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Cat. No.: HY-189800

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GRP78-IN-4

GRP78-IN-4 is a GRP78 inhibitor with an IC₅₀ value of 1.1 μM. GRP78-IN-4 induces the unfolded protein response through the PERK/eIF2α/ATF4/CHOP and IRE1/XBP1s signaling pathways. GRP78-IN-4 exhibits cytotoxicity in cancer cell lines. GRP78-IN-4 can be used for research on lung cancer.

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

Formula: C₂₂H₂₈N₄O₃S
Molecular Weight:428.55

Storage:

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

GRP78-IN-4 Chemical Structure

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

IC₅₀ & Target

^[1]

Grp78

1.1 μM (IC₅₀)

eIF2-α

All HSP Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	CC₅₀	3.2 μM	Cytotoxicity against human A549 lung cancer cells assessed as viability reduction incubated 72 hrs by MTT assay. Cytotoxicity against human A549 lung cancer cells assessed as viability reduction incubated 72 hrs by MTT assay.	acs.jmedchem.6c01794

In Vitro

Anti-cancerOthers

Anti-cancer

GRP78-IN-4 (Compound 12) (72 h) selectively kills A549 lung cancer cells with a CC₅₀ of 3.2 μM^[1].

Others

GRP78-IN-4 has an IC₅₀ of 0.6 μM for GRP78 SBD and 1.2 μM for GRP78 FL^[1].
GRP78-IN-4 (0-16 μM) activates the PERK and IRE1 branches of the unfolded protein response (UPR) in A549 cells, increases the phosphorylation level of eIF2α, and upregulates the expression of ATF4 and CHOP as well as the XBP1 splicing product XBP1s^[1].

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

Related Protocols :

Chemical Information

Molecular Weight 428.55
Formula C₂₂H₂₈N₄O₃S
SMILES

O=C(C(N1)=CC2=C1C=CC=C2OC)N[C@@H](CCCC)C(NC3=NC(C(C)C)=CS3)=O
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]. Zhu X, et al. Development of Isoform-Selective GRP78 Inhibitors from a Direct-to-Biology Strategy. Journal of Medicinal Chemistry. 2026 Sep 24;69(18):21421-39.

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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.

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100 mg

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