An EIF2AK3 activator
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CCT020312

Item No. 36577

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-bromo-3-[5-(4-bromophenyl)-1-[3-(diethylamino)-1-oxopropyl]-4,5-dihydro-1H-pyrazol-3-yl]-4-phenyl-2(1H)-quinolinone
CAS Number
324759-76-4
Molecular Formula
C31H30Br2N4O2
Formula Weight
650.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: SolubleEthanol: Soluble
SMILES
O=C(CCN(CC)CC)N1C(C2=CC=C(Br)C=C2)CC(C3=C(C4=CC=CC=C4)C5=CC(Br)=CC=C5NC3=O)=N1
InChi Code
InChI=1S/C31H30Br2N4O2/c1-3-36(4-2)17-16-28(38)37-27(20-10-12-22(32)13-11-20)19-26(35-37)30-29(21-8-6-5-7-9-21)24-18-23(33)14-15-25(24)34-31(30)39/h5-15,18,27H,3-4,16-17,19H2,1-2H3,(H,34,39)
InChi Key
OAXDKXMGESZLKV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

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    1 mg

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    5 mg

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    Cayman Chemical
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    Product Description

    CCT020312 is an activator of eukaryotic translation initiation factor 2α kinase 3 (EIF2AK3).1 It increases phosphorylation of eIF2α at serine 51 in HT-29 colon carcinoma and MCF-7 breast cancer cells when used at a concentration of 10 µM, an effect not seen in cells transfected with EIF2AK3 siRNA. It reduces phosphorylation of the tumor suppressor retinoblastoma (Rb) protein in HT-29 cells (EC50 = 5.1 µM). CCT020312 (10 µM) rapidly reduces the level of cyclin D1 in HT-29 cells. It also inhibits the growth of HT-29 cells (GI50 = 2.1 µM).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Stockwell, S.R., Platt, G., Barrie, S.E., et al. Mechanism-based screen for G1/S checkpoint activators identifies a selective activator of EIF2AK3/PERK signalling. PLoS One 7(1), e28568 (2012).