PR-619

Name: PR-619
Brand: GlpBio
SKU: GC13208
Availability: InStock
Rating: 5 (30 reviews)

رقم الكتالوجGC13208

PR-619 is a broad-spectrum DUB (deubiquitinating enzyme) inhibitor. PR-619 has demonstrated robust DUB inhibitory activity (5-20 µM) and growth inhibitory activity with IC₅₀ of 2 µM in HEK 293T cells..

Products are for research use only. Not for human use. We do not sell to patients.

Cas No.: 2645-32-1

الحجم السعر المخزون الكميّة

5mg
29٫00
متوفر

10mM (in 1mL DMSO)
58٫00
متوفر

25mg
75٫00
متوفر

100mg
204٫00
متوفر

Tel：(909) 407-4943 Email: sales@glpbio.com

مراجعات العميل

بناء على آراء العملاء.

GlpBio Citations
GlpBio Citations

Bioactive Compounds Premium Provider
Bioactive Compounds Premium Provider

Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Bba Mol Basis Dis 1870.1 (2024): 166891.

Description Protocol Chemical Properties Product Documents

Product Documents

Quality Control & SDS

View current batch:

Purity: >98.50%
COA (Certificate Of Analysis)

SDS (Safety Data Sheet)

Datasheet

Purity: >98.00%
COA (Certificate Of Analysis)

SDS (Safety Data Sheet)

Datasheet

Protocol

Cell experiment [1]:

Cell lines

Preparation Method

T24 and BFTC-905 cells were treated with various concentrations of PR-619 (3-15 µM) for 24 h, 48 h, and 72 h, respectively. Cell viability was assessed using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay.

Reaction Conditions

3-15 µM；24 h, 48 h, and 72 h

Applications

PR-619 effectively induced cytotoxicity and apoptosis in both T24 and BFTC cells in a dose- and time-dependent manner. Additionally, we found that PR-619 induced cytotoxicity in low-grade RT-4 UC cells and cisplatin-resistant UC cells (T24/R) in a dose- and time-dependent manner.

Animal experiment [2]:

Animal models

8-week-old male nude mice

Preparation Method

A total of 5 × 10⁵ JJ012 or SW1353 cells were suspended in 200 µL of serum-free medium and an equal amount of Matrigel. The cell suspension thus derived was then injected subcutaneously into the dorsal side of 8-week-old male nude mice. When the tumor grew to ~150 mm3, mice were randomly assigned to either the PR-619 treatment group or the control group. Mice in the treatment group received PR-619 10 mg/kg intraperitoneal injection twice daily for 48 days. Mice in the untreated control group received an injection of DMSO solution.

Dosage form

10 mg/kg; i.p.

Applications

PR-619 showed significant anti-tumor effects on xenograft tumors from both cell lines.

References:

[1] Kuo KL, et al. The Deubiquitinating Enzyme Inhibitor PR-619 Enhances the Cytotoxicity of Cisplatin via the Suppression of Anti-Apoptotic Bcl-2 Protein: In Vitro and In Vivo Study. Cells. 2019 Oct 17;8(10):1268.
[2] Lin WC, et al. Anti-tumor effects of deubiquitinating enzyme inhibitor PR-619 in human chondrosarcoma through reduced cell proliferation and endoplasmic reticulum stress-related apoptosis. Am J Cancer Res. 2023 Jul 15;13(7):3055-3066.

PR-619 is a broad-spectrum DUB (deubiquitinating enzyme) inhibitor. PR-619 has demonstrated robust DUB inhibitory activity (5-20 µM) and growth inhibitory activity with IC₅₀ of 2 µM in HEK 293T cells^[1].
PR-619 at 40 µM induced an above-background TOP2A and TOP2B signal in K562 cells^[2]. In vitro efficacy test shown that the anti-tumor effects of PR-619 on the JJ012 and SW1353 human chondrosarcoma cell lines, with PR-619 concentrations ranging from 2.5 to 17.5 µM for 24 and 48 h. PR-619 significantly reduced the viability of chondrosarcoma cells in a dose- and time-dependent manner^[3]. In vitro, PR-619 treatment (0 - 80 µM) significantly inhibited cell viability at 24 and 48 h in a dose-dependent manner. Furthermore, PR-619 (20 µM) treatment for 48 h significantly induced apoptosis in cisplatin-resistant T24/R cells^[4].
In vivo, mice were intraperitoneally treated with PR-619 (10 mg/kg each day) enhanced the antitumor effect of cisplatin in a xenograft mouse model of T24/R^[4].
Altun M, et al. (2011) Activity-based chemical proteomics accelerates inhibitor development for deubiquitylating enzymes. Chem Biol 18:1401-1412.
Cowell IG, et al. The Deubiquitinating Enzyme Inhibitor PR-619 is a Potent DNA Topoisomerase II Poison. Mol Pharmacol. 2019 Nov;96(5):562-572.
Lin WC, et al. Anti-tumor effects of deubiquitinating enzyme inhibitor PR-619 in human chondrosarcoma through reduced cell proliferation and endoplasmic reticulum stress-related apoptosis. Am J Cancer Res. 2023 Jul 15;13(7):3055-3066.
[4] Hsu FS, et al. PR-619, a General Inhibitor of Deubiquitylating Enzymes, Diminishes Cisplatin Resistance in Urothelial Carcinoma Cells through the Suppression of c-Myc: An In Vitro and In Vivo Study. Int J Mol Sci. 2021 Oct 28;22(21):11706.
References:

Cas No. 2645-32-1 SDF

Chemical Name (2,6-diamino-5-thiocyanatopyridin-3-yl) thiocyanate

Canonical SMILES C1=C(C(=NC(=C1SC#N)N)N)SC#N

Formula C₇H₅N₅S₂ M.Wt 223.28

الذوبان ≥ 11.15mg/mL in DMSO Storage Store at -20°C

General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.

Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution

1 mg 5 mg 10 mg

1 mM 4.4787 mL 22.3934 mL 44.7868 mL

5 mM 0.8957 mL 4.4787 mL 8.9574 mL

10 mM 0.4479 mL 2.2393 mL 4.4787 mL

حاسبة المولارية

حاسبة التخفيف

كتلة

=

تركيز

x

مقدار

x

ميغاواط *

** عند إعداد حلول المخزون، دائمًا استخدم الوزن الجزيئي الخاص بالدفعة للمنتج على ملصق القارورة MSDS / CoA (متوفر عبر الإنترنت).

احسب

التركيز (البداية)

x

حجم الصوت (البداية)

=

التركيز (النهائي)

x

حجم الصوت (النهائي)

C₁

V₁

C₂

V₂

احسب

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

مراجعات

Review for PR-619

Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

5 Star

100%

4 Star

0%

3 Star

0%

2 Star

0%

1 Star

0%

Review for PR-619

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

Overall Rating

★

★

★

★

★

Review Title

المراجعة

اللقب

البريد الإلكتروني

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.

Cell experiment [1]:
Cell lines
Preparation Method	T24 and BFTC-905 cells were treated with various concentrations of PR-619 (3-15 µM) for 24 h, 48 h, and 72 h, respectively. Cell viability was assessed using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay.
Reaction Conditions	3-15 µM；24 h, 48 h, and 72 h
Applications	PR-619 effectively induced cytotoxicity and apoptosis in both T24 and BFTC cells in a dose- and time-dependent manner. Additionally, we found that PR-619 induced cytotoxicity in low-grade RT-4 UC cells and cisplatin-resistant UC cells (T24/R) in a dose- and time-dependent manner.
Animal experiment [2]:
Animal models	8-week-old male nude mice
Preparation Method	A total of 5 × 10⁵ JJ012 or SW1353 cells were suspended in 200 µL of serum-free medium and an equal amount of Matrigel. The cell suspension thus derived was then injected subcutaneously into the dorsal side of 8-week-old male nude mice. When the tumor grew to ~150 mm3, mice were randomly assigned to either the PR-619 treatment group or the control group. Mice in the treatment group received PR-619 10 mg/kg intraperitoneal injection twice daily for 48 days. Mice in the untreated control group received an injection of DMSO solution.
Dosage form	10 mg/kg; i.p.
Applications	PR-619 showed significant anti-tumor effects on xenograft tumors from both cell lines.
References: [1] Kuo KL, et al. The Deubiquitinating Enzyme Inhibitor PR-619 Enhances the Cytotoxicity of Cisplatin via the Suppression of Anti-Apoptotic Bcl-2 Protein: In Vitro and In Vivo Study. Cells. 2019 Oct 17;8(10):1268. [2] Lin WC, et al. Anti-tumor effects of deubiquitinating enzyme inhibitor PR-619 in human chondrosarcoma through reduced cell proliferation and endoplasmic reticulum stress-related apoptosis. Am J Cancer Res. 2023 Jul 15;13(7):3055-3066.

Cas No.	2645-32-1	SDF
Chemical Name	(2,6-diamino-5-thiocyanatopyridin-3-yl) thiocyanate
Canonical SMILES	C1=C(C(=NC(=C1SC#N)N)N)SC#N
Formula	C₇H₅N₅S₂	M.Wt	223.28
الذوبان	≥ 11.15mg/mL in DMSO	Storage	Store at -20°C
General tips	Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition	Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Prepare stock solution
		1 mg	5 mg	10 mg
	1 mM	4.4787 mL	22.3934 mL	44.7868 mL
	5 mM	0.8957 mL	4.4787 mL	8.9574 mL
	10 mM	0.4479 mL	2.2393 mL	4.4787 mL