1. Apoptosis
    MAPK/ERK Pathway
    PI3K/Akt/mTOR
    Metabolic Enzyme/Protease
  2. Apoptosis
    JNK
    Akt
    Caspase
    FXR
  3. Guggulsterone

Guggulsterone (Synonyms: Z/E-Guggulsterone)

Cat. No.: HY-107738
Handling Instructions

Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt. Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively.

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

Guggulsterone Chemical Structure

Guggulsterone Chemical Structure

CAS No. : 95975-55-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 77 In-stock
Estimated Time of Arrival: December 31
5 mg USD 70 In-stock
Estimated Time of Arrival: December 31
10 mg USD 130 In-stock
Estimated Time of Arrival: December 31
50 mg USD 400 In-stock
Estimated Time of Arrival: December 31
100 mg USD 700 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt[1]. Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively[2].

IC50 & Target[1]

JNK

 

Akt

 

Caspase

 

In Vitro

Guggulsterone (0.5-20 μM; 24 hours) suppresses TREM-1, TLR4 and TNF-α expression as well as the phosphorylation of IκBα and NF-κB p65 by LPS[2].

Western Blot Analysis[1]

Cell Line: RAW 264.7 murine macrophage cells
Concentration: 0.5, 5, 10, 20 μM
Incubation Time: 24 hours
Result: Suppressed TREM-1, TLR4, and TNF-α expression as well as the phosphorylation of IκBα and NF-κB p65 by LPS.
In Vivo

Guggulsterone (orally; 100 mg/kg once per day for 8 days) significantly improved the survival rates of wild-type mice with TNBS-induced colitis[2].

Animal Model: Wild-type mice with TNBS-induced colitis[2]
Dosage: 100 mg/kg
Administration: Orally; once per day; for 8 days
Result: Improved the survival rates of wild-type mice with TNBS-induced colitis.
Molecular Weight

312.45

Formula

C₂₁H₂₈O₂

CAS No.

95975-55-6

SMILES

C[[email protected]@]1(/C2=C/C)[[email protected]](CC2=O)([H])[[email protected]@]3([H])[[email protected]]([[email protected]@]4(C(CC3)=CC(CC4)=O)C)([H])CC1

Shipping

Room temperature in continental US; may vary elsewhere

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 20.83 mg/mL (66.67 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2005 mL 16.0026 mL 32.0051 mL
5 mM 0.6401 mL 3.2005 mL 6.4010 mL
10 mM 0.3201 mL 1.6003 mL 3.2005 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: ≥ 2.08 mg/mL (6.66 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (6.66 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.66 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Guggulsterone
Cat. No.:
HY-107738
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