GRP78-IN-1

Cat. No.: HY-145857: FAQs
Data Sheet Handling Instructions

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GRP78-IN-1 exhibits several interactions with GRP78 residues with binding energy of -8.07 kcal/mol. GRP78-IN-1 shows the potent cytotoxic, anti-proliferative in cancer cells. GRP78-IN-1 exhibits promising apoptosis in breast cancer cells and wound healing properties.

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

GRP78-IN-1 Chemical Structure

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

Grp78

In Vitro

GRP78-IN-1 (compound 3i) (0.01, 0.1, 1, 10, 100 µM; 48 h) shows the most potent cytotoxic effect (IC₅₀s of 2.06, 12.57, 9, 18, 4.9, 2.19, 62.48 µM in MCF-1, PANC-1, HCT-116, PC-3, A549, MDA-MB-231 and FR-2 cells, respectively)^[1].
GRP78-IN-1 (1, 2, 4, 6 µM) shows a steady increase in the expression of pro-apoptotic proteins viz. Par-4, apoptotic cascade in BAX and cleaved caspase 9 cells^[1].
GRP78-IN-1 (1, 2, 4, 6 µM; 48 h) inhibits the motility of MCF-7 and A549 cells in a dose-dependent manner^[1].

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

Cell Cytotoxicity Assay^[1]

Cell Line:	MCF-1, MDA-MB-231, PANC-1, HCT-116, PC-3, A549, FR-2cells
Concentration:	0.01, 0.1, 1, 10, 100 µM
Incubation Time:	48 h
Result:	Showed the most promising cytotoxic effect (IC₅₀s is 2.06, 12.57, 9, 18, 4.9, 2.19, 62.48 µM in MCF-1, PANC-1, HCT-116, PC-3, A549, MDA-MB-231 and FR-2 cells, respectively).

Western Blot Analysis^[1]

Cell Line:	BCL-2, BAX, cleaved caspase 9, MCF-7, A549 cells
Concentration:	1, 2, 4, 6 µM
Incubation Time:
Result:	Showed a steady increase in the expression of pro-apoptotic proteins viz. Par-4, apoptotic cascade in BAX and cleaved caspase 9 cells.

Molecular Weight

342.40

Formula

C₂₁H₂₃FO₃

SMILES

[H][C@@]12CC[C@]3(O[C@H]3[C@@]14OC(C(CC5=CC=C(C=C5)F)=C4CC[C@H]2C)=O)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Rasool JU, et al. Palladium catalyzed migratory heck coupling of arteannuin B and boronic acids: An approach towards the synthesis of antiproliferative agents in breast and lung cancer cells. Bioorg Chem. 2022, 122:105694. [Content Brief]

GRP78-IN-1 Related Classifications

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The molarity calculator equation

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

The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GRP78-IN-1HSPApoptosisHeat shock proteinsbreast cancerlung cancertoxicityarteannuin BapoptoticMCF7 cellsA549 cellsInhibitorinhibitorinhibit

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