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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Androgen Receptor (AR)-R9-AR-PIP
R9-AR-PIP

Chemical Structure : R9-AR-PIP

CAS No.:

R9-AR-PIP (Peptide QLGLGRVY-cc-R9)

货号: PC-24653Not For Human Use, Lab Use Only.

R9-AR-PIP is a small peptide mimicking androgen receptor (AR) PIP-box that inhibit the PCNA/AR interaction, inhibits the expression of AR target genes, AR transcriptional activity and the growth of AR-expressing cells, binds to GFP-PCNA with Kd of 2.73 uM in MST assays.

规格 价格 库存 数量
25 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

R9-AR-PIP is a small peptide mimicking androgen receptor (AR) PIP-box that inhibit the PCNA/AR interaction, inhibits the expression of AR target genes, AR transcriptional activity and the growth of AR-expressing cells, binds to GFP-PCNA with Kd of 2.73 uM in MST assays.
R9-AR-PIP contains eight amino acid residues of the AR PIP-box sequence and nine arginine residues linked with two cystine residues.
R9-AR-PIP inhibited the growth of androgen-dependent LNCaP cells both in the absence and presence of DHT with an IC50 value of 8-10 uM.
R9-AR-PIP inhibits the expression of AR target genes and cell growth.
R9-AR-PIP inhibits AR occupancy at the androgen response element (ARE) in PSA and p21 genes, and expression of AR target genes, and induces cytotoxicity in AR-positive castration-resistant prostate cancer (CRPC) cells.
R9-AR-PIP also significantly inhibits transcriptional activity of AR-FL upon dihydrotestosterone stimulation and the constitutive activity of AR-V7.
R9-AR-PIP inhibits the ARE occupancy by AR-FL and AR-Vs in CCNA2 gene that encodes cyclin A2 and cyclin A2 expression.

物理化学性质&存储条件

分子量 2518.03
分子式 C101H185N49O23S2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Sequence: Glu-Leu-Gly-Leu-Gly-Arg-Val-Tyr-Cys-Cys-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg

参考文献

1. Lu S, et al. Int J Oncol. 2021 Jul;59(1):41.

2. Lu S, et al. Prostate. 2024 Dec;84(16):1456-1467.

3. Lu S, et al. Oncotarget. 2025 May 20;16:383-395.

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