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CBL0137 hydrochloride

🥰Excellent
Catalog No. T4361Cas No. 1197397-89-9
Alias Curaxin-137 hydrochloride, Curaxin 137 hydrochloride, CBL-C137 hydrochloride, CBLC137 hydrochloride

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.

CBL0137 hydrochloride

CBL0137 hydrochloride

🥰Excellent
Purity: 99.35%
Catalog No. T4361Alias Curaxin-137 hydrochloride, Curaxin 137 hydrochloride, CBL-C137 hydrochloride, CBLC137 hydrochlorideCas No. 1197397-89-9
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.
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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Purity:99.35%
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Product Introduction

Bioactivity
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.
Targets&IC50
FACT:, p53:0.37 μM(EC50), NF-κB:0.47 μM(EC50)
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]
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.
AliasCuraxin-137 hydrochloride, Curaxin 137 hydrochloride, CBL-C137 hydrochloride, CBLC137 hydrochloride
Chemical Properties
Molecular Weight372.88
FormulaC21H25ClN2O2
Cas No.1197397-89-9
SmilesCl.CC(C)NCCn1c2ccc(cc2c2cc(ccc12)C(C)=O)C(C)=O
Relative Density.no data available
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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