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Key Documents

SML2332

Sigma-Aldrich

Dynarrestin

≥98% (HPLC)

Synonym(s):

4-(4-Diethylaminophenyl)-2-(2,4-difluoro-phenylamino)-thiazole-5-carboxylic acid ethyl ester

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About This Item

Empirical Formula (Hill Notation):
C22H23F2N3O2S
CAS Number:
Molecular Weight:
431.50
UNSPSC Code:
12352200

Assay

≥98% (HPLC)

form

powder

color

white to brown

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

CCN(CC)C1=CC=C(C2=C(C(OCC)=O)SC(NC3=C(F)C=C(F)C=C3)=N2)C=C1

Biochem/physiol Actions

Dynarrestin is a potent and selective reversible inhibitor of cytoplasmic dyneins 1 and 2 that inhibits dynein 1-dependent microtubule binding and motility without affecting ATP hydrolysis. It inhibits endosome movement and disturbs mitosis in cells. Dynarrestin inhibits dynein 2-mediated intraflagellar transport of the cargo IFT88 and flux of Smo within cilia. Also it inhibits cancer cells proliferation downstream of Smo.
Dynarrestin is an aminothiazole derivative, which can bind to protein tyrosine phosphatase interacting protein 51 (PTPIP51). This interaction helps in regulating various signaling pathways that lead to proliferation and migration. Dynarrestin blocks hedgehog (Hh)-dependent signaling in mouse and human cells.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

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Eric Dietel et al.
PloS one, 14(5), e0216642-e0216642 (2019-05-11)
LDC3/Dynarrestin, an aminothiazole derivative, is a recently developed small molecule, which binds protein tyrosine phosphatase interacting protein 51 (PTPIP51). PTPIP51 interacts with various proteins regulating different signaling pathways leading to proliferation and migration. Her2 positive breast cancer cells (SKBR3) express
Susanne Höing et al.
Cell chemical biology, 25(4), 357-369 (2018-02-06)
Aberrant hedgehog (Hh) signaling contributes to the pathogenesis of multiple cancers. Available inhibitors target Smoothened (Smo), which can acquire mutations causing drug resistance. Thus, compounds that inhibit Hh signaling downstream of Smo are urgently needed. We identified dynarrestin, a novel

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