420350
ICMT Inhibitor
The ICMT Inhibitor controls the biological activity of ICMT. This small molecule/inhibitor is primarily used for Cancer applications.
別名:
ICMT Inhibitor, 2-(5-(3-Methylphenyl)-1-octyl-1H-indol-3-yl)acetamide, 2-(1-Octyl-5-m-tolyl-1H-indol-3-yl) acetamide, Cysmethynil, Cysmethynil, Isoprenylcysteine Carboxyl Methyltransferase Inhibitor
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この商品について
実験式（ヒル表記法）:
C25H32N20
分子量:
612.66
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥95% (HPLC)
Form:
semisolid
Storage condition:
OK to freeze, protect from light
Quality Segment
assay
≥95% (HPLC)
form
semisolid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
pale yellow
solubility
DMSO: 100 mg/mL
shipped in
ambient
storage temp.
−20°C
General description
A cell-permeable indole acetamide compound that inhibits Icmt (isoprenylcysteine carboxyl methyltransferase) activity in an acceptor substrate isoprenylated cysteine-competitive (Ki = 0.02 µM; IC50 = 0.29 and 2.1 µM, respectively, with or without inhibitor preincubation; Substrate = S-farnesyl-L-cysteine) and donor substrate AdoMet-noncompetitive manner, exhibiting no activity against FTase, gernaylgeranyltransferase type I, CaaX protease Rce1, AdoMet-dependent DNA methyltransferase, SssI DNA methyltransferase, or PCMT1 protein methyltransferase. Shown to inhibit the proliferation of non-cancer MEF cells (by 100% at 30 µM) and prevent anchorage-independent growth of colon cancer DKOB8 (by >90% at 20 µM) in a dose- and Icmt-dependent manner. Cysmethynil (25 µM) induces G1 cell cycle-arrest and autophagy-mediated, but not apoptotic, cell death in prostate cancer PC3 cells with concomitant PI 3-K/Akt and mTOR signaling blockage, consistent with inhibition of Icmt-mediated activation of Ras and Rheb GTPases. Murine PC3 xenograft studies reveal limited in vivo efficacy (tumor volume on day 28 = 9- and 22-fold of day 0, respectively, with or without 200 mg/kg/i.p. q.o.d.).
A cell-permeable indole acetamide that acts as a substrate-competitive and AdoMet-noncompetitive Icmt (isoprenylcysteine carboxyl methyltransferase) inhibitor (Ki = 0.02 µM; IC50 = 0.29 µM; Substrate = S-farnesyl-L-cysteine), exhibiting no activity against FTase, gernaylgeranyltransferase type I, CaaX protease Rce1, AdoMet-dependent DNA methyltransferase, SssI DNA methyltransferase, or PCMT1 protein methyltransferase. Cysmethynil (25 µM) induces G1 cell cycle-arrest and autophagy-mediated, but not apoptotic, cell death in prostate cancer PC3 cells with concomitant PI 3-K/Akt and mTOR signaling blockage, consistent with inhibition of Icmt-mediated activation of Ras and Rheb GTPases. Murine PC3 xenograft studies reveal limited in vivo efficacy.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C).
Other Notes
Go, M.L., et al. 2010. J. Med. Chem.53, 6838; Wang, M., et al. 2008. J. Biol. Chem.283, 18678; Baron, R.A., et al. 2007. Biochemistry46, 554; Winter-Vann, A.M., et al. 2005. Proc. Natl. Acad. Sci. USA102, 4336.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Regulatory Review (Z)
保管分類
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
420350-10MG: + 420350-MG:
jan
試験成績書（COA）
製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。