Cas No.: | 115150-59-9 |
Synonyms: | RW-{Me-Phe}-WLM-NH2 |
SMILES: | CC(C)C[C@@H](C(=O)N[C@@H](CCSC)C(=O)N)NC(=O)[C@@H](CC1=CNC2=CC=CC=C21)NC(=O)[C@H](CC3=CC=CC=C3)N(C)C(=O)[C@@H](CC4=CNC5=CC=CC=C54)NC(=O)[C@H](CCCN=C(N)N)N |
Formula: | C49H66N12O6S |
M.Wt: | 951.19 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO |
Description: | Antagonist G is a potent vasopressin antagonist. Antagonist G is also a weak antagonist of GRP and Bradykinin. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy[1][2]. |
In Vitro: | Antagonist G (0-100 μM) induces apoptosis is redox-sensitive and caspase-dependently in SCLC cells[2]. Antagonist G activates JNK1 in SCLC cells[2]. Antagonist G is not intrinsically a free radical oxygen donor but stimulates free radical generation specifically within SCLC cells (6.2-fold) and increases the activity of the redox-sensitive transcription factor AP-1 by 61%[2]. Cell Viability Assay[2] Cell Line: SCLC cell lines NCI-H69, NCI-H510 and CHO-K1 cells. Concentration: 0-100 μM. Incubation Time: 24 h. Result: Inhibited cell growh. |
References: | [1]. P J Woll, et al. A neuropeptide antagonist that inhibits the growth of small cell lung cancer in vitro. Cancer Res. 1990 Jul 1;50(13):3968-73. [2]. A C MacKinnon, et al. [Arg6, D-Trp7,9, NmePhe8]-substance P (6–11) (antagonist G) inducesP-1 transcription and sensitizes cells to chemotherapy. Br J Cancer. 2000 Oct; 83(7): 941–948. |