Glabrescione B

Cat No.:V69838 Purity: ≥98%
Glabrescione B is the first compound to bind to the Hedgehog (Hh) regulator Gli1 and impair its activity by interfering with Gli1-DNA interactions.
Glabrescione B Chemical Structure CAS No.: 65893-94-9
Product category: Gli
This product is for research use only, not for human use. We do not sell to patients.
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1mg
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Product Description
Glabrescione B is the first compound to bind to the Hedgehog (Hh) regulator Gli1 and impair its activity by interfering with Gli1-DNA interactions. Glabrescione B suppresses the growth of Hedgehog-dependent tumor cells and inhibits the self-renewal and cloning abilities of tumor-derived stem cells.
Biological Activity I Assay Protocols (From Reference)
Targets
Gli1-DNA Interaction[1]
ln Vitro
Glabrescione B (5 μM; 24-72 hours) suppresses the proliferation of Gli-dependent basal cell carcinoma[2]. Glabrescione B (1-10 μM; 24-48 hours) reduces Gli1 mRNA expression levels[2].
Cell Assay
Cell Proliferation Assay [1]
Cell Types: ASZ001 BCC cells
Tested Concentrations: 5 μM
Incubation Duration: 24-72 hrs (hours)
Experimental Results: Basal cell carcinoma cell proliferation was impaired.

Western Blot Analysis[1]
Cell Types: ASZ001 BCC cells
Tested Concentrations: 1-10 μM
Incubation Duration: 24-48 hrs (hours)
Experimental Results: Gli1 mRNA expression levels was decreased.
Animal Protocol
Animal/Disease Models: Female NOD/SCID (severe combined immunodeficient) mouse (ASZ001 BCC allografts)[2]
Doses: 100 μmol/kg
Route of Administration: Ip; every second day for 18 days
Experimental Results: A significant reduction of tumor growth as well as Gli1 mRNA levels was observed.
References
[1]. Ingallina C, et al. Polymeric glabrescione B nanocapsules for passive targeting of Hedgehog-dependent tumor therapy in vitro. Nanomedicine (Lond). 2017;12(7):711-728.
[2]. Infante P, et al. Gli1/DNA interaction is a druggable target for Hedgehog-dependent tumors. EMBO J. 2015;34(2):200-217.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C27H30O6
Molecular Weight
450.52
CAS #
65893-94-9
SMILES
C/C(/C)=C\COC1=C(OC/C=C(\C)/C)C=CC(C2C(=O)C3C(=CC(OC)=CC=3OC)OC=2)=C1
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Solubility Data
Solubility (In Vitro)
DMSO: 100 mg/mL (221.97 mM)
Solubility (In Vivo)
Solubility in Formulation 1: 2.5 mg/mL (5.55 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: 2.5 mg/mL (5.55 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (5.55 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.2197 mL 11.0983 mL 22.1966 mL
5 mM 0.4439 mL 2.2197 mL 4.4393 mL
10 mM 0.2220 mL 1.1098 mL 2.2197 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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