PR-619

SKU: orb1307302

Description

PR-619

Research Area

Cell Biology, Molecular Biology, Protein Biochemistry

Key Properties

• CAS Number: 2645-32-1
• MW: 223.28
• Purity: 99.83%
• Formula: C₇H₅N₅S₂
• SMILES: Nc1nc(N)c(SC#N)cc1SC#N
• Target: Autophagy,DUB,Apoptosis
• Solubility: DMSO:55 mg/mL (246.33 mM)

Bioactivity

• Target IC50:
  USP4:3.93 μM(EC50)|UCHL3:2.95 μM(EC50)|JOSD2:1.17 μM(EC50)|USP8:4.90 μM(EC50)|SENP6 core:2.37 μM(EC50)
• 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 showe the most significant antitumor effects on T24 and BFTC-905 xenograft tumors compared to monotherapy.
• 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 concentration 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. 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.
• Cell Research:
  72 h hours later, 0.2 mg mL resazurin prepared in phosphate-buffered saline is added to each well an the cells are incubated for an additional 3-6 h the fluorescence o the resazurin reduction product is measured using E = 35 nM and E = 90 nM filters on a ffluorimeter the EC50 Values are calculated in Prism.(Only for Reference)

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

G0/G1, ER-stress, Inhibitor, inhibit, JOSD2, Deubiquitinase, DUBs, 2,6-Diamino-3,5-dithiocyanopyridine, Autophagy, arrest, Apoptosis, tau, UCH-L3, ubiquitination, PR619, PR-619, PR 619, SENP6 core, USP4, USP8

Compound Identifiers

PubChem CID

2817763