Ceapin A7

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Description: Selective inhibitor of ATF6α; sensitizes cells to ER stress
Chemical Name: N-[1-[[2,4-bis(Trifluoromethyl)phenyl]methyl]-1H-pyrazol-4-yl]-5-(2-furanyl)-3-isoxazolecarboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews

Biological Activity for Ceapin A7

Ceapin A7 is a selective inhibitor of ATF6α (IC50=0.59 μM). The compound selectively inhibits ATF6α over ATF6β and other branches of the unfolded protein response (UPR). Ceapin A7 inhibits ER stress-induced upregulation of BiP in vitro. Ceapin A7 inhibits cleavage and functional activation of endogenous ATF6 in response to ER stress in vitro.

Technical Data for Ceapin A7

M. Wt 470.33
Formula C20H12F6N4O3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2323027-38-7
PubChem ID 154730128
InChI Key UJTDYOXTXGBHEG-UHFFFAOYSA-N
Smiles FC(F)(C1=CC(C(F)(F)F)=C(C=C1)CN2C=C(C=N2)NC(C3=NOC(C4=CC=CO4)=C3)=O)F

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Ceapin A7

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 47.03 100
ethanol 4.7 10

Preparing Stock Solutions for Ceapin A7

The following data is based on the product molecular weight 470.33. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.13 mL 10.63 mL 21.26 mL
5 mM 0.43 mL 2.13 mL 4.25 mL
10 mM 0.21 mL 1.06 mL 2.13 mL
50 mM 0.04 mL 0.21 mL 0.43 mL

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References for Ceapin A7

References are publications that support the biological activity of the product.

Gallagher et al (2016) Ceapins are a new class of unfolded protein response inhibitors, selectively targeting the ATF6a branch. eLife PMID: 27435960

Gallagher and Walter (2016) Ceapins inhibit ATF6a signaling by selectively preventing transport of ATF6a to the Golgi apparatus during ER stress. eLife PMID: 27435962


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Citations for Ceapin A7

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