CRT5
- CAS No.
- 1034297-58-9
- Chemical Name:
- CRT5
- Synonyms
- CRT5;CRT5 (CRT0066051);Benzamide, 3-[6-amino-5-(6-ethoxy-2-naphthalenyl)-3-pyridinyl]-N-[2-(dimethylamino)ethyl]-
- CBNumber:
- CB53067542
- Molecular Formula:
- C28H30N4O2
- Molecular Weight:
- 454.56
- MDL Number:
- MFCD29081160
- MOL File:
- 1034297-58-9.mol
CRT5 price More Price(12)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Cayman Chemical | 18532 | CRT5 ≥98% | 1034297-58-9 | 1mg | $32 | 2024-03-01 | Buy |
Cayman Chemical | 18532 | CRT5 ≥98% | 1034297-58-9 | 5mg | $139 | 2024-03-01 | Buy |
Cayman Chemical | 18532 | CRT5 ≥98% | 1034297-58-9 | 10mg | $243 | 2024-03-01 | Buy |
Cayman Chemical | 18532 | CRT5 ≥98% | 1034297-58-9 | 25mg | $533 | 2024-03-01 | Buy |
TRC | C782015 | CRT5 | 1034297-58-9 | 25mg | $415 | 2021-12-16 | Buy |
CRT5 Chemical Properties,Uses,Production
Description
Protein kinase D (PKD) is a serine/threonine protein kinase that is activated by diacylglycerol, commonly downstream of PKC signaling. The three human PKD isoforms target a variety of proteins to alter cell proliferation, survival, invasion, and protein transport. CRT5 is a pyrazine benzamide that prevents activation of all three isoforms of PKD in endothelial cells treated with VEGF (IC50s = 1, 2, and 1.5 nM for PKD1, PKD2, and PKD3, respectively). It has little effect on a panel of additional kinases when given at 1 μM. CRT5 blocks phosphorylation of PKD1 on Ser916 and PKD2 on Ser876, but does not affect PKC-dependent PKD phosphorylation or PKD autophosphorylation. It also decreases VEGF-induced endothelial migration, proliferation, and tubulogenesis.
Uses
CRT5 is used in the characterization of biological effects of a novel protein kinase D inhibitor in endothelial cells.
in vitro
the non-linear regression analysis revealed that ld50 value of crt5 was 17 μm. the biochemical ic50 value of crt5 for pkd1, pkd2 and pkd3 were 1, 2 and 1.5 nm, respectively [1]. crt5 (1 μm) completely inhibited pkd1 and pkd2, but showed little inhibitory effect on the pkc isoforms. crt5 significantly reduced vegf-induced phosphorylation of hsp27 at the position ser82. crt5 significantly reduced the migratory response towards vegf by 42–51%. crt5 decreased the proliferation of control cells not treated with vegf to a less extent. vegf increased huvec tubule formation in a collagen-based assay. crt5 markedly inhibited vegf-induced tubulogenesis [1].
References
[1] evans i m, bagherzadeh a, charles m, et al. characterization of the biological effects of a novel protein kinase d inhibitor in endothelial cells[j]. biochemical journal, 2010, 429(3): 565-572.
CRT5 Preparation Products And Raw materials
Raw materials
Preparation Products
CRT5 Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
Career Henan Chemica Co | +86-0371-86658258 +8613203830695 | laboratory@coreychem.com | China | 30250 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8474 | 58 |
Shenyang Zhongshen Zekang Biomedical Technology Research Co., Ltd | +86-18341751992 +86-15382112998 | 757984502@qq.com | China | 892 | 58 |
Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
Wuhan Jingkang en Biomedical Technology Co., Ltd | +8613720134139 | orders@jknbiochem.com | China | 5225 | 58 |
Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696,15000506266 15000506266 | China | 4296 | 55 | |
Pharmacodia (Beijing) Co.,Ltd | +86-400-851-9921 | sales@pharmacodia.com | China | 2317 | 55 |
Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9707 | 58 |
ShangHai Biochempartner Co.,Ltd | 17754423994 17754423994 | 2853530910@QQ.com | China | 8014 | 62 |