2. Epigenetics Apoptosis NF-κB
  3. Histone Acetyltransferase MDM-2/p53 NF-κB
  4. CBL0137

CBL0137  (Synonyms: Curaxin 137; CBL-C137)

目录号: HY-18935
产品使用指南

摩尔计算器

CBL0137 是一种 curaxin 化合物，是一种组蛋白伴侣促进染色质转录 (FACT) 抑制剂。CBL0137 下调 NF-?B 并激活 p53。CBL0137 可恢复组蛋白 H3 乙酰化和三甲基化。CBL0137 是一种抗癌剂。CBL0137 诱导癌细胞凋亡 (apoptosis)。

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CBL0137 Chemical Structure

CBL0137 Chemical Structure

CAS No. : 1197996-80-7

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CBL0137 的其他形式现货产品:

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Other Forms of CBL0137:

CBL0137 相关抗体

Top Publications Citing Use of Products

    CBL0137 purchased from MCE. Usage Cited in: Oncogene. 2022 Nov 10.  [Abstract]

    CBL0137 (1 μM) substantiality reduces cell proliferation and induces cell apoptosis (Ki67 for proliferation and cleaved-caspase3 (CC3) for apoptosis) in two EwS lines (A-673 and SK-N-MC cells).

    查看 NF-κB 亚型特异性产品:

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    NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    CBL0137, a curaxin compound, is a histone chaperone facilitates chromatin transcription (FACT) inhibitor. CBL0137 downregulates NF-?B and activates p53. CBL0137 restores both histone H3 acetylation and trimethylation. CBL0137 is an anticancer agent. CBL0137 induces cancer cell apoptosis[1].

    体外研究
    (In Vitro)

    Treatment with CBL-0137 leads to complete absence of living cells at concentrations above 2.5 μM. CBL-0137 causes a greater reduction in the number of colonies formed of not only MiaPaCa-2 cells when combined with gemcitabine, but also gemcitabine-resistant PANC-1 cells. Treatment of human pancreatic cancer cells with CBL-0137 results in a dose dependent reduction of protein and mRNA levels of RRM1 and RRM2. CBL-0137 is able to prevent gemcitabine induced expression of RRM1 and RRM2 on mRNA and protein levels[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    CBL0137 相关抗体:
    体内研究
    (In Vivo)

    The CBL-0137 monotherapy group and the CBL-0137-gemcitabine combination group samples show large necrotic fields, numerous apoptotic bodies and loss of tumor cells. Sub-optimal doses of 50 to 60 mg/kg CBL-0137 causes similar enhancement of gemcitabine antitumor activity as that produced by the maximum tolerated dose (MTD) of 90 mg/kg as indicated by the lack of statistically significant differences among the combination groups. CBL0137 hydrochloride inhibits FACT function through depletion of the pool of active FACT involved in transcription elongation[1]. CBL-0137, given by oral gavage at a nontoxic dose of 30 mg/kg per day on a 5 days on/2 days off schedule, suppresses tumor growth in xenografts of colon (DLD-1), renal cell carcinoma (Caki-1), and melanoma (Mel-7) tumor cell lines and transplanted surgical samples from patients with pancreatic ductal adenocarcinoma[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    336.43

    Formula

    C21H24N2O2
    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    纯度 & 产品资料
    参考文献
    Kinase Assay
    [1]

    MiaPaca2 and BxPC-3 cells are treated with CBL-0137for 4 or 24h. 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. GAPDH is used as a loading control. Proteins are visualized using ECL kit[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [1]

    Cells are resuspended in serum free Dulbecco's Modified Eagle Medium (DMEM) and treated with different concentrations of CBL-0137 for 1h. After that 105 from each treatment condition are plated in 3 wells of 6-well plate in 2mL of serum-free DMEM/F12 medium supplemented with 0.4% BSA, 0.2×B27, 10 ng/mL recombinant EGF and containing 0.25% agarose. 103 cells from each treatment condition are plated in 3 wells of 6-well plate in regular FBS containing medium. Colonies are counted using inverted microscope 7 to 15 days after plating[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    10-week old female athymic nude mice (n=8 per treatment group) are deeply anesthetized with ketamine/xylazine. Using laparotomy, 2× 106 PANC-1 cells are inoculated into the tail of the pancreas of each mouse. Two weeks following inoculation (tumor presence confirmed by ultrasound), treatment commenced. The following regimens are used: 1) vehicles, 100mg/kg captisol i.v. and sterile water via gavage, 2) 50 to 90 mg/kg CBL-0137 in 100 mg/mL captisol i.v. delivered via tail vein once per week, 3) 10 to 20 mg/kg CBL-0137 p.o. via oral gavage, 5 days on/2 days off, 4). Tumor measurement is done with digital calipers. Tumor volume is calculated using the equation L×W2/2 where L is the longest dimension and W is the dimension perpendicular to W. Mice are followed until at least one tumor per mouse reached 1000 mm3 or 90 days from start of treatment, whichever comes first[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    参考文献

    CBL0137 相关分类

    • 摩尔计算器

    • 稀释计算器

    The molarity calculator equation

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    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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    浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    CBL01371197996-80-7Curaxin 137 CBL-C137CBL 0137CBL-0137Curaxin137Curaxin-137Histone AcetyltransferaseMDM-2/p53NF-κBHATsHATNuclear factor-κBNuclear factor-kappaBsmall-cell lung canceranticancerpancreatic cancerFACTInhibitorinhibitorinhibit

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