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.
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- Formule: C22H28N4O3S
- Masse moléculaire:428.55
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
[1]|
Grp78 1.1 μM (IC50) |
eIF2-α |
Cellular Effect
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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
GRP78-IN-4 (Compound 12) (72 h) selectively kills A549 lung cancer cells with a CC50 of 3.2 μM[1].
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.
Chemical Information
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Masse moléculaire 428.55
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Formule C22H28N4O3S
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SMILES
O=C(C(N1)=CC2=C1C=CC=C2OC)N[C@@H](CCCC)C(NC3=NC(C(C)C)=CS3)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)