[CAS NO. 1111556-37-6] Takinib (EDHS-206)

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PRODUCTS SPECIFICATIONS [1111556-37-6]

Catalog

SLK-S8663

Brand

Selleck

CAS

1111556-37-6

DESCRIPTION [1111556-37-6]

Overview

MDL	MFCD11822633
Molecular Weight	322.36
Molecular Formula	C18H18N4O2
SMILES	O=C(C1=CC=CC(C(N)=O)=C1)NC2=NC3=CC=CC=C3N2CCC

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	3.1021 mL	15.5106 mL	31.0212 mL
5 mM	0.6204 mL	3.1021 mL	6.2042 mL
10 mM	0.3102 mL	1.5511 mL	3.1021 mL
50 mM	0.0620 mL	0.3102 mL	0.6204 mL

Description

Takinib (EDHS-206) is a potent and selective inhibitor with an IC50 of 9.5 nM, more than 1.5 log more potent than the second and third ranked targets, (120 nM) and (390 nM), respectively. Takinib induces .

Targets

TAK1 ^[1] (Cell-free assay)	IRAK4 ^[1] (Cell-free assay)	IRAK1 ^[1] (Cell-free assay)
9.5 nM	120 nM	390 nM

In vitro

Takinib is an inhibitor of autophosphorylated and non-phosphorylated TAK1 that binds within the ATP-binding pocket and inhibits by slowing down the rate-limiting step of TAK1 activation. At 10 μM, Takinib shows significant inhibitory activity (<10% enzyme activity after exposure) on six serine/threonine kinases, including TAK1, IRAK4, IRAK1, GCK, CLK2, and MINK1. TAK1/MAP3K7 is most potently inhibited with a half maximal inhibitory concentration (IC50) value of 9.5 nM. In cell models of rheumatoid arthritis and metastatic breast cancer, Takinib treatment results in TNF-a-dependent induction of apoptosis due to inhibition of TAK1 as a key switch between survival and cell death. Takinib does not inhibit any of the MAP2Ks or MAP3Ks family members, i.e., MKK6/MAP2K6, MEKK1/ MAP3K1, MKK1/MAP2K1. Takinib also shows no efficacy toward the TAK1-closely related MAP3K5/ASK1. Takinib potently and selectively targets TAK1 and induces apoptosis in TNF-a-stimulated breast cancer and RA in vitro models.

References

[1] Totzke J, et al. Cell Chem Biol. 2017, 24(8):1029-1039.e7.
[2] Song Z, et al. Proc Natl Acad Sci U S A. 2020 Nov 17;117(46):28980-28991.