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NSC 632839 DUB inhibitor

Name: NSC 632839
Brand: Selleck Chemicals
SKU: S4922
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S4922

NSC 632839 is not only a DUB inhibitor, but also a deSUMOylase inhibitor, it inhibits USP2, USP7, and SENP2 with EC50 of 45 μM, 37 μM, and 9.8 μM, respectively.

Chemical Structure

Molecular Weight: 339.86

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Quality Control

Batch: Purity: 99.65%

99.65

Related Targets	Proteasome E1 Activating E3 Ligase p97 SUMO E2 conjugating
Other DUB Inhibitors	PR-619 P5091 P22077 b-AP15 IU1 ML323 LDN-57444 VLX1570 TCID EOAI3402143

Solubility

In vitro
Batch:

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.35mg/ml (1.03mM)	Taking the 1 mL working solution as an example, add 50 μL of 7 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.11mg/ml (0.32mM)	Taking the 1 mL working solution as an example, add 50 μL of 2.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

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.

Chemical Information, Storage & Stability

Molecular Weight	339.86	Formula	C₂₁H₂₁NO.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	157654-67-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=CC=C(C=C1)C=C2CNCC(=CC3=CC=C(C=C3)C)C2=O.Cl

Mechanism of Action

Features	Less potent than NSC 144303 in inducing apoptosis of E1A and E1A/C9DN cells.
Targets/IC₅₀/Ki	SENP2 (Cell-free assay) 9.8 μM(EC50) USP7 (Cell-free assay) 37 μM(EC50) USP2 (Cell-free assay) 45 μM(EC50)
In vitro	NSC 632839 inhibits purified USP2- and USP7-mediated cleavage of Ub-PLA2. This compound does not inhibit the reporter enzyme PLA2 over the concentration range tested (1.2–150 μM), indicating that the reported inhibition is selective for isopeptidases. It is capable of sustaining caspase-3/caspase-7 activity in the absence of a functional caspase-9 in E1A and E1A/C9DN cells. This chemical induces apoptosis with IC50 of 15.65 μM and 16.23 μM in E1A and E1A/C9DN cells, respectively. It (10 μM) provokes the accumulation of polyubiquitins in E1A cells expressing HA-tagged ubiquitin. It (10 μM) dramatically increases the levels of Noxa and Mcl-1 in E1A cells during a time course analysis. It (10 μM) provokes mitochondrial fragmentation in a higher percentage of cells with an intact outer mitochondrial membrane compared with etoposide.
References	[1] https://pubmed.ncbi.nlm.nih.gov/18424514/ [2] https://pubmed.ncbi.nlm.nih.gov/16982768/

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