655200 Sigma-AldrichTX-1123 - CAS 157397-06-3 - Calbiochem
A cell-permeable, reversible, and substrate-competitive arylidene-cyclopentenedione derived tyrphostin that acts as an inhibitor for Src, eEF2-K, and PKA, and EGFR-K/PKC at much higher concentrations.
More>> A cell-permeable, reversible, and substrate-competitive arylidene-cyclopentenedione derived tyrphostin that acts as an inhibitor for Src, eEF2-K, and PKA, and EGFR-K/PKC at much higher concentrations. Less<<TX-1123 - CAS 157397-06-3 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
Synonyms: 2-((3,5-di-tert-Butyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione, PKA Inhibitor XII
Recommended Products
Overview
| Replacement Information |
|---|
Key Spec Table
| CAS # | Empirical Formula |
|---|---|
| 157397-06-3 | C₂₀H₂₄O₃ |
Products
| Catalogue Number | Packaging | Qty/Pack | |
|---|---|---|---|
| 655200-10MGCN | 塑膠安瓿;塑膠針藥瓶 | 10 mg |
| Description | |
|---|---|
| Overview | A cell-permeable, reversible, and substrate-competitive arylidene-cyclopentenedione derived tyrphostin that acts as an inhibitor for Src, eEF2-K, and PKA (IC50 = 2.2, 3.2, and 9.6 µM, respectively), while it inhibits EGFR-K and PKC at much higher concentrations (IC50 = 320 µM). Displays potent antitumor activity (EC50 = 3.66 and 39 µM in HepG2 and HCT116 tumor cells, respectively) with greatly reduced mitochondrial- (≥1000-fold) and hepato-toxicity (≥50-fold) when compared with another tyrphostin, AG 17 (Cat. No. 658425). It is therefore a more promising candidate as a therapeutic agent for cancer treatment. |
| Catalogue Number | 655200 |
| Brand Family | Calbiochem® |
| Synonyms | 2-((3,5-di-tert-Butyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione, PKA Inhibitor XII |
| References | |
|---|---|
| References | Hori, H., et al. 2003. Cell. Mol. Biol. Lett. 8, 528. Hori, H., et al. 2002. Bioorg. Med. Chem. 10, 3257. |
| Product Information | |
|---|---|
| CAS number | 157397-06-3 |
| ATP Competitive | Y |
| Form | Yellow solid |
| Hill Formula | C₂₀H₂₄O₃ |
| Chemical formula | C₂₀H₂₄O₃ |
| Reversible | Y |
| Structure formula Image | |
| Quality Level | MQ100 |
| Applications |
|---|
| Biological Information | |
|---|---|
| Primary Target | Src |
| Primary Target IC<sub>50</sub> | 2.2, 3.2, and 9.6 µM against Src, eEF2-K, and PKA, respectively |
| Purity | ≥95% by HPLC |
| Physicochemical Information | |
|---|---|
| Cell permeable | Y |
| Dimensions |
|---|
| Materials Information |
|---|
| Toxicological Information |
|---|
| Safety Information according to GHS |
|---|
| Safety Information |
|---|
| Product Usage Statements |
|---|
| Packaging Information | |
|---|---|
| Packaged under inert gas | Packaged under inert gas |
| Transport Information |
|---|
| Supplemental Information |
|---|
| Specifications |
|---|
| Global Trade Item Number | |
|---|---|
| Catalogue Number | GTIN |
| 655200-10MGCN | 04055977184709 |
Documentation
TX-1123 - CAS 157397-06-3 - Calbiochem MSDS
| Title |
|---|
TX-1123 - CAS 157397-06-3 - Calbiochem Certificates of Analysis
| Title | Lot Number |
|---|---|
| 655200 |
References
| Reference overview |
|---|
| Hori, H., et al. 2003. Cell. Mol. Biol. Lett. 8, 528. Hori, H., et al. 2002. Bioorg. Med. Chem. 10, 3257. |