Description Features In vitro
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PIK-93

Description Features In vitro
Product Name
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
Formula Weight
389.88
MOL File
593960-11-3.mol
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PIK-93 Property

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
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Safety

WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML0546
Product name
PIK93
Purity
≥98% (HPLC)
Packaging
5mg
Price
$123
Updated
2024/03/01
Sigma-Aldrich
Product number
528122
Product name
PI 3,4-K inhibitor, PIK-93
Packaging
5mg
Price
$335
Updated
2023/01/07
Cayman Chemical
Product number
10009212
Product name
PIK-93
Purity
≥98%
Packaging
1mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
10009212
Product name
PIK-93
Purity
≥98%
Packaging
5mg
Price
$93
Updated
2024/03/01
Sigma-Aldrich
Product number
SML0546
Product name
PIK93
Purity
≥98% (HPLC)
Packaging
25mg
Price
$297.6
Updated
2024/03/01
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PIK-93 Chemical Properties,Usage,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

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PIK-93 Suppliers

Austria 1 China 103 Germany 1 India 1 Ukraine 1 United Kingdom 2 United States 17 Global 126
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
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55
J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
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China
ProdList
94657
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Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
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China
ProdList
6005
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61
Jinan Trio PharmaTech Co., Ltd.
Tel
+86 (531) 88811783
Fax
+86 (531) 55696010 QQ 1762738062
Email
sales@trio-pharmatech.com (International market)
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China
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Xi’an chemsoar Medical Technology Co., ltd
Tel
029-86538357
Fax
029-87871708
Country
China
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234
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57
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
meilunui@163.com
Country
China
ProdList
4727
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58
Hangzhou Sage Chemical Co., Ltd.
Tel
+86057186818502 13588463833
Fax
Pls mail us for more information!
Email
info@sagechem.com
Country
China
ProdList
10266
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Shanghai civi chemical technology co.,Ltd
Tel
86-21-34053660
Fax
86-21-34053661
Email
sale@labgogo.com
Country
China
ProdList
9865
Advantage
52
NCE Biomedical Co.,Ltd.
Tel
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Fax
+86-27-87599188
Country
China
ProdList
1493
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55
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
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61
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View Lastest Price from PIK-93 manufacturers

Career Henan Chemical Co
Product
N-[5-[4-Chloro-3-[[(2-hydroxyethyl)amino]sulfonyl]phenyl]-4-methyl-2-thiazolyl]acetamide 593960-11-3
Price
US $2.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
100kg
Release date
2018-12-23

593960-11-3, PIK-93Related Search:

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  • N-[5-[4-Chloro-3-[[(2-hydroxyethyl)amino]sulfonyl]phenyl]-4-methyl-2-thiazolyl]acetamide
  • PIK 93
  • PI-93
  • AcetaMide, N-[5-[4-chloro-3-[[(2-hydroxyethyl)aMino]sulfonyl]phenyl]-4-Methyl-2-thiazolyl]-
  • PIK-93,PIK93
  • N-[5-[4-Chloro-3-[(2-hydroxyethyl)sulfamoyl]phenyl]-4-methylthiazol-2-yl]acetamide
  • N-[5-[4-Chloro-3-[[(2-hydroxyethyl)amino]sulfonyl]phenyl]-4-methyl-2-thiazolyl]acetamide PIK 93
  • PIK 93 N-[5-[4-Chloro-3-[[(2-hydroxyethyl)amino]sulfonyl]phenyl]-4-methyl-2-thiazolyl]acetamide
  • N-(5-(4-Chloro-3-(N-(2-hydroxyethyl)sulfamoyl)phenyl)-4-methylthiazol-2-yl)acetamide
  • PI 3,4-K inhibitor, PIK-93
  • PI 3,4-K inhibitor, PIK-93 - CAS 593960-11-3 - Calbiochem
  • PIK-93;PIK 93;PIK93
  • N-[5-[4-Chloro-3-[[(2-hydroxyethyl)amino]sulfonyl]phenyl]-4-methyl-2-thiazoly]acetamide
  • CS-426
  • Shokat PI3K/PIK-93
  • PI 3-4-K inhibitor PIK-93 PIK93
  • PI4K,Phosphatidylinositol 4 kinases,PI4 kinases,Phosphoinositide 3-kinase,inhibit,Inhibitor,Virus Protease,PIK93,PIK-93,PI3K
  • N-[5-[4-chloro-3-(2-hydroxyethylsulfamoyl)phenyl]-4-methyl-1,3-thiazol-2-yl]acetamide
  • 593960-11-3
  • Inhibitors
  • Akt
  • mTOR
  • PI3K