CBL0137 (hydrochloride)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
EC50: 0.37 μM for activating p53; 0.47 μM for inhibiting NF-κB
CBL0137 (hydrochloride) is a curaxin that activates p53 and inhibits NF-κB.
The p53 and nuclear factor κB (NF-κB) pathways are dysregulated in almost all tumors, making them attractive targets for therapeutic activation and inhibition, respectively.
In vitro: CBL0137 was identified as a metabolically stable curaxin activating p53 and inhibiting NF-κB. CBL0137 could functionally inactivate chromatin transcription complex, resulting in the effects on p53 and NF-κB and promoting cancer cell death [1]. It was also found that CBL0137 alone was a potent inducer of apoptosis in pancreatic cancer cell lines and was toxic not only for proliferating bulk tumor cells, but also for pancreatic cancer stem cells [2].
In vivo: In mice, CBL0137 was effective against orthotopic gemcitabine resistant PANC-1 model and patient derived xenografts, in which CBL0137 anti-tumor effect related with overexpression of FACT. Moreover, the combination effects of CBL0137 and gemcitabine might be explained by the ability of CBL0137 to inhibit several transcriptional programs induced by gemcitabine, including NF-kappaB response and expression of ribonucleotide reductase [2].
Clinical trial: A phase 1 trial of CBL0137 in patients with metastatic or unresectable advanced solid neoplasm and a study of IV CBL0137 in previously treated hematological subjects are crrently recruiting patients [https://clinicaltrials.gov/ct2/results term=CBL0137&Search=Search].
References:
1. A. V. Gasparian, C. A. Burkhart, A. A. Purmal, et al. Curaxins: Anticancer compounds that simultaneously suppress NF-κB and activate p53 by targeting FACT. Sci.Transl.Med. 3(95), (2011).
2. C. Burkhart, D. Fleyshman, R. Kohrn, et al. Curaxin CBL0137 eradicates drug resistant cancer stem cells and potentiates efficacy of gemcitabine in preclinical models of pancreatic cancer. Oncotarget 5(22), 11038-11053 (2014).
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 372.9 |
Cas No. | 1197397-89-9 |
Formula | C21H24N2O2·HCl |
Synonyms | CBLC137, Curaxin 137 |
Solubility | insoluble in EtOH; ≥15.47 mg/mL in H2O; ≥19.95 mg/mL in DMSO |
Chemical Name | 1,1'-[9-[2-[(1-methylethyl)imino]ethyl]-9H-carbazole-3,6-diyl]bis-ethanone, monohydrochloride |
SDF | Download SDF |
Canonical SMILES | CC(C1=CC=C2C(C(C=C(C(C)=O)C=C3)=C3N2CCNC(C)C)=C1)=O.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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