2-Methyl-5-nitrobenzenesulfonic acid [(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]methylhydrazide hydrochloride
PIK-75
CAS: 372196-77-5
Molecular Formula: C16H15BrClN5O4S
2-Methyl-5-nitrobenzenesulfonic acid [(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]methylhydrazide hydrochloride - Names and Identifiers
| Name | PIK-75 |
| Synonyms | PFK-15 PIK 75 PIK-75 PIK-75 HCl PIK-75 Hydrochloride (E)-N'-((6-Bromoimidazo[1,2-a]pyridin-3-yl)methylene)-N,2-dimethyl-5-nitrobenzenesulfonohydraz 2-Methyl-5-nitrobenzenesulfonic acid [(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]methylhydrazide hydrochloride (E)-N'-((6-bromoH-imidazo[1,2-a]pyridin-3-yl)methylene)-N,2-dimethyl-5-nitrobenzenesulfonohydrazide hydrochloride 2-Methyl-5-nitrobenzenesulfonic acid [(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]methylhydrazide hydrochloride PIK-75 |
| CAS | 372196-77-5 |
2-Methyl-5-nitrobenzenesulfonic acid [(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]methylhydrazide hydrochloride - Physico-chemical Properties
| Molecular Formula | C16H15BrClN5O4S |
| Molar Mass | 488.7434 |
| Melting Point | >156°C (dec.) |
| Solubility | DMSO (Slightly), Methanol (Slightly) |
| Appearance | Solid |
| Color | Light Beige to Beige |
| Storage Condition | Inert atmosphere,Store in freezer, under -20°C |
| Use | PIK-75 is a p110α inhibitor with IC50 of 5.8 nM (200 times stronger than that on p110β). The subtype-specific mutant in Ser773 also effectively inhibits DNA-PK with IC50 of 2 nM. |
| In vitro study | In combination with purified p110α, PIK-75 is a non-competitive inhibitor with a Ki of 36 nM. PIK-75 also potently inhibited DNA-PK with an IC50 of 2 nM. PIK-75 (1 μm) reduced cell longevity by significantly reducing mitochondrial activity in unstimulated non-asthmatic airway smooth muscle cells (ASM), asthmatic ASM cells, and lung fibroblasts. PIK75 acts on TGFβ-stimulated ASM cells to reduce mitochondrial activity only in asthmatic cells and has no effect on non-asthmatic cells. Recent studies have shown that PIK-75 (10 nM) acts on airway smooth muscle cells (ASM) to inhibit TNF-α-induced CD38 mRNA expression and significantly reduce TNF-α-induced ADP-ribose cyclase activity. in combination with purified p110α, PIK-75 is a non-competitive inhibitor with K I of 36 nM. PIK-75 also potently inhibited DNA-PK with an IC50 of 2 nM. PIK-75 (1 μm) reduced cell longevity by significantly reducing mitochondrial activity in unstimulated non-asthmatic airway smooth muscle cells (ASM), asthmatic ASM cells, and lung fibroblasts. PIK75 acts on TGFβ-stimulated ASM cells to reduce mitochondrial activity only in asthmatic cells and has no effect on non-asthmatic cells. Recent studies have shown that PIK-75 (10 nM) acts on airway smooth muscle cells (ASM) to inhibit TNF-α-induced CD38 mRNA expression and significantly reduce TNF-α-induced ADP-ribose cyclase activity. |
| In vivo study | Action on ErbB3WT tumor model on PIK-75 reduced HRGβ1 chemotaxis and reduced pAkt levels by 40%. In addition, PIK-75 acts on ErbB3WT primary tumors, significantly reducing tumor cell motility, and invasion. PIK-75 acts on CD1 male mice, resulting in severe impairment of insulin tolerance test (ITT) and glucose tolerance test (GTT), and increased glucose production during pyruvate glucose tolerance test (PTT). PIK-75 reduced HRGβ1 chemotaxis and reduced pAkt levels by 40% in the ErbB3WT tumor model. In addition, PIK-75 acts on ErbB3WT primary tumors, significantly reducing tumor cell motility, and invasion. PIK-75 acts on CD1 male mice, resulting in severe impairment of insulin tolerance test (ITT) and glucose tolerance test (GTT), and increased glucose production during pyruvate glucose tolerance test (PTT). |
2-Methyl-5-nitrobenzenesulfonic acid [(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]methylhydrazide hydrochloride - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.046 ml | 10.23 ml | 20.461 ml |
| 5 mM | 0.409 ml | 2.046 ml | 4.092 ml |
| 10 mM | 0.205 ml | 1.023 ml | 2.046 ml |
| 5 mM | 0.041 ml | 0.205 ml | 0.409 ml |
Last Update：2024-01-02 23:10:35
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Product Name: PIK-75 Visit Supplier Webpage Request for quotationCAS: 372196-77-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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