Cat. No.: HY-N1405

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Cucurbitacin I

(Synonyms: Elatericin B; JSI-124; NSC-521777)

13 Cited Publications

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Based on 13 publication(s) in Google Scholar

Cucurbitacin I is a natural selective inhibitor of JAK2/STAT3, with potent anti-cancer activity.

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Pureté: 99.60%
CAS No.: 2222-07-3
Formule: C₃₀H₄₂O₇
Masse moléculaire:514.65

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Cucurbitacin I Chemical Structure

CAS No.: 2222-07-3

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (13)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Bioz

Activité biologique

Description

Cucurbitacin I is a natural selective inhibitor of JAK2/STAT3, with potent anti-cancer activity.

IC₅₀ & Target

JAK2

STAT3

Voir tous les produits spécifiques à Isoform STAT :

Voir tous les produits spécifiques à Isoform JAK :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	140 nM Compound: Cucurbitacin I	Growth inhibition of human A549 cells Growth inhibition of human A549 cells	[PMID: 28814374]
C8166	CC₅₀	14.4 μg/mL Compound: 7	Cytotoxicity against human C8166 cells by MTT method Cytotoxicity against human C8166 cells by MTT method	[PMID: 18088099]
C8166	EC₅₀	0.7 μg/mL Compound: 7	Antiviral activity against HIV1 in C8166 cells after 72 hrs Antiviral activity against HIV1 in C8166 cells after 72 hrs	[PMID: 18088099]
Cancer cell lines	IC₅₀	<0.4 μM Compound: Cucurbitacin I	Growth inhibition of human breast cancer cells Growth inhibition of human breast cancer cells	[PMID: 15332833]
Cancer cell lines	IC₅₀	<0.4 μM Compound: Cucurbitacin I	Growth inhibition of human CNS cancer cells Growth inhibition of human CNS cancer cells	[PMID: 15332833]
Cancer cell lines	IC₅₀	<0.4 μM Compound: Cucurbitacin I	Growth inhibition of human colon cancer cells Growth inhibition of human colon cancer cells	[PMID: 15332833]
Cancer cell lines	IC₅₀	<0.4 μM Compound: Cucurbitacin I	Growth inhibition of human lung cancer cells Growth inhibition of human lung cancer cells	[PMID: 15332833]
HepG2	EC₅₀	3.16 μM Compound: 5	Hepatoprotective activity in human HepG2 cells assessed as inhibition of CCl4-induced toxicity after 24 hrs by MTT assay Hepatoprotective activity in human HepG2 cells assessed as inhibition of CCl4-induced toxicity after 24 hrs by MTT assay	[PMID: 21459003]
HepG2	IC₅₀	15.8 μM Compound: 5	Cytotoxicity against human HepG2 cells after 24 hrs assessed as inhibition of cell viability by MTT assay Cytotoxicity against human HepG2 cells after 24 hrs assessed as inhibition of cell viability by MTT assay	[PMID: 21459003]
HL-60	IC₅₀	0.1 nM Compound: 2	Cytotoxicity against human HL60 cells after 72 hrs by WST-8 assay Cytotoxicity against human HL60 cells after 72 hrs by WST-8 assay	[PMID: 20347305]
HSC-T6	EC₅₀	0.02 μM Compound: 5	Antiproliferative activity against serum-stimulated rat HSC-T6 cells after 24 hrs by MTT assay Antiproliferative activity against serum-stimulated rat HSC-T6 cells after 24 hrs by MTT assay	[PMID: 21459003]
HSC-T6	IC₅₀	3.6 μM Compound: 5	Cytotoxicity against rat HSC-T6 cell after 24 hrs by MTT assay Cytotoxicity against rat HSC-T6 cell after 24 hrs by MTT assay	[PMID: 21459003]
HT-1080	IC₅₀	0.47 nM Compound: 2	Cytotoxicity against human HT1080 cells after 72 hrs by WST-8 assay Cytotoxicity against human HT1080 cells after 72 hrs by WST-8 assay	[PMID: 20347305]
HT-29	IC₅₀	0.19 μM Compound: 12	Cytotoxicity against human HT-29 cells after 3 days by sulforhodamine B assay Cytotoxicity against human HT-29 cells after 3 days by sulforhodamine B assay	[PMID: 22239601]
JY	IC₅₀	0.95 μM Compound: 3	Inhibition of LFA1 expressed in human JY cells interaction with ICAM1-IG expressed in human HeLa cell monolayer after 45 mins by cell adhesion assay Inhibition of LFA1 expressed in human JY cells interaction with ICAM1-IG expressed in human HeLa cell monolayer after 45 mins by cell adhesion assay	[PMID: 7852999]
MCF7	IC₅₀	0.0607 μM Compound: 7	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTS/PMS assay Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTS/PMS assay	[PMID: 25756299]
U-937	IC₅₀	0.3 nM Compound: 2	Cytotoxicity against human U937 cells after 72 hrs by WST-8 assay Cytotoxicity against human U937 cells after 72 hrs by WST-8 assay	[PMID: 20347305]

In Vitro

Exposure of the COLO205 cells to Cucurbitacin I significantly decreases cell viability. The anticancer activity of Cucurbitacin I is accomplished by downregulating p-STAT3 and MMP-9 expression^[1].
PE-induced cell enlargement and upregulation of ANF and β-MHC are significantly suppressed by pretreatment of the cardiomyocytes with Cucurbitacin I. Notably, Cucurbitacin I also impaires connective tissue growth factor (CTGF) and MAPK signaling, pro-hypertrophic factors, as well as TGF-β/Smad signaling, the important contributing factors to fibrosis^[2].
Incubation of the Seax cell line with the Jak/Stat3 inhibitor Cucurbitacin I result in a time- and concentration-dependent decrease of P-Stat3 and Stat3. In freshly isolated Sz cells (n=3), Cucurbitacin I induces a concentration-dependent decrease in Stat3 expression whereas P-Stat3 is undetectable. Finally, incubation of freshly isolated Sz cells (n=4) with 30 μM Cucurbitacin I for 6 hours induces apoptosis in the large majority (73-91%) of tumor cells^[3].

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

In Vivo

No major side effects are noted throughout the study. It is shown that average tumor volumes at the end of the study are as follows: control, 616 mm³ (±130); CQ, 580 mm³ (±107); Cucurbitacin I, 346mm³ (±79); and combination, 220mm³ (±62). The differences in tumor volume between the Cucurbitacin I and control, combination and control, and combination and Cucurbitacin I arms are significant. Furthermore, combination-treated tumors exhibit a significantly lower average tumor weight at study termination than the control. Moreover, there was no effect on the body weights of mice^[4].

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

Chemical Information

CAS No. 2222-07-3
Appearance Solid
Masse moléculaire 514.65
Formule C₃₀H₄₂O₇
Color White to yellow
SMILES

CC(C)(C1=CC[C@@]2([H])[C@@]3(C[C@@H](O)[C@@H]([C@]3(C4)C)[C@@](C)(O)C(/C=C/C(C)(O)C)=O)C)C(C(O)=C[C@@]1([H])[C@]2(C)C4=O)=O
Synonyms

Elatericin B; JSI-124; NSC-521777
Structure Classification
- Terpenoids
- Triterpenes
Initial Source
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (13)

All WB

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Journal Impact Factor

Nature

CD300ld on neutrophils is required for tumour-driven immune suppression. [Abstract]

2023 Sep;621(7980):830-839. PMID: 37674079
J Neuroinflammation

Photobiomodulation inhibits the activation of neurotoxic microglia and astrocytes by inhibiting Lcn2/JAK2-STAT3 crosstalk after spinal cord injury in male rats. [Abstract]

2021 Nov 5;18(1):256. PMID: 34740378
Arch Pharm Res

JAK2/STAT3-dependent regulation of MDM4/MDM2-p53 signaling in methotrexate-induced ferroptosis and nephrotoxicity. [Abstract]

2026 Feb;49(2):223-241. PMID: 41723769
Neural Regen Res

Single-cell RNA sequencing reveals the heterogeneity and interactions of immune cells and Müller glia during zebrafish retina regeneration. [Abstract]

2025 Dec 1;20(12):3635-3648. PMID: 38934409
Cancer Cell Int

Progranulin promoted the proliferation, metastasis, and suppressed apoptosis via JAK2-STAT3/4 signaling pathway in papillary thyroid carcinoma. [Abstract]

2023 Sep 2;23(1):191. PMID: 37660003
Chem Biol Interact

Induction of cardiotoxicity in zebrafish embryos by 1,1-dichloro-2,2-bis(p-chlorophenyl)ethylene through the JAK-STAT and NOTCH signaling pathways. [Abstract]

2022 Dec 1:368:110226. PMID: 36280156
Mol Cell Endocrinol

In vitro primary hyperparathyroidism model application of computationally repurposed drugs. [Abstract]

2024 Apr 1:583:112159. PMID: 38228226
Parasit Vectors

LILRB4 regulates the function of decidual MDSCs via the SHP-2/STAT6 pathway during Toxoplasma gondii infection. [Abstract]

2023 Jul 17;16(1):237. PMID: 37461040
Cell Cycle

Blocking Notch signal pathway suppresses the activation of neurotoxic A1 astrocytes after spinal cord injury. [Abstract]

2019 Nov;18(21):3010-3029. PMID: 31530090

Cucurbitacin I purchased from MedChemExpress. Usage Cited in: Cell Cycle. 2019 Nov;18(21):3010-3029. [Abstract]

Western blot analysis of C3, NICD, p-Stat3, and Stat3 expression in astrocytes treated with MCM or MCM plus the Stat3 inhibitor JSI-124 (0.2 or 0.5 μM) for 24 h.
Photodiagnosis Photodyn Ther

Photobiomodulation reduces spinal cord edema by decreasing the expression of AQP4 in the astrocytes of male spinal cord injury rats via the JAK2/STAT3 signaling pathway. [Abstract]

2024 Dec:50:104364. PMID: 39401645
Biochem Biophys Res Commun

Chinese herb related molecules Catechins, Caudatin and Cucurbitacin-I inhibit the proliferation of glioblastoma by activating KDELR2-mediated endoplasmic reticulum stress. [Abstract]

2023 Dec 20:687:149196. PMID: 37939504
Research Square Preprint

2023 Oct 11.
Research Square Preprint

2021 May.

Solvant et solubilité

In Vitro:

DMSO : ≥ 100 mg/mL (194.31 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

1.9431 mL

9.7153 mL

19.4307 mL

5 mM

0.3886 mL

1.9431 mL

3.8861 mL

10 mM

0.1943 mL

0.9715 mL

1.9431 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 3 mg/mL (5.83 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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.

Protocol 2

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

Solubility: ≥ 3 mg/mL (5.83 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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: ≥ 3 mg/mL (5.83 mM); Clear solution

This protocol yields a clear solution of ≥ 3 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 (30.0 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

Protocole

Animal Administration^[4]

Mice^[4]
BALB/c nude (nu/nu) female mice are used. U251 cells (5×10⁶ cells in 50 μL of serum-free DMEM) are inoculated subcutaneously into the right flank of 5-week-old female mice after acclimatization for a week. Tumor growth is measured daily with calipers. When the tumors reach a mean volume of 90-120 mm³, animals are randomized into groups. In the first experiment, 16 mice are randomly assigned to Cucurbitacin I (1 mg/kg/day in 20% DMSO in PBS) or drug vehicle control (20% DMSO in PBS) and dosed intraperitoneally with 100 μL of vehicle or drug once daily for 18 days, whereas, in the second, 20 mice are assigned to four groups. Control animals receive 20% DMSO in PBS vehicle, whereas treated animals are injected with Cucurbitacin I (1 mg/kg/day) in 20% DMSO in PBS, CQ (25 mg/kg/day) in 20% DMSO in PBS, and Cucurbitacin I (1 mg/kg/day) plus CQ (25 mg/kg/day) in 20% DMSO in PBS and dosed intraperitoneally with 100 μL of vehicle or drug once daily for 15 days^[4].

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (282 KB)
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Portuguese - PT (480 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)
Instruction de manipulation (2659 KB)

Références

[1]. Song J, et al. Cucurbitacin I inhibits cell migration and invasion and enhances chemosensitivity in colon cancer. Oncol Rep. 2015 Apr;33(4):1867-71. [Content Brief]

[2]. Moon Hee Jeong, et al. Cucurbitacin I Attenuates Cardiomyocyte Hypertrophy via Inhibition of Connective Tissue Growth Factor (CCN2) and TGF- β/Smads Signalings. PLoS One. 2015 Aug 21;10(8):e0136236. [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

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9431 mL	9.7153 mL	19.4307 mL	48.5767 mL
	5 mM	0.3886 mL	1.9431 mL	3.8861 mL	9.7153 mL
	10 mM	0.1943 mL	0.9715 mL	1.9431 mL	4.8577 mL
	15 mM	0.1295 mL	0.6477 mL	1.2954 mL	3.2384 mL
	20 mM	0.0972 mL	0.4858 mL	0.9715 mL	2.4288 mL
	25 mM	0.0777 mL	0.3886 mL	0.7772 mL	1.9431 mL
	30 mM	0.0648 mL	0.3238 mL	0.6477 mL	1.6192 mL
	40 mM	0.0486 mL	0.2429 mL	0.4858 mL	1.2144 mL
	50 mM	0.0389 mL	0.1943 mL	0.3886 mL	0.9715 mL
	60 mM	0.0324 mL	0.1619 mL	0.3238 mL	0.8096 mL
	80 mM	0.0243 mL	0.1214 mL	0.2429 mL	0.6072 mL
	100 mM	0.0194 mL	0.0972 mL	0.1943 mL	0.4858 mL

Keywords

Cucurbitacin I

13 Cited Publications

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Cucurbitacin I

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

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Terpenoids Library

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Publications Citing Use of MedChemExpress (MCE) Cucurbitacin I

Voir tous les produits spécifiques à Isoform STAT

Voir tous les produits spécifiques à Isoform JAK

Activité biologique

Chemical Information

Publications (13)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Cucurbitacin I Related Classifications

Cat. No.: HY-N1405