate | Kojic acid | Uridine | Fumaric acid | 1,4-Naphthoquinone | Glucosamine | Ethyl linoleate | N,N-Dimethylacetamide | Magnesium sulfate |
| Related Compound Libraries | Anti-Colorectal Cancer Compound Library | Failed Clinical Trials Compound Library | Bioactive Compound Library | Anti-Ovarian Cancer Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Aging Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
