Home Ubiquitin E1 Activating inhibitor DKM 2-93 For research use only.

DKM 2-93

DKM 2-93 is a relatively selective lead inhibitor of ubiquitin-like modifier activating enzyme 5 (UBA5).

DKM 2-93 Chemical Structure

DKM 2-93 Chemical Structure

CAS: 65836-72-8

Purity & Quality Control

Batch: S584101 DMSO] 49 mg/mL] false] Ethanol] 14 mg/mL] false] Water] Insoluble] false Purity: 99.49%
99.49

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Biological Activity

Description DKM 2-93 is a relatively selective lead inhibitor of ubiquitin-like modifier activating enzyme 5 (UBA5).
Targets
UBA5 [1]
In vitro
In vitro DKM 2-93 not only impairs pancreatic cancer cell survival in PaCa2, but also Panc1 cells with 50 % effective concentration values of 90 and 30 μM, respectively[1].
Cell Research Cell lines PaCa2 and Panc1 pancreatic cancer cells
Concentrations --
Incubation Time 48 h
Method

Cells are plated the evening before the experiment, and allowed to adhere overnight. For both survival and proliferation assays, cells are plated in regular media. Before dosing, the media is aspirated from all wells and replaced with the appropriate media and drug dosage. For the chemical genetics screen, cells are treated with either DMSO or the cysteine-reactive fragment for 48 h and cell viability is assessed by Hoescht stain.
In Vivo
In vivo DKM 2-93 daily treatment significantly impairs tumor growth of PaCa2 cells in vivo in tumor xenograft studies in immune-deficient mice without causing any weight loss or overt toxicity[1].
Animal Research Animal Models C.B17 SCID male mice (6-8 weeks old)
Dosages 50 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 243.69 Formula

C11H14ClNO3
CAS No. 65836-72-8 SDF --
Smiles COC1=C(C=C(C=C1)CNC(=O)CCl)OC
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 49 mg/mL ( (201.07 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 14 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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

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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 %

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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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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