2. Apoptosis
    NF-κB
  3. MDM-2/p53
    NF-κB
  4. CBL0137 hydrochloride

CBL0137 hydrochloride  (Synonyms: Curaxin-137 hydrochloride; CBL-C137 hydrochloride)

Cat. No.: HY-18935A Purity: 99.66%
COA Handling Instructions

CBL0137 hydrochloride is an inhibitor of the histone chaperone, FACT. CBL0137 hydrochloride can also activate p53 and inhibits NF-κB with EC50s of 0.37 and 0.47 µM, respectively.

For research use only. We do not sell to patients.

CBL0137 hydrochloride Chemical Structure

CBL0137 hydrochloride Chemical Structure

CAS No. : 1197397-89-9

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 135 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 135 In-stock
Estimated Time of Arrival: December 31
Solid
2 mg USD 77 In-stock
Estimated Time of Arrival: December 31
5 mg USD 165 In-stock
Estimated Time of Arrival: December 31
10 mg USD 286 In-stock
Estimated Time of Arrival: December 31
25 mg USD 616 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1089 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    CBL0137 hydrochloride 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).

    View All NF-κB Isoform Specific Products:

    View All Isoforms
    NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    CBL0137 hydrochloride is an inhibitor of the histone chaperone, FACT. CBL0137 hydrochloride can also activate p53 and inhibits NF-κB with EC50s of 0.37 and 0.47 µM, respectively.

    IC50 & Target

    p53

    0.37 μM (IC50)

    NF-κB

    0.47 μM (IC50)

    In Vitro

    Treatment with CBL0137 hydrochloride leads to complete absence of living cells at concentrations above 2.5 μM. CBL0137 hydrochloride causes a greater reduction in the number of colonies formed of not only MiaPaCa-2 cells when combines with gemcitabine, but also gemcitabine-resistant PANC-1 cells. Treatment of human pancreatic cancer cells with CBL0137 hydrochloride results in a dose dependent reduction of protein and mRNA levels of RRM1 and RRM2[1].

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

    The CBL0137 hydrochloride monotherapy group and the CBL0137 hydrochloride-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 CBL0137 hydrochloride 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]. CBL0137 hydrochloride, 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.
    Clinical Trial
    Molecular Weight

    372.89

    Appearance

    Solid

    Formula

    C21H25ClN2O2
    CAS No.
    SMILES

    CC(NCCN1C2=C(C3=C1C=CC(C(C)=O)=C3)C=C(C(C)=O)C=C2)C.[H]Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
    Solvent & Solubility
    In Vitro: 

    DMSO : 33.33 mg/mL (89.38 mM; Need ultrasonic)

    H2O : 10 mg/mL (26.82 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6818 mL 13.4088 mL 26.8176 mL
    5 mM 0.5364 mL 2.6818 mL 5.3635 mL
    10 mM 0.2682 mL 1.3409 mL 2.6818 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (6.70 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (6.70 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.66%

    COA (251 KB) LCMS (266 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [1]

    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. 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 CBL0137 hydrochloride for 1h. After that 105 cells from each treatment condition are plated in 3 wells of 6-well plate in 2 mL 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, 100 mg/kg captisol i.v. and sterile water via gavage, 2) 50 to 90 mg/kg CBL0137 hydrochloride in 100 mg/mL captisol i.v. delivered via tail vein once per week, 3) 10 to 20 mg/kg CBL0137 hydrochloride p.o. via oral gavage, 5 days on/2 days off. 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.
    References
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    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.

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    CBL01371197397-89-9Curaxin-137CBL-C137CBL 0137CBL-0137Curaxin137Curaxin 137MDM-2/p53NF-κBNuclear factor-κBNuclear factor-kappaBInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Salutation

    Applicant Name *

    		 

    Email address *

    Phone number *

    		 

    Organization name *

    Department *

    		 

    Requested quantity *

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    CBL0137 hydrochloride
    Cat. No.:
    HY-18935A
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email address *

    Phone number

    		 

    Department *

    Organization name *

    		 

    Country or Region *

    Remarks

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.