1169755-45-6

1169755-45-6 structure

Name: INDY
Chemical Name: (Z)-1-(3-ethyl-5-hydroxybenzo[d]thiazol-2(3H)-ylidene)propan-2-one
CAS Number: 1169755-45-6
Molecular Formula: C₁₂H₁₃NO₂S
Molecular Weight: 235.30200
Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK DYRK
Create Date: 2016-11-18 15:26:04
Modify Date: 2024-01-09 17:51:22
INDY is a potent and ATP-competitive Dyrk1A and Dyrk1B inhibitor with IC50s of 0.24 μM and 0.23 μM, respectively. INDY binds in the ATP pocket of the enzyme and has a Ki value of 0.18 μM for Dyrk1A. INDY sharply reduces the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells[1][2].

Name	(Z)-1-(3-ethyl-5-hydroxybenzo[d]thiazol-2(3H)-ylidene)propan-2-one
Synonyms	Phencyclidine hydrochloride

Description	INDY is a potent and ATP-competitive Dyrk1A and Dyrk1B inhibitor with IC50s of 0.24 μM and 0.23 μM, respectively. INDY binds in the ATP pocket of the enzyme and has a Ki value of 0.18 μM for Dyrk1A. INDY sharply reduces the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells[1][2].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Protein Tyrosine Kinase/RTK >> DYRK
Target	IC50: 0.24 μM (Dyrk1A) and 0.23 μM (Dyrk1B)[1] Ki: 0.18 μM (Dyrk1A)[1]
In Vitro	INDY (0.3-30 μM; 20 hours) mildly inhibits tau-phosphorylation at 3 μM, and nearly completely inhibits at 30 μM[1]. INDY effectively reverses the aberrant tau-phosphorylation and rescues the repressed NFAT (nuclear factor of activated T cell) signalling induced by Dyrk1A (dual-specificity tyrosine-(Y)-phosphorylation-regulated kinase 1A) overexpression[1]. Western Blot Analysis[1] Cell Line: COS7 cells transfected with either EGFP-Dyrk1A and EGFP-tau Concentration: 0.3, 1, 3, 10, 30 μM Incubation Time: 20 hours Result: Mildly inhibited tau-phosphorylation at 3 μM, and nearly completely inhibited at 30 μM.
In Vivo	ProINDY (2.5 μM) recoveres apparently normal development of the Xenopus embryo[1].
References	[1]. Ogawa Y, et al. Development of a novel selective inhibitor of the Down syndrome-related kinase Dyrk1A. Nat Commun. 2010 Oct 5;1:86. [2]. Pozo N, et al. Inhibition of DYRK1A destabilizes EGFR and reduces EGFR-dependent glioblastomagrowth. J Clin Invest. 2013 Jun;123(6):2475-87.

Molecular Formula	C₁₂H₁₃NO₂S
Molecular Weight	235.30200
Exact Mass	235.06700
PSA	70.47000
LogP	2.07890
Storage condition	-20°C

RIDADR	NONH for all modes of transport

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