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STK16-IN-1 Sale

目录号 : GC32984

An inhibitor of STK16

STK16-IN-1 Chemical Structure

Cas No.:1223001-53-3

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥756.00
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5mg
¥687.00
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10mg
¥1,205.00
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25mg
¥2,543.00
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50mg
¥4,552.00
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100mg
¥8,122.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Kinase experiment:

STK16-IN-1 is generally prepared with 1:3 serial dilutions for 4 concentrations (100 nM, 50 nM, 20 nM, and 10 nM); 6 concentrations are used (1 mM to 10 μM) for ATP competition experiments. The kinase reaction is performed with 1×kinase reaction buffer. Reactions in each well are started immediately by adding ATP and kept going for half an hour under 37°C. After the plate cooled for 5 minutes at room temperature, 5 μL of ADP-Glo reagent is added into each well to stop the reaction and consume the remaining ADP within 40 minutes. At the end, 10 μL of kinase detection reagent is added into the well and incubated for 1 hour to produce a luminescence signal[1].

Cell experiment:

MCF-7, HCT116, HeLa cells are treated with STK16-IN-1 (0, 5, 10 μM) for 72 hours and apoptotic cells are analyzed by flow cytometry using Annexin V/PI apoptosis detection kit[1].

References:

[1]. Liu F, et al. Discovery of a Highly Selective STK16 Kinase Inhibitor. ACS Chem Biol. 2016 Jun 17;11(6):1537-43.

产品描述

STK16-IN-1 is an inhibitor of the serine/threonine kinase STK16 (IC50 = 295 nM).1 It is selective for STK16 over mTOR, PI3Kδ, and PI3Kγ in an enzyme assay (IC50s = 5,560, 856, and 867 nM, respectively) and over 440 additional kinases in a KinomeScan profiling assay. It decreases the growth of MCF-7 cells (GI50 = ~10 ?M) and increases the number of binucleated cells. STK16-IN-1 (2.5-5 ?M) potentiates the antiproliferative effects of colchicine , paclitaxel , doxorubicin , and cisplatin in MCF-7 cells.

1.Liu, F., Wang, J., Yang, X., et al.Discovery of a highly selective STK16 kinase inhibitorACS Chem. Biol.11(6)1537-1543(2016)

Chemical Properties

Cas No. 1223001-53-3 SDF
Canonical SMILES FC1=CC=C(N2C(C(C=CC2=O)=CN3)=C4C3=NC=C4)C=C1C
分子式 C17H12FN3O 分子量 293.3
溶解度 DMSO : 15 mg/mL (51.14 mM) 储存条件 Store at -20°C
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1 mM 3.4095 mL 17.0474 mL 34.0948 mL
5 mM 0.6819 mL 3.4095 mL 6.819 mL
10 mM 0.3409 mL 1.7047 mL 3.4095 mL
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Research Update

The STK16 inhibitor STK16-IN-1 inhibits non-adrenergic and non-neurogenic smooth muscle contractions in the human prostate and the human male detrusor

Naunyn Schmiedebergs Arch Pharmacol 2020 May;393(5):829-842.PMID:31867686DOI:10.1007/s00210-019-01797-x.

Mixed lower urinary tract symptoms (LUTS) (voiding symptoms suggestive of benign prostatic hyperplasia plus storage symptoms, which can be caused by overactive bladder) are common in men. Unwanted contraction of prostate and/or bladder smooth muscle has been implied in the pathophysiology of male LUTS. Here, we examined effects of the serine/threonine kinase 16 (STK16) inhibitor STK16-IN-1 on contraction of human tissues from the prostate and male detrusor. Tissues were obtained from radical prostatectomy and radical cystectomy. Contractions were studied in an organ bath and STK16 expressions by Western blot analyses and fluorescence staining. In prostate tissues, STK16-IN-1 (1 μM) inhibited contractions induced by endothelin-1 and the thromboxane A2 analog U46619. Contractions of prostate tissues induced by noradrenaline, the α1-agonists phenylephrine and methoxamine, or electric field stimulation (EFS) were not changed by STK16-IN-1. In male detrusor tissues, STK16-IN-1 inhibited contractions induced by the cholinergic agonists carbachol and metacholine, and contractions induced by U46619. EFS-induced contractions of detrusor tissues were not changed by STK16-IN-1. Western blot analyses of prostate and detrusor tissues revealed bands matching the molecular weight of STK16. Fluorescence staining of prostate tissues using STK16 antibodies resulted in immunoreactivity in smooth muscle cells. STK16-IN-1 selectively inhibits non-adrenergic/non-neurogenic smooth muscle contractions in the male prostate and to limited extent in the bladder. Because non-adrenergic contractions in the male LUTS may account for limited efficacy of α1-blockers and for α1-blocker-resistant symptoms, studies assessing add-on of STK16-IN-1 to α1-blockers in mixed LUTS appear feasible.

Discovery of a Highly Selective STK16 Kinase Inhibitor

ACS Chem Biol 2016 Jun 17;11(6):1537-43.PMID:27082499DOI:10.1021/acschembio.6b00250.

STK16, a serine/threonine protein kinase, is ubiquitously expressed and is conserved among all eukaryotes. STK16 has been implicated to function in a variety of cellular processes such as VEGF and cargo secretion, but the pathways through which these effects are mediated remain to be elucidated. Through screening of our focused library of kinase inhibitors, we discovered a highly selective ATP competitive inhibitor, STK16-IN-1, which exhibits potent inhibitory activity against STK16 kinase (IC50: 0.295 μM) with excellent selectivity across the kinome as assessed using the KinomeScan profiling assay (S score (1) = 0.0). In MCF-7 cells, treatment with STK16-IN-1 results in a reduction in cell number and accumulation of binucleated cells, which can be recapitulated by RNAi knockdown of STK16. Co-treatment of STK16-IN-1 with chemotherapeutics such as cisplatin, doxorubicin, colchicine, and paclitaxel results in a slight potentiation of the antiproliferative effects of the chemotherapeutics. STK16-IN-1 provides a useful tool compound for further elucidating the biological functions of STK16.