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Ro 26-4550 trifluoroacetate Sale

目录号 : GC12565

reversible inhibitor of interleukin-2 (IL-2) binding to its receptor

Ro 26-4550 trifluoroacetate Chemical Structure

Cas No.:1217448-66-2

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10mg
¥4,190.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

IC50: 3 μM

Ro 26-4550 trifluoroacetate is a competitive reversible inhibitor of interleukin-2 (IL-2) binding to its receptor [1].

Interleukin-2 (IL-2) (a 15.5 kDa cytokine) plays a predominant role in the growth of activated T cells. IL-2 induces T-cell proliferation followed by binding on the T-cell surface with picomolar affinity to a heterotrimeric receptor complex (consisting of R, , and chains). It has proven clinically effective as immunosuppressive agents that antibodies recognize the R receptor subunit (IL-2RR) and discrupte IL-2 binding. Small molecules are capable of preventing the IL-2/IL-2RR interaction as potential orally active successors to the antibody drugs [1].

In vitro: The region of IL-2 perturbed by association with Ro 26-4550 was shown to be involved in the binding to IL-2RR. This suggests that Ro 26-4550 competes with IL-2RR for its binding site on IL-2 to interfer with IL-2/IL-2RR binding. [1] .

Analyses of the X-ray structure of Ro 26-4550 binding at the “hot spot” of IL-2 showed that the protein is changeable and then undergo significant rearrangements to create the small molecule binding site. This observation refutes the perception that protein-protein interactions are flat and featureless and indicates that the surface of IL-2 could exist additional nonobvious binding sites (binding a small molecule with high affinity). However, accurate structure-based predictions will be more difficult because of the adaptive nature of the site [2].

In vivo: So far, no study in vivo has been conducted.

Clinical trial: So far, no clinical study has been conducted.

References:
[1].  Tilley JW, Chen L, Fry DC, Emerson SD, Powers GD, Biondi D, Varnell T, Trilles R, Guthrie R, Mennona F, Kaplan G, LeMahieu RA, Carson M, Han R-J, Liu C-M, Palermo R, Ju G. Identification of a small molecule inhibitor of the IL-2/IL-2Rr receptor interaction which binds to IL-2. J. Am. Chem. Soc. 1997, 119, 7589-7590
[2] Braisted AC, Oslob JD, Delano WL, Hyde J, McDowell RS, Waal N, Yu C, Arkin MR, Raimundo BC.  Discovery of a potent small molecule IL-2 inhibitor through fragment assembly. J Am Chem Soc. 2003 Apr 2;125(13):3714-5.

Chemical Properties

Cas No. 1217448-66-2 SDF
化学名 (S)-methyl 2-(2-((R)-1-carbamimidoylpiperidin-3-yl)acetamido)-3-(4-(phenylethynyl)phenyl)propanoate 2,2,2-trifluoroacetate
Canonical SMILES OC(C(F)(F)F)=O.NC(N1CCC[C@H](CC(N[C@H](C(OC)=O)CC2=CC=C(C#CC3=CC=CC=C3)C=C2)=O)C1)=N
分子式 C26H30N4O3.CF3CO2H 分子量 560.57
溶解度 <28.03mg/ml in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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溶解性数据

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1 mM 1.7839 mL 8.9195 mL 17.839 mL
5 mM 0.3568 mL 1.7839 mL 3.5678 mL
10 mM 0.1784 mL 0.8919 mL 1.7839 mL
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