(Z)-TG003


Catalog No. Size PriceQuantity
M15070-2 Contact sales@xcessbio.com for quotation $100

Description

TG003 is a potent and ATP-competitive Cdc2-like kinase (Clk) inhibitor with IC50 of 20 nM, 200 nM, and 15 nM for Clk1, Clk2, and Clk4, respectively. No inhibitory effect on Clk3, SRPK1, SRPK2, or PKC.

Product information

CAS Number: 300801-52-9

Molecular Weight: 249.33

Formula: C13H15NO2S

Chemical Name: (1Z)-1-(3-ethyl-5-methoxy-1, 3-benzothiazol-2-ylidene)propan-2-one

Smiles: CC(=O)/C=C1\SC2=CC=C(C=C2N\1CC)OC

InChiKey: BGVLELSCIHASRV-QPEQYQDCSA-N

InChi: InChI=1S/C13H15NO2S/c1-4-14-11-8-10(16-3)5-6-12(11)17-13(14)7-9(2)15/h5-8H,4H2,1-3H3/b13-7-

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Solubility (25°C). 6 mg/mLwarmed(24.06 mM). Insoluble.

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

TG003 inhibits SF2/ASF-dependent splicing of human β-globin in vitro by suppression of Clk1/Sty-mediated phosphorylation. TG003 inhibits Clk1/Sty kinase activity in mammalian cells, while has no toxic effect on growth of HeLa and COS-7 cells at 10 μM concentration. TG003 blocks IL-1β RNA production by platelets by inhibiting splicing of IL-1β heteronuclear RNA. During 3T3-L1 adipocyte differentiation, TG003 also blocks alternative splicing of PKCβII and expression of PPARγ1 and PPARγ2.

In Vivo:

TG003 (10 μM) rescues the embryonic defects induced by excessive Clk activity in Xenopus.

Products are for research use only. Not for human use.

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