CBL0137
Based on 13 publication(s) in Google Scholar
CBL0137, a curaxin compound, is a histone chaperone facilitates chromatin transcription (FACT) inhibitor. CBL0137 downregulates NF-κB and activates p53. CBL0137 restores both histone H3 acetylation and trimethylation. CBL0137 is an anticancer agent. CBL0137 induces cancer cell apoptosis.
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- Pureté: 99.73%
- CAS No.: 1197996-80-7
- Formule: C21H24N2O2
- Masse moléculaire:336.43
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Chemical Information
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Solvant et solubilité
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Apoptosis Compound Library
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Publications Citing Use of MedChemExpress (MCE) CBL0137
More- Cell. 2024 Dec 26;187(26):7533-7550.e23. [Abstract]
- Adv Mater. 2024 Jul;36(29):e2313991. [Abstract]
- Cancer Res. 2021 Jun 1;81(11):3105-3120. [Abstract]
- Nano Today. 2025 Oct.
- J Neuroinflammation. 2025 Oct 27;22(1):243. [Abstract]
- Cell Death Dis. 2024 Oct 27;15(10):779. [Abstract]
- Cell Death Dis. 2020 Dec 2;11(12):1029. [Abstract]
- Oncogene. 2023 Jan;42(1):11-25. [Abstract]
- Eur J Med Chem. 2024 Apr 15:270:116377. [Abstract]
- Mol Med Rep. 2024 Nov;30(5):209. [Abstract]
- Res Sq. 2026 May 19.
- bioRxiv. 2026 Apr 22:2026.04.20.719605. [Abstract]
- bioRxiv. 2026 Mar 25.
Customer Validation & Images
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IF
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RT-PCR
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RT-PCR
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Cell Imaging/Staining
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Histological Imaging/Staining
Activité biologique
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 (HY-17026), 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1197996-80-7
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Appearance Solid
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Masse moléculaire 336.43
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Formule C21H24N2O2
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Color White to light yellow
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SMILES
CC(NCCN1C2=C(C3=C1C=CC(C(C)=O)=C3)C=C(C(C)=O)C=C2)C
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Synonyms
Curaxin 137; CBL-C137
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (13)
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Journal Impact Factor
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Most Recent
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Cell
Type III interferons induce pyroptosis in gut epithelial cells and impair mucosal repair. [Abstract]2024 Dec 26;187(26):7533-7550.e23. PMID: 39500322
CBL0137 purchased from MedChemExpress. Usage Cited in: Cell. 2024 Dec 26;187(26):7533-7550.e23. [Abstract]
ALI organoid cultures were treated with CBL0137 hydrochloride (5 μM; 16 h) during homeostasis. Z-NA expression was assessed by immunofluorescence.
CBL0137 purchased from MedChemExpress. Usage Cited in: Cell. 2024 Dec 26;187(26):7533-7550.e23. [Abstract]
DNA dot blot from ALI cultures (homeostasis), small intestine (ex vivo), or spheroids left untreated (NT) or treated with CBL0137 hydrochloride (5 μM; 16 h).
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Adv Mater
2024 Jul;36(29):e2313991. PMID: 38692575
CBL0137 purchased from MedChemExpress. Usage Cited in: Adv Mater. 2024 Jul;36(29):e2313991. [Abstract]
CBL0137 hydrochloride (5 μM; 8 h) remarkably facilitated Z-DNA formation in HCT116 cells.
CBL0137 purchased from MedChemExpress. Usage Cited in: Adv Mater. 2024 Jul;36(29):e2313991. [Abstract]
CBL0137 hydrochloride (5 μM; 8 h) remarkably facilitated Z-DNA formation in four human tumor cells (HCT116, A549, MDA-MB-231; HeLa).
CBL0137 purchased from MedChemExpress. Usage Cited in: Adv Mater. 2024 Jul;36(29):e2313991. [Abstract]
Long comet tail in the CBL0137 hydrochloride (5 μM; 8 h) treatment group was observed.
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Cancer Res
Inhibition of the FACT Complex Targets Aberrant Hedgehog Signaling and Overcomes Resistance to Smoothened Antagonists. [Abstract]2021 Jun 1;81(11):3105-3120. PMID: 33853831 -
CBL0137 purchased from MedChemExpress. Usage Cited in: Nano Today. 2025 Oct.
Confocal fluorescence images and quantitative analysis of ZBP1 expression in RAW264.7 cells treated with HA@BPSN, free CBL0137, and CBL@BPSN for 24 hours.
CBL0137 purchased from MedChemExpress. Usage Cited in: Nano Today. 2025 Oct.
Raw264.7 cells treated with BPSN, CBL@BPSN, HA@BPSN, and free CBL0137 (24 h). Extraction of total RNA and assessment of relative mRNA levels of the indicated cytokine and chemokine genes using qRT-PCR.
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J Neuroinflammation
2025 Oct 27;22(1):243. PMID: 41146204
CBL0137 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2025 Oct 27;22(1):243. [Abstract]
CBL0137 (CBL) reduces HSV-1 replication in BMDMs. BMDMs were either mock-infected or infected with HSV-1 (MOI = 10) and treated with or without CBL (1 μM) 2 h post-infection. Virus DNA was measured by qPCR 6 h after infection. Each point represents an independent experiment.
CBL0137 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2025 Oct 27;22(1):243. [Abstract]
CBL0137 (1 μM, 2 h) induced BMDM death during HSV-1 infection. Left: representative image of live cells (Calcein-AM, green) and dead cells (PI, red). Scale bar: 50 μm. Right: quantification of PI⁺ cells. Each dot represents an independent experiment (n = 3).
CBL0137 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2025 Oct 27;22(1):243. [Abstract]
CBL0137 defends against HSV-1 retinal infection. Mice were IVT injected with PBS (CTRL) or HSV-1(4×10⁴ PFU). CBL0137 (2 μg, administered intravitreally) or PBS (mock) was co-injected with HSV-1.HE staining showing eye morphology. CBL preserved retinal structure in both WT and STING-/- mice following HSV-1 infection and prevented retinal necrosis in STING-/- mice at 9 dpi. Scale bars: overview 1 mm; magnified 100 μm.
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Cell Death Dis
Sensing of endogenous retroviruses-derived RNA by ZBP1 triggers PANoptosis in DNA damage and contributes to toxic side effects of chemotherapy. [Abstract]2024 Oct 27;15(10):779. PMID: 39465258 -
Cell Death Dis
Effective inhibition of MYC-amplified group 3 medulloblastoma by FACT-targeted curaxin drug CBL0137. [Abstract]2020 Dec 2;11(12):1029. PMID: 33268769 -
Oncogene
Therapeutic targeting the oncogenic driver EWSR1::FLI1 in Ewing sarcoma through inhibition of the FACT complex. [Abstract]2023 Jan;42(1):11-25. PMID: 36357572
CBL0137 purchased from MedChemExpress. Usage Cited in: Oncogene. 2023 Jan;42(1):11-25. [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).
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Eur J Med Chem
Mono-quinoxaline-induced DNA structural alteration leads to ZBP1/RIP3/MLKL-driven necroptosis in cancer cells. [Abstract]2024 Apr 15:270:116377. PMID: 38581731 -
Mol Med Rep
PDCD4 promotes inflammation/fibrosis by activating the PPAR‑γ/NF‑κB pathway in mouse atrial myocytes. [Abstract]2024 Nov;30(5):209. PMID: 39301631 -
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bioRxiv
2026 Apr 22:2026.04.20.719605. PMID: 42079300 -
Solvant et solubilité
DMSO : 11.11 mg/mL (33.02 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.11 mg/mL (3.30 mM); Clear solution
This protocol yields a clear solution of ≥ 1.11 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.1 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.11 mg/mL (3.30 mM); Clear solution
This protocol yields a clear solution of ≥ 1.11 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.1 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Barone TA, et al. Anticancer drug candidate CBL0137, which inhibits histone chaperone FACT, is efficacious in preclinical orthotopic models of temozolomide-responsive and -resistant glioblastoma. Neuro Oncol. 2017 Feb 1;19(2):186-196. h [Content Brief]
[2]. Burkhart C, et al. Curaxin CBL0137 eradicates drug resistant cancer stem cells and potentiates efficacy of gemcitabine in preclinical models of pancreatic cancer. Oncotarget. 2014 Nov 30;5(22):11038-53. [Content Brief]
[3]. Ehteda A, et al. Dual targeting of the epigenome via FACT complex and histone deacetylase is a potent treatment strategy for DIPG. Cell Rep. 2021 Apr 13;35(2):108994. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9724 mL | 14.8619 mL | 29.7239 mL | 74.3097 mL |
| 5 mM | 0.5945 mL | 2.9724 mL | 5.9448 mL | 14.8619 mL | |
| 10 mM | 0.2972 mL | 1.4862 mL | 2.9724 mL | 7.4310 mL | |
| 15 mM | 0.1982 mL | 0.9908 mL | 1.9816 mL | 4.9540 mL | |
| 20 mM | 0.1486 mL | 0.7431 mL | 1.4862 mL | 3.7155 mL | |
| 25 mM | 0.1189 mL | 0.5945 mL | 1.1890 mL | 2.9724 mL | |
| 30 mM | 0.0991 mL | 0.4954 mL | 0.9908 mL | 2.4770 mL |
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