PR-619 NEW
| Price | $45 | $55 | $83 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: PR-619 | CAS No.: 2645-32-1 |
| Purity: 99.83% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | PR-619 |
| Description | PR-619 (2,6-Diamino-3,5-dithiocyanopyridine) is a DUB inhibitor that inhibits USP2/4/5/7/8 (EC50=7.2/3.93/8.61/6.86/4.9 μM). PR-619 induces endoplasmic reticulum stress and activates autophagy. |
| Cell Research | 72 h hours later, 0.2 mg/mL resazurin prepared in phosphate-buffered saline is added to each well and the cells are incubated for an additional 3-6 h. The fluorescence of the resazurin reduction product is measured using Ex=535 nm and Em=590 nm filters on a fluorimeter. The EC50 values are calculated in Prism.(Only for Reference) |
| Kinase Assay | Ub-PLA2 assay: Recombinant enzymes in 20 mM Tris-HCl, pH 8.0, 2 mM CaCl2 and 2 mM β-mercaptoethanol (DUB assay buffer) are preincubated with single doses or dose ranges of PR-619 or P22077 for 30 minutes in a 96 well plate before the addition of Ub-PLA2 and NBD C6-HPC. The liberation of a fluorescent product within the linear range of the assay is monitored at room temperature using a fluorescence plate reader. Vehicle (2%(v/v) DMSO) and 10 mM N-ethylmaleimide are included as controls. Where ≥60% inhibition is observed, EC50 values are determined using a sigmoidal dose response equation. |
| In vitro | METHODS: HEK293T cells were treated with PR-619 (5-50 μM) for 6 h. Target protein expression levels were measured by Western Blot. RESULTS: PR-619 interfered with probe labeling at concentrations of 5 μM and above. PR-619 inhibited probe labeling of USP7, but also targeted many other DUBs in the same concentration range, consistent with its broader inhibitory profile. [1] METHODS: The leukemia cell line K562 was treated with PR-619 (40 μM) for 2 h. Targeting was detected by Immunofluorescence. RESULTS: PR-619 induced a different distribution of TOP2A and TOP2B fluorescence signals, consisting of large signal foci. FK2 ubiquitin fluorescence signals partially overlapped with those of TOP2A and TOP2B, as well as SUMO2/3. [2] |
| In vivo | METHODS: To detect anti-tumor activity in vivo, PR-619 (10 mg/kg once daily) and cisplatin (10 mg/kg three times weekly) were intraperitoneally injected into Nude mice bearing T24 or BFTC-905 xenografts for three weeks. RESULTS: The combination of cisplatin and PR-619 showed the most significant antitumor effects on T24 and BFTC-905 xenograft tumors compared to monotherapy. [3] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : < 1 mg/mL (insoluble） |
| Keywords | DUBs | PR619 | PR-619 | tau | G0/G1 | Autophagy | Deubiquitinase | ER-stress | ubiquitination | inhibit | Inhibitor | Apoptosis | arrest |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Sodium 4-phenylbutyrate | L-Ascorbic acid | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Tributyrin | Curcumin | Paeonol | Naringin | Gefitinib |
| Related Compound Libraries | DNA Damage & Repair Compound Library | Bioactive Compound Library | Endoplasmic Reticulum Stress Compound Library | Ubiquitination Compound Library | HIF-1 Signaling Pathway Compound Library | Autophagy Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Cell Cycle Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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