CBL0137 hydrochloride
Based on 14 publication(s) in Google Scholar
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.
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- Pureté : 99.72%
- CAS No.: 1197397-89-9
- Formule: C21H25ClN2O2
- Masse moléculaire:372.89
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) CBL0137 hydrochloride
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]
- Cell Death Dis. 2024 Oct 27;15(10):779. [Abstract]
- Cell Death Dis. 2020 Dec 2;11(12):1029. [Abstract]
- J Neuroinflammation. 2025 Oct 27;22(1):243. [Abstract]
- Nano Today. 2025 Oct.
- Oncogene. 2023 Jan;42(1):11-25. [Abstract]
- Eur J Med Chem. 2024 Apr 15:270:116377. [Abstract]
- EMBO Rep. 2026 Jul 11.
- 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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RT-PCR
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Cell Imaging/Staining
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Histological Imaging/Staining
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IF
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RT-PCR
Activité biologique
Description
IC50 & Target
[2]|
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1197397-89-9
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Appearance Solid
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Masse moléculaire 372.89
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Formule C21H25ClN2O2
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Color Off-white to yellow
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SMILES
CC(NCCN1C2=C(C3=C1C=CC(C(C)=O)=C3)C=C(C(C)=O)C=C2)C.[H]Cl
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Synonyms
Curaxin-137 hydrochloride; CBL-C137 hydrochloride
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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, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Publications (14)
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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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 -
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 -
J Neuroinflammation
2025 Oct 27;22(1):243. PMID: 41146204
CBL0137 hydrochloride 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 hydrochloride 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 hydrochloride 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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CBL0137 hydrochloride 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 hydrochloride 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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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 hydrochloride 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 -
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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
In Vitro:
DMSO : 25 mg/mL (67.04 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)
H2O : 10 mg/mL (26.82 mM; Need ultrasonic)
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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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: ≥ 2.5 mg/mL (6.70 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.70 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
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, 1 year; -20°C, 6 months (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
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Pureté et documentation
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Fiche technique (293 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. 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]
[2]. Gasparian AV, et al. Curaxins: anticancer compounds that simultaneously suppress NF-κB and activate p53 by targeting FACT. Sci Transl Med. 2011 Aug 10;3(95):95ra74. [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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.6818 mL | 13.4088 mL | 26.8176 mL | 67.0439 mL |
| 5 mM | 0.5364 mL | 2.6818 mL | 5.3635 mL | 13.4088 mL | |
| 10 mM | 0.2682 mL | 1.3409 mL | 2.6818 mL | 6.7044 mL | |
| 15 mM | 0.1788 mL | 0.8939 mL | 1.7878 mL | 4.4696 mL | |
| 20 mM | 0.1341 mL | 0.6704 mL | 1.3409 mL | 3.3522 mL | |
| 25 mM | 0.1073 mL | 0.5364 mL | 1.0727 mL | 2.6818 mL | |
| DMSO | 30 mM | 0.0894 mL | 0.4470 mL | 0.8939 mL | 2.2348 mL |
| 40 mM | 0.0670 mL | 0.3352 mL | 0.6704 mL | 1.6761 mL | |
| 50 mM | 0.0536 mL | 0.2682 mL | 0.5364 mL | 1.3409 mL | |
| 60 mM | 0.0447 mL | 0.2235 mL | 0.4470 mL | 1.1174 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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