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CBL0137 hydrochloride

CBL0137 hydrochloride
CBL0137 hydrochloride (Curaxin-137 hydrochloride) activates p53 and inhibits NF-kB (EC50: 0.37/0.47 μM) in the cell-based p53 and NF-kB reporter assays, respectively. It also suppresses histone chaperone FACT.
Catalog No. T4361Cas No. 1197397-89-9
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Purity:99.35%
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CBL0137 hydrochloride

Catalog No. T4361Cas No. 1197397-89-9
CBL0137 hydrochloride (Curaxin-137 hydrochloride) activates p53 and inhibits NF-kB (EC50: 0.37/0.47 μM) in the cell-based p53 and NF-kB reporter assays, respectively. It also suppresses histone chaperone FACT.
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Pack SizePriceAvailabilityQuantity
1 mg$43In Stock
5 mg$131In Stock
10 mg$217In Stock
25 mg$436In Stock
50 mg$591In Stock
100 mg$787In Stock
1 mL x 10 mM (in DMSO)$108In Stock
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Product Introduction

Bioactivity
Description
CBL0137 hydrochloride (Curaxin-137 hydrochloride) activates p53 and inhibits NF-kB (EC50: 0.37/0.47 μM) in the cell-based p53 and NF-kB reporter assays, respectively. It also suppresses histone chaperone FACT.
Targets&IC50
NF-κB:0.47 μM(EC50), p53:0.37 μM(EC50), FACT:
In vitro
In pancreatic cancer cell lines, CBL0137 is an effective inducer of apoptosis. It is toxic not only for proliferating various tumor cells, but also for pancreatic cancer stem cells. CBL0137 can activate p53 and inhibit cellular stress pathways mediated by HSF-1 and NF-κB. CBL0137 binds DNA but does not cause any sort of chemical modifications in DNA. However, CBL0137 binding to DNA leads to functional inactivation of the Facilitates Chromatin Transcription (FACT) complex. In CBL0137-treated cells, FACT is lost from the nucleoplasm and trapped in chromatin, resulting in the inhibition of FACT-dependent transcription, including NF-kB-mediated transcription. Additionally, chromatin trapping of FACT leads to casein kinase 2 (CK2)-dependent phosphorylation and activation of p53.
In vivo
In mice, CBL0137 is potent against several Pancreatic ductal adenocarcinoma (PDA) models, including patient derived xenografts and orthotopic gemcitabine resistant PANC-1 model. CBL0137 targets glioblastoma (GBM) according to its proposed mechanism of action, crosses the blood-brain barrier, and is efficacious in both TMZ-responsive and -resistant orthotopic models. The property of crossing the blood-brain barrier, especially when administered i.v, bodes well for the potential of this drug to treat CNS tumors. In orthotopic models, i.v. administration leads to greater tumor tissue accumulation than oral dosing, leading to greater bioavailability.
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.
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.
AliasCBL0137, CBLC137, Curaxin 137, CBL-C137 hydrochloride, Curaxin-137 hydrochloride
Chemical Properties
Molecular Weight372.88
FormulaC21H25ClN2O2
Cas No.1197397-89-9
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: 25 mg/mL (67.05 mM), Sonication is recommended.
DMSO: 36 mg/mL (96.5 mM)
Solution Preparation Table
H2O/DMSO
1mg5mg10mg50mg
1 mM2.6818 mL13.4091 mL26.8183 mL134.0914 mL
5 mM0.5364 mL2.6818 mL5.3637 mL26.8183 mL
10 mM0.2682 mL1.3409 mL2.6818 mL13.4091 mL
20 mM0.1341 mL0.6705 mL1.3409 mL6.7046 mL
50 mM0.0536 mL0.2682 mL0.5364 mL2.6818 mL

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