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PRN694

Catalog No. T16578 CAS 1575818-46-0

PRN694 shows extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo. PRN694 is an irreversible, highly selective, and effective covalent interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) dual inhibitor (IC50s: 0.3 nM and 1.4 nM, respectively).

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PRN694, CAS 1575818-46-0

Pack Size	Availability	Price/USD
25 mg	10-14 weeks	$ 7,140.00
50 mg	10-14 weeks	$ 9,280.00
100 mg	10-14 weeks	$ 13,400.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description	PRN694 shows extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo. PRN694 is an irreversible, highly selective, and effective covalent interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) dual inhibitor (IC50s: 0.3 nM and 1.4 nM, respectively).
Targets&IC50	RLK:1.4 nM, BLK:125 nM, BTK:17 nM, JAK3:30 nM, BMX:17 nM, ITK:0.3 nM, TEC:3.3 nM
In vitro	PRN694 obviously decreases NK cell FcR-induced killing at concentrations exceeding 0.37 μM. PRN694 inhibits TEC, BTK, BMX, BLK, JAK3 with IC50s of 3.3, 17, 17, 125, 30 nM, respectively. Immunoblot analysis of TCR activation pathways shows that PRN694 blocks activation or nuclear translocation of NFAT1, JunB, pIκBα, and pERK. Results display inhibition of Ca2+ signaling with PRN694 at all concentrations above 1 nM. Day 6 flow cytometry analysis reveals that PRN694 significantly inhibits the anti-CD3/CD28-induced proliferation of both CD4 and CD8 T-cells (p<0.01)[1].
In vivo	RN694 treatment also causes obviously lower weights relative to the vehicle (p<0.05). Colitis studies show reduced numbers of CD4+ T cells present in the colonic epithelium of PRN694-treated mice compare with controls. The PRN694 occupancy of ITK is 98, 95, and 54% at 1, 6, and 14 h, respectively. The concentrations of PRN694 in the plasma are 2.8, 0.66, and 0.027 μM at 1, 6, and 14 h, respectively. At 14 h, the plasma level of PRN694 is over 10 fold lower than the IC50 in whole blood [1][2].

Molecular Weight	543.67
Formula	C28H35F2N5O2S
CAS No.	1575818-46-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 125 mg/mL (229.92 mM), Sonication and heating are recommended.

References and Literature

1. Zhong Y, et al. Targeting interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) using a novel covalent inhibitor PRN694. J Biol Chem. 2015 Mar 6;290(10):5960-78. 2. Cho HS, et al. A Small Molecule Inhibitor of ITK and RLK Impairs Th1 Differentiation and Prevents Colitis Disease Progression. J Immunol. 2015 Nov 15;195(10):4822-31.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

PRN694 1575818-46-0 Others PRN 694 PRN-694 inhibitor inhibit

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