CCT020312
CCT020312 is a potent and selective EIF2AK3 Activator. CCT020312 modulates the biological activity of EIF2AK3. CCT020312 sensitizes cancer cells with defective taxane-induced EIF2A phosphorylation to paclitaxel treatment. CCT020312 is a novel small molecule chemical tool for the selective activation of EIF2A-mediated translation control with utility for proof-of-concept applications in EIF2A-centered therapeutic approaches, and as a chemical starting point for pathway selective agent development. CCT020312 is potent, and EIF2AK3 selective agent and can act as a sensitizer to chemotherapy-associated stresses as elicited by taxanes.
For research use only. We do not sell to patients.
Chemical Information
| Name | CCT020312 |
|---|---|
| Iupac Chemical Name | 6-Bromo-3-[5-(4-bromo-phenyl)-1-(3-diethylamino-propionyl)-4,5-dihydro-1H-pyrazol-3-yl]-4-phenyl-1H-quinolin-2-one |
| Synonyms | CCT020312; CCT-020312; CCT 020312. |
| Molecular Formula | C31H30Br2N4O2 |
| Molecular Weight | 650.40 |
| Smile | O=C1NC2=C(C=C(Br)C=C2)C(C3=CC=CC=C3)=C1C4=NN(C(CCN(CC)CC)=O)C(C5=CC=C(Br)C=C5)C4 |
| InChiKey | OAXDKXMGESZLKV-UHFFFAOYSA-N |
| InChi | 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) |
| CAS Number | 324759-76-4 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| HS Code |
| Targets | |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Stockwell SR, Platt G, Barrie SE, Zoumpoulidou G, Te Poele RH, Aherne GW,
Wilson SC, Sheldrake P, McDonald E, Venet M, Soudy C, Elustondo F, Rigoreau L,
Blagg J, Workman P, Garrett MD, Mittnacht S. Mechanism-based screen for G1/S
checkpoint activators identifies a selective activator of EIF2AK3/PERK
signalling. PLoS One. 2012;7(1):e28568. doi: 10.1371/journal.pone.0028568. PubMed
PMID: 22253692; PubMed Central PMCID: PMC3257223.
2: Bruch J, Xu H, Rösler TW, De Andrade A, Kuhn PH, Lichtenthaler SF, Arzberger
T, Winklhofer KF, Müller U, Höglinger GU. PERK activation mitigates tau pathology
in vitro and in vivo. EMBO Mol Med. 2017 Feb 1. pii: e201606664. doi:
10.15252/emmm.201606664. [Epub ahead of print] PubMed PMID: 28148553.
Chemical Structure
