Art. -Nr.: HY-18935

CBL0137

(Synonyms: Curaxin 137; CBL-C137)

13 Cited Publications

Kundenbewertung

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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Reinheit: 99.73%
CAS. Nr.: 1197996-80-7
Formel: C₂₁H₂₄N₂O₂
Molecular Weight:336.43

Speicherung:

4°C, sealed storage, away from moisture

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

CBL0137 Chemical Structure

CAS. Nr.: 1197996-80-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (13)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen :

Alle NF-κB Isoform-spezifische Produkte anzeigen :

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 (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.

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 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].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1197996-80-7
Appearance Solid
Molecular Weight 336.43
Formel C₂₁H₂₄N₂O₂
Color White to light yellow
SMILES

CC(NCCN1C2=C(C3=C1C=CC(C(C)=O)=C3)C=C(C(C)=O)C=C2)C
Synonyms

Curaxin 137; CBL-C137
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

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

Publications (13)

All RT-PCRCell Imaging/StainingHistological Imaging/StainingBio/Physico-chemical AssayIF

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Journal Impact Factor

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).
Adv Mater

Manipulating Radiation-Sensitive Z-DNA Conformation for Enhanced Radiotherapy. [Abstract]

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.
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
Nano Today

2025 Oct.

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.
J Neuroinflammation

STING activates ZBP1-mediated PANoptosis to defend against HSV-1 retinal infection. [Abstract]

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.
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).
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
Res Sq

2026 May 19.
bioRxiv

Mechanisms controlling the deposition and dynamics of histone variant H2BE. [Abstract]

2026 Apr 22:2026.04.20.719605. PMID: 42079300
bioRxiv

2026 Mar 25.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.9724 mL

14.8619 mL

29.7239 mL

5 mM

0.5945 mL

2.9724 mL

5.9448 mL

10 mM

0.2972 mL

1.4862 mL

2.9724 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.11 mg/mL (3.30 mM); Clear solution

This protocol yields a clear solution of ≥ 1.11 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.1 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

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].

MedChemExpress (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].

MedChemExpress (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].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

CBL0137

13 Cited Publications

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CBL0137

Apoptosis Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

NF-κB Signaling Compound Library

Stem Cell Signaling Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Pyroptosis Compound Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

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Anti-Obesity Compound Library

Transcription Factor-Targeted Library

Anti-Liver Cancer Compound Library

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Antidepressant Compound Library

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Cancer Stem Cells Compound Library

Pain-Related Compound Library

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Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

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Bioactive Compound Library Max

MCE Bioactive Compound Library

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Bioactive Compound Library

Anti-Fibrosis Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) CBL0137

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen

Alle NF-κB Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (13)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CBL0137 Related Classifications

HY-18935 Related Classifications