CBL0137 (hydrochloride)
- CAS No.
- 1197397-89-9
- Chemical Name:
- CBL0137 (hydrochloride)
- Synonyms
- CBL0137 HCl;CBL0137(CBL-0137);CBL-C137 hydrochloride;CBL0137 (hydrochloride);Curaxin-137 hydrochloride;CBL0137 HCl (CBL-0137 HCl);1-[6-acetyl-9-[2-(propan-2-ylamino)ethyl]carbazol-3-yl]ethanone,hydrochloride;1,1'-(9-(2-(Isopropylamino)ethyl)-9H-carbazole-3,6-diyl)diethanone hydrochloride;1,1'-(9-(2-(Isopropylamino)ethyl)-9H-carbazole-3,6-diyl)diethanone hydrochloride;CBL0137 hydrochloride,Curaxin-137,Nuclear factor-κB,inhibit,Inhibitor,Curaxin137,CBL-C137,Nuclear factor-kappaB,NF-κB,CBL 0137,MDM-2/p53,CBL-0137,CBL-0137 hydrochloride
- CBNumber:
- CB03152588
- Molecular Formula:
- C21H25ClN2O2
- Molecular Weight:
- 372.89
- MDL Number:
- MOL File:
- 1197397-89-9.mol
- MSDS File:
- SDS
storage temp. | Store at -20°C |
---|---|
solubility | insoluble in EtOH; ≥15.47 mg/mL in H2O; ≥19.95 mg/mL in DMSO |
form | crystalline solid |
color | Off-white to yellow |
FDA UNII | FOY14S7DFX |
CBL0137 (hydrochloride) price More Price(18)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Cayman Chemical | 19373 | CBL0137 (hydrochloride) ≥98% | 1197397-89-9 | 1mg | $109 | 2024-03-01 | Buy |
Cayman Chemical | 19373 | CBL0137 (hydrochloride) ≥98% | 1197397-89-9 | 5mg | $481 | 2024-03-01 | Buy |
Cayman Chemical | 19373 | CBL0137 (hydrochloride) ≥98% | 1197397-89-9 | 10mg | $908 | 2024-03-01 | Buy |
TRC | C227210 | CBL0137Hydrochloride | 1197397-89-9 | 5mg | $45 | 2021-12-16 | Buy |
ApexBio Technology | C3192 | CBL0137(hydrochloride) | 1197397-89-9 | 2mg | $70 | 2021-12-16 | Buy |
CBL0137 (hydrochloride) Chemical Properties,Uses,Production
Description
Curaxins are small molecules that simultaneously activate p53 and inhibit NF-κB without causing detectable genotoxicity. CBL0137 is a water soluble and metabolically stable curaxin that activates p53 with an EC50 value of 0.37 μM and inhibits NF-κB with an EC50 value of 0.47 μM. It functionally inactivates the facilitates chromatin transcription complex, driving the effects on p53 and NF-κB and promoting cancer cell death. CBL0137 has broad anticancer activity in mice when administered orally, eradicates drug-resistant cancer stem cells, and potentiates efficacy of gemcitabine in preclinical models of pancreatic cancer.
Uses
CBL0137 Hydrochloride, is an inhibitor of the histone chaperone. It can also activate p53 and inhibits NF-κB with EC50s of 0.37 and 0.47 μM, respectively.
Uses
Curaxins are small molecules that simultaneously activate p53 and inhibit NF-κB without causing detectable genotoxicity. CBL0137 is a water soluble and metabolically stable curaxin that activates p53 with an EC50 value of 0.37 μM and inhibits NF-κB with an EC50 value of 0.47 μM. It functionally inactivates the facilitates chromatin transcription complex, driving the effects on p53 and NF-κB and promoting cancer cell death. CBL0137 has broad anticancer activity in mice when administered orally, eradicates drug-resistant cancer stem cells, and potentiates efficacy of gemcitabine in preclinical models of pancreatic cancer.[Cayman Chemical]
Biological Activity
CBL0137 (CBLC137, Curaxin 137) HCl activates p53 and inhibits NF-kB with IC50 of 0.37 μM and 0.47 μM, respectively, in cell experiments. It also inhibits the histone molecular chaperone FACT, which promotes the formation of chromatin transcriptional complexes.
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].
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).
CBL0137 (hydrochloride) Preparation Products And Raw materials
Raw materials
Preparation Products
CBL0137 (hydrochloride) Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
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BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
Tianjin Xinshengjiahe Science & Technology Development Co,.Ltd | +86-86-22-87899925 +86-8618522618860 | 18522618860@163.com | China | 694 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
Dalian Meilun Biotech Co., Ltd. | 0411-62910999 13889544652 | meilunui@163.com | China | 4672 | 58 |
Guangzhou Isun Pharmaceutical Co., Ltd | 020-39119399 18927568969 | isunpharm@qq.com | China | 4428 | 55 |
Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696,15000506266 15000506266 | China | 4334 | 55 | |
BOC Sciences | 16314854226 | info@bocsci.com | United States | 9926 | 65 |
Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9806 | 58 |