PIK-93
- CAS No.
- 593960-11-3
- Chemical Name:
- PIK-93
- Synonyms
- PI-93;PIK 93;CS-426;PIK-93,PIK93;Shokat PI3K/PIK-93;PIK-93;PIK 93;PIK93;PI 3,4-K inhibitor, PIK-93;PI 3-4-K inhibitor PIK-93 PIK93;PI 3,4-K inhibitor, PIK-93 - CAS 593960-11-3 - Calbiochem;N-[5-[4-Chloro-3-[(2-hydroxyethyl)sulfamoyl]phenyl]-4-methylthiazol-2-yl]acetamide
- CBNumber:
- CB22484673
- Molecular Formula:
- C14H16ClN3O4S2
- Molecular Weight:
- 389.88
- MDL Number:
- MFCD12922510
- MOL File:
- 593960-11-3.mol
| storage temp. | 2-8°C |
|---|---|
| solubility | DMSO: soluble15mg/mL, clear |
| form | powder |
| color | white to beige |
| InChIKey | JFVNFXCESCXMBC-UHFFFAOYSA-N |
| CAS DataBase Reference | 593960-11-3 |
PIK-93 price More Price(25)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML0546 | PIK93 ≥98% (HPLC) | 593960-11-3 | 5mg | $123 | 2024-03-01 | Buy |
| Sigma-Aldrich | 528122 | PI 3,4-K inhibitor, PIK-93 | 593960-11-3 | 5mg | $335 | 2023-01-07 | Buy |
| Cayman Chemical | 10009212 | PIK-93 ≥98% | 593960-11-3 | 1mg | $32 | 2024-03-01 | Buy |
| Cayman Chemical | 10009212 | PIK-93 ≥98% | 593960-11-3 | 5mg | $93 | 2024-03-01 | Buy |
| Sigma-Aldrich | SML0546 | PIK93 ≥98% (HPLC) | 593960-11-3 | 25mg | $297.6 | 2024-03-01 | Buy |
PIK-93 Chemical Properties,Uses,Production
Description
PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM; shown to inhibit PI3Kα with IC50 of 39 nM.
Features
A novel and potent inhibitor of both PI3Kγ and PI4KIIIβ.
In vitro
PIK-93 inhibits PI3Kγ and PI4KIIIβ, with IC50 values of 16 nM and 19 nM, respectively. PIK-93 also inhibits other members of PI3Ks, including PI3Kα, β, and δ, with IC50 values of 39 nM, 0.59 μM, and 0.12 μM, respectively. PIK-93 shows no obvious inhibitory effect against a panel of other kinases, even at a concentration of 10 μM. In differentiated HL60 (dHL60) cells, PIK-93 (0.5 μM–1 μM) impairs consolidation and stability of the leading edge formed after treatment with uniform f-Met-Leu-Phe (fMLP). PIK-93 alters the localization, but not the amount, of the fMLP-dependent accumulation of total F-actin. In fMLP gradients, PIK-93 reduces the chemotactic index and triples the cells' turning frequency. In COS-7 cells, PIK-93 (250 nM) effectively abrogates the accumulation of CERT-PH domain and FL-Cer in Golgi. PIK-93 of the same concentration also significantly inhibits the conversion of [3H]serine-labeled endogenous ceramide to sphingomyelin. These facts indicate a key role of PI4KIIIβ in ceramide transport between the ER and Golgi, as well as in the regulation of spingomyelin synthesis. In T6.11 cells, PIK-93 (300 nM) reduces carbachol-induced translocation of TRPC6 to the plasma membrane and net Ca2+ entry. A recent report shows that PIK-93 has anti-enterovirus effects, as revealed by its inhibition of both poliovirus (PV) and hepatitis C virus (HCV) replication, with EC50 values of 0.14 µM and 1.9 µM, respectively.
Description
PIK-93 is an inhibitor of phosphatidylinositol 4-kinase IIIβ (PI4KIIIβ; IC50 = 19 nM). It is selective for PI4KIIIβ over PI4KIIIα and PI4KIIα (IC50s = 1,100 and >100,000 nM, respectively). However, it also inhibits the PI3K catalytic subunits (IC50s = 39, 590, 120, and 16 nM for p110α, p110β, p110δ, and p110γ, respectively). PIK-93 reduces enteroviral RNA replication when used at a concentration of 125 nM in HeLa cells. It also inhibits the transport of ceramide from the endoplasmic reticulum to the Golgi apparatus.
Uses
PIK 93 is a PI3Kγ and PI4KIIIβ inhibitor.
Enzyme inhibitor
This potent and selective PI3Kγ/PI4KIIIβ inhibitor (FW = 389.88; CAS 593960-11-3; Solubility (25°C): 78 mg/mL DMSO, <1 mg/mL Water), also known as N-[5-[4-chloro-3-[(2-hydroxyethyl)sulfamoyl]phenyl]-4- methylthiazol-2-yl]acetamide, impairs actin filament consolidation and stability at the leading edge in cells treated with N-formyl-Met-Leu-Phe as well as ceramide transport between ER and Golgi compartments. The inhibition of PI3K by PIK-93, LY294002, or wortmannin decreased carbachol-induced translocation of TRPC6 to the plasma membrane and carbachol-induced net Ca2+ entry into T6.11 cells. PIK-93 inhibits both poliovirus (PV) and hepatitis C virus (HCV) replication, with EC50 values of 0.14 μM and 1.9 μM, respectively. Targets: PI3Kγ, IC50 = 16 nM; PI4KIIIβ, IC50 = 19 nM; PI3Kα, IC50 = 39 nM; PI3Kδ, IC50 = 0.12 μM; and PI3Kβ, IC50 = 0.59 μM.
target
PI3Kγ
References
[1] monet m, francoeur n, boulay g. involvement of phosphoinositide 3-kinase and pten protein in mechanism of activation of trpc6 protein in vascular smooth muscle cells. j biol chem. 2012 may 18;287(21):17672-81.
[2] tóth b, balla a, ma h et al. phosphatidylinositol 4-kinase iiibeta regulates the transport of ceramide between the endoplasmic reticulum and golgi. j biol chem. 2006 nov 24;281(47):36369-77.
[3] hsu, n. y., et al. 2010. viral reorganization of the secretory pathway generates distinct organelles for rna replication. cell 141:799-811.
[4] arita m, kojima h, nagano t et al. phosphatidylinositol 4-kinase iii beta is a target of enviroxime-like compounds for antipoliovirus activity. j virol. 2011 mar;85(5):2364-72.
PIK-93 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 | sales@capotchem.com | China | 29797 | 60 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| career henan chemical co | +86-0371-86658258 | sales@coreychem.com | China | 29914 | 58 |
| Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 967 | 58 |
| Hubei xin bonus chemical co. LTD | 86-13657291602 | linda@hubeijusheng.com | CHINA | 22968 | 58 |
| Chongqing Chemdad Co., Ltd | +86-023-61398051 +8613650506873 | sales@chemdad.com | China | 39916 | 58 |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 47465 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| Dayang Chem (Hangzhou) Co.,Ltd. | 571-88938639 +8617705817739 | info@dycnchem.com | CHINA | 52867 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
View Lastest Price from PIK-93 manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
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2019-07-06 | N-[5-[4-Chloro-3-[[(2-hydroxyethyl)amino]sulfonyl]phenyl]-4-methyl-2-thiazolyl]acetamide
593960-11-3
|
US $2.00 / kg | 1kg | 99% | 100kg | Career Henan Chemical Co |
-
- N-[5-[4-Chloro-3-[[(2-hydroxyethyl)amino]sulfonyl]phenyl]-4-methyl-2-thiazolyl]acetamide
593960-11-3
- US $2.00 / kg
- 99%
- Career Henan Chemical Co