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AP20187
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AP20187图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
1mg电议
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
AP20187 (B/B Homodimerizer) 是一种细胞渗透性配体,用于二聚化 FK506 结合蛋白 (FKBP) 融合蛋白并启动生物信号级联和基因表达或破坏蛋白质-蛋白质相互作用。

Cell lines

CHO-AA8-Tet off cells

Preparation method

The solubility of this compound in DMSO is >74.1mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Reaction Conditions

Applications

The cDNAs for the MLL-AF9 fusion protein were transfected in triplicate into CHO cells along with a Myc E box HSV TK luciferase reporter and a CMV-driven Renilla luciferase control plasmid. Results are expressed as a ratio of normalized firefly luciferase activity to the activity of cells transfected with an MSCV neomycin control vector. In the presence of the dimerizer AP20187, cells transfected with MLL-FKBP showed strong dose-dependent transactivation of the Myc E box HSV TK reporter. The dimerization of the fusion protein activated transcription with nearly 250-fold.

Animal models

CD1 mice

Dosage form

Intraperitoneal injection, 10 mg/kg

Applications

To evaluate LFv2IRE expression and tyrosine phosphorylation, CD1 mice were injected via the tail vein with GC of AAV2/8-TBG-LFv2IRE or AAV2/1-MCK-LFv2IRE vector 4 weeks before the AP20187 injection. AP20187-dependent LFv2IRE tyrosine phosphorylation was evident 2 hr after drug administration, peaked 6 hr later, and returned to baseline after 24 hr. Low LFv2IRE basal phosphorylation was detected in liver samples from mice receiving AAV2/8-TBG-LFv2IRE but not stimulated with AP20187, suggesting minimal leakiness of the system.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

产品描述

AP20187 is a small dimerizer drug [1].

To solve the graft-versus-host disease, the in vivo behavior of the transplanted cells should be controlled. AP20187 is used in the conditional system as a chemical inducer of dimerization (CID). Another component is a fusion protein. The CIDs have advantages in gene therapy, it offers the possibility of achieving selection without the toxic effects. In vivo studies show that AP20187 can produces a notable expansion of transduced red cells, platelets, and to a lesser extent, granulocytes [1].

AP20187 is also reported to be used in an AP20187–LFv2IRE system. In this system, AP20187 administration causes the activation of LFv2IRE and results in increased uptake of both hepatic glycogen content and muscular glucose [2].

References:
[1] Neff T, Blau CA. Pharmacologically regulated cell therapy. Blood. 2001 May 1;97(9):2535-40.
[2] Cotugno G, Formisano P, Giacco F, Colella P, Beguinot F, Auricchio A. AP20187-mediated activation of a chimeric insulin receptor results in insulin-like actions in skeletal muscle and liver of diabetic mice. Hum Gene Ther. 2007 Feb;18(2):106-17.