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CBL0137 hydrochloride

Catalog No. T4361 CAS 1197397-89-9

Synonyms: CBL0137, CBLC137, Curaxin 137, CBL-C137 hydrochloride, Curaxin-137 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.

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CBL0137 hydrochloride Chemical Structure

CBL0137 hydrochloride, CAS 1197397-89-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 43.00
2 mg	In stock	$ 61.00
5 mg	In stock	$ 131.00
10 mg	In stock	$ 227.00
25 mg	In stock	$ 491.00
50 mg	In stock	$ 716.00
100 mg	In stock	$ 945.00
1 mL * 10 mM (in DMSO)	In stock	$ 108.00

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Purity: 99.35%

Purity: 98.59%

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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.

Synonyms	CBL0137, CBLC137, Curaxin 137, CBL-C137 hydrochloride, Curaxin-137 hydrochloride
Molecular Weight	372.88
Formula	C21H25ClN2O2
CAS No.	1197397-89-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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)

References and Literature

1. Gasparian AV,etal.Curaxins: anticancer compounds that simultaneously suppress NF-κB and activate p53 by targeting FACT.Sci Transl Med. 2011 Aug 10;3(95):95ra74. 2. Burkhart C,etal.Curaxin CBL20137 eradicates drug resistant cancer stem cells and potentiates efficacy of gemcitabine in preClinicalal models of pancreatic cancer.Oncotarget. 2014 Nov 30;5(22):11038-53. 3. Barone TA,etal.Anticancer drug candidate CBL20137, which inhibits histone chaperone FACT, is efficacious in preClinicalal orthotopic models of temozolomide-responsive and -resistant glioblastoma.Neuro Oncol. 2017 Feb 1;19(2):186-196.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library Inhibitor Library Anti-Breast Cancer Compound Library Bioactive Compounds Library Max Autophagy Compound Library Anti-Pancreatic Cancer Compound Library Ubiquitination Compound Library

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Keywords

CBL0137 hydrochloride 1197397-89-9 Apoptosis NF-Κb Others NF-κB p53 Curaxin-137 Nuclear factor-κB CBL-C 137 Hydrochloride CBL0137 inhibit CBL0137 Hydrochloride Inhibitor CBL-0137 Hydrochloride Curaxin137 CBL-C137 CBLC137 CBL 0137 Nuclear factor-kappaB Curaxin 137 CBLC 137 MDM-2/p53 CBL-0137 CBL-C137 hydrochloride CBL-0137 hydrochloride Curaxin-137 Hydrochloride CBL-C-137 Hydrochloride CBL-C137 Hydrochloride CBLC-137 Curaxin-137 hydrochloride CBL 0137 Hydrochloride inhibitor

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