[CAS NO. 1381930-17-1]  TBK1/IKKε-IN-4

Ships within Stock Price Qty Total
$0.00
$0.00
Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis
request a quote
If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [1381930-17-1]

Fulfillment
Catalog
AS106976
Brand
Arctom Scientific
CAS
1381930-17-1

DESCRIPTION [1381930-17-1]

Overview

MDL-
Molecular Weight533.62
Molecular FormulaC28H35N7O4
SMILESCOC1=CC=C(N2N=CC3=CN=C(NC4=CC(OCCCN5CCN(C)CC5)=C(OC)C(OC)=C4)N=C32)C=C1

For research use only. We do not sell to patients.

Summary

TBK1/IKKε-IN-4 is a 6-aminopyrazolopyrimidine derivative and a potent, selective TBK1 and IKKε inhibitor with IC 50 values of 13 nM and 59 nM, respectively. TBK1/IKKε-IN-4 shows 100- to 1000-fold less activity against other protein kinases including PDK1, PI3K family members and mTOR [1] .


IC50 & Target

IKKε

59 nM (IC 50 )

TBK1

13 nM (IC 50 )


In Vitro

TBK1/IKKε-IN-4 (Compound II; 96 hours; A549 andHCC44 cells) treatmentdisplays selective toxicity in TBK1-dependent cancer cell lines (IC 50 of ~ 4.2 µM for H441 cells and IC 50 of ~0.4 µM for A549 cells) [1] .
TBK1/IKKε-IN-4 (Compound II; 0-2 µM; 30 minutes; HCC44 cells) treatment inhibits the AKT activity [1] .
TBK1/IKKε-IN-4 (Compound II) inhibits LPS-induced expression of IFNβ (IC 50 =62 nM), and the IFNβ target genes IP10 (IC 50 =78 nM) and Mx1 (IC 50 =20 nM). TBK1/IKKε-IN-4 effectively blocksTLR3-dependent IRF3 nuclear translocation in cells with an IC 50 under 100 nM, but does not impair TNFR1-dependent p65 NFκB nuclear translocation with doses as high as 20 µM [1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis [1]

Cell Line: HCC44 cells
Concentration: 0 µM, 0.5 µM, 1 µM, 2 µM
Incubation Time: 30 minutes
Result: Was sufficient to blunt baseline AKT activity.

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)


Solvent & Solubility

In Vitro:

DMSO : 70 mg/mL ( 131.18 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8740 mL 9.3700 mL 18.7399 mL
5 mM 0.3748 mL 1.8740 mL 3.7480 mL
10 mM 0.1874 mL 0.9370 mL 1.8740 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 4.75 mg/mL (8.90 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 3.5 mg/mL (6.56 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: 3.5 mg/mL (6.56 mM); Suspended solution; Need ultrasonic

* All of the co-solvents are available by MCE.