[CAS NO. 1315355-93-1] NG25
PRODUCTS SPECIFICATIONS [1315355-93-1]
DESCRIPTION [1315355-93-1]
Overview
| MDL | MFCD19443255 |
|---|---|
| Molecular Weight | 537.58 |
| Molecular Formula | C29H30F3N5O2 |
| SMILES | O=C(NC1=CC(C(F)(F)F)=C(CN(CC2)CCN2CC)C=C1)C3=CC(OC4=C5C(NC=C5)=NC=C4)=C(C)C=C3 |
22 Publications Citing Use of MCE
- [1]Nat Cell Biol. 2017 Oct;19(10):1248-1259.
- [2]Cell Death Differ. 2019 Dec;26(12):2520-2534.
- [3]J Cell Biol. 2018 Aug 6;217(8):2727-2742.
- [4]Oncogene. 2017 Oct 5;36(40):5620-5630.
- [5]Sci Signal. 2018 Jul 10;11(538). pii: eaan5850.
- [6]Cell Death Dis. 2022 Apr 30;13(4):421.
- [7]J Immunol. 2015 Aug 1;195(3):1100-11.
- [8]Biofactors. 2020 Sep;46(5):813-820.
- [9]J Am Heart Assoc. 2021 Feb 16;10(4):e014311.
- [10]J Cell Mol Med. 2020 Sep;24(18):10946-10957.
- [11]J Mol Cell Cardiol. 2021 Feb;151:31-43.
- [12]Sci Rep. 2016 Sep 7;6:32737.
- [13]Biochem Biophys Res Commun. 2014 Oct 10;453(1):106-11.
- [14]Mol Med Rep. 2018 Jan;17(1):1710-1716.
- [15]BMC Res Notes. 2022 Nov 26;15(1):352.
- [16]Oncotarget. 2021 Oct 12;12(21):2158-2168.
- [17]Institut für Zellbiologie und Immunologie der Universität Stuttgart. 2020 Sep.
- [18]Faculty of Medicine and Health Sciences, Department of Clinical and Molecular Medicine. 2020 Jul.
- [19]Oncotarget. 2017 Nov 1;8(61):104330-104346.
- [20]Oncotarget. 2016 Oct 25;7(43):69173-69187.
- [21]School of Medicine. University of North Carolina. 2016.
- [22]Harvard Medical School LINCS LIBRARY
Summary
NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC 50 s of 149 nM and 21.7 nM, respectively.
IC50 & Target
|
MAP4K2 21.7 nM (IC 50 ) |
TAK1 149 nM (IC 50 ) |
LYN 12.9 nM (IC 50 ) |
GSK 56.4 nM (IC 50 ) |
ABL,ARG 75.2 nM (IC 50 ) |
FER 82.3 nM (IC 50 ) |
SRC 113 nM (IC 50 ) |
|
|
Eph B2 672 nM (IC 50 ) |
ZAK 698 nM (IC 50 ) |
Eph A2 773 nM (IC 50 ) |
Eph B4 999 nM (IC 50 ) |
ZC1/HGK 3250 nM (IC 50 ) |
RAF1 7590 nM (IC 50 ) |
||
In Vitro
NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC 50 s of 149 nM and 21.7 nM, respectively. NG25 also potently suppresses several kinases such as LYN, CSK, FER, p38α, ABL,ARG and SRC, with IC 50 s of 12.9, 56.4, 82.3, 102, 75.2, and 113 nM, respectively [1] . NG25 is very potent suppressor of CpG B- or CpG A-stimulated secretion of IFNα and CL097-stimulated secretion of IFNβ, with complete inhibition by 400 nM [2] . NG25 treatment reduces cell viability of all tested breast cancer cell lines in a dose dependent manner. NG25 (2 μM) enhances the cytotoxic effect of Dox on breast cancer cells [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 93.01 mM ; Need ultrasonic)
H 2 O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.8602 mL | 9.3009 mL | 18.6019 mL |
| 5 mM | 0.3720 mL | 1.8602 mL | 3.7204 mL |
| 10 mM | 0.1860 mL | 0.9301 mL | 1.8602 mL |
References
- [1] Tan L, et al. Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2). J Med Chem. 2015 Jan 8;58(1):183-96.
- [2] Pauls E, et al. Essential role for IKKβ in production of type 1 interferons by plasmacytoid dendritic cells. J Biol Chem. 2012 Jun 1;287(23):19216-28.
- [3] Wang Z, et al. TAK1 inhibitor NG25 enhances doxorubicin-mediated apoptosis in breast cancer cells. Sci Rep. 2016 Sep 7;6:32737.
