PIK-75 HCl

製品コードS1205

PIK-75 HCl化学構造

分子量(MW):488.74

PIK-75は1種のp110α阻害剤で、このIC50値が5.8 nM です。PIK-75はp110αに作用する効果がp110βに作用する効果より200倍が高くなります。PIK-75はSer773でアイソフォーム特異性突然変異で、DNA-PKを有効に抑制します。無細胞試験でこのIC50値が2 nMです。

サイズ 価格 在庫  
JPY 10079.16 あり
JPY 21598.20 あり
JPY 53275.56 あり

カスタマーフィードバック(6)

  • A549 cells were treated with DMSO or PIK-75 (200 nM) for 1 h and subsequently stimulated with izTRAIL for 24 h. Long-term survival was visualized after 7 days by crystal violet staining. One of two independent experiments is shown.

    Cell Death Differ 2014 21(3), 491-502. PIK-75 HCl purchased from Selleck.

    A549 cells were treated with PIK-75 (100 nM) or SNS-032 (300 nM) for the indicated times. Cells were lysed and subjected to western blotting. One representative of two independent experiments is shown.

    Cell Death Differ 2014 21(3), 491-502. PIK-75 HCl purchased from Selleck.

  • Knockdown of BRCA1 sensitizes cells to PI3K/AKT pathway inhibitors. MCF7 cells transfected with either BRCA1-siRNA or control-siRNA were treated with increasing amounts of inhibitors targeting the PI3K/AKT pathway for 48 h in triplicate. Viable cells were measured by MTT assay.

    Mol Carcinog 2012 52, 667-75 . PIK-75 HCl purchased from Selleck.

    DW compounds dose-dependently and persistently blocked the PI3K/mTOR signaling pathway in RH30 cells. DW09849 persistently inhibited PI3K signaling. RH30 cells treated with 0.1 uM DW09849 or PIK-75 were harvested at indicated times (0, 0.25, 0.75, 1.5, 3, 6, 12, and 24 hours). Western blot analyses were conducted to detect the indicated proteins. Data shown are representative of three independent experiments. Con, concentration.

    J Pharmacol Exp Ther 2014 348(3), 432-41. PIK-75 HCl purchased from Selleck.

  • Theconcentrations ofatumornecrosis factor-α(TNF-α),binterleukin-6(IL-6), and c macrophage inflammatory protein-2 (MIP-2) in lipopolysaccharide(LPS)-activated RAW264.7 cells measured by enzyme-linked immunosorbent assay. LPS: the LPS (100 ng/mL) group. LPS+V: the LPS plus vasopressin (100 pg/mL) group. LPS+V+LY: the LPS plus vasopressin plus nonspecific PI3K inhibitor LY294002 (10μM) group. LPS+V+PIK: the LPS plus vasopressin plus specific PI3Kαinhibitor PIK-75 (50 nM) group.LPS+V+TGX: the LPS plus vasopressin plus specific PI3Kβ inhibitor TGX-221 (50 nM) group. LPS+V+IC: the LPS plus vasopressin plus specific PI3Kδ inhibitor IC-87114 (5 μM) group. LPS+V+AS: the LPS plus vasopressin plus specific PI3Kγ inhibitor AS252424 (300 nM) group. Data were derived from six culture dishes from each group andexpressed as the means±standard errors. *P< 0.05, the LPS+Vgroup versus the LPS group; #P<0.05, versus the LPS+V group.

    Inflammation, 2017, 40(2):435-441. PIK-75 HCl purchased from Selleck.

    For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of PIK-75 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan.

    Dr. Yong-Weon Yi from Georgetown University Medical Center. PIK-75 HCl purchased from Selleck.

製品安全説明書

PI3K阻害剤の選択性比較

生物活性

製品説明 PIK-75は1種のp110α阻害剤で、このIC50値が5.8 nM です。PIK-75はp110αに作用する効果がp110βに作用する効果より200倍が高くなります。PIK-75はSer773でアイソフォーム特異性突然変異で、DNA-PKを有効に抑制します。無細胞試験でこのIC50値が2 nMです。
特性 PI3K and DNA-PK inhibitor.
ターゲット
DNA-PK [2]
(Cell-free assay)
p110α [1]
(Cell-free assay)
p110γ [1]
(Cell-free assay)
p110δ [1]
(Cell-free assay)
p110β [1]
(Cell-free assay)
2 nM 5.8 nM 76 nM 0.51 μM 1.3 μM
体外試験

PIK-75 shows the impressive potency and isoform selectivity at p110α while the corresponding IC50 values are 1300 nM, 76 nM and 510 nM for other PI3K isoforms, p110β, -γ, and -δ, respectively. Furthermore, when binding to purified p110α, PIK-75 is a noncompetitive inhibitor with respect to ATP with Ki of 36 nM and competitive with respect to the substrate PI with Ki of 2.3 nM. [1] PIK-75 also shows potent inhibition of DNA-PK. [2] PIK-75 (1 μM) reduces cell survival by significantly decreasing mitochondrial activity in unstimulated nonasthmatic airway smooth muscle (ASM) cells, asthmatic ASM cells, and lung fibroblasts. While in TGFβ-stimulated ASM cells, PIK75 only decreases mitochondrial activity in asthmatic cells without effects in nonasthmatic cells. [3] A recent study shows that PIK-75 (10 nM) inhibits TNF-α-induced CD38 mRNA expression and significantly attenuates of TNF-α-induced ADP-ribosyl cyclase activity in human airway smooth muscle cells. [4]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MV4-11 cells MljUR5l1d3SxeHnjxsBie3OjeR?= NGniO3I4OiCq MoHoR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUXY1NTFzIHPlcIx{KGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuT2yxIHHzd4F6NCCLQ{WwQVAvODB|IN88US=> Ml3hNlY{PDl4Mke=
human NZOV9 cells MmjEVJJwdGmoZYLheIlwdiCjc4PhfS=> NGnlb3FCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7aU3Y6KGOnbHzzMEBKSzVyPUCuNFY3KM7:TR?= NVf1ZXRoOTd6Nkm1NlI>
human NZB5 cells M3nHeXBzd2yrZnXyZZRqd25iYYPzZZk> MlTvRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQWlK1JINmdGy|LDDJR|UxRTBwME[5JO69VQ>? NX7VdJY5OTd6Nkm1NlI>

多くの細胞株試験データを見る場合、クリックしてください

体内試験 In the ErbB3WT tumor model, PIK-75 reduces in vitro chemotactic response to HRGβ1 and lowers pAkt levels by 40%. Besides, PIK-75 significantly reduces tumor cell motility and in vivo invasion in ErbB3WT primary tumors. [5] In the CD1 male mice, PIK-75 leads to serious impairments in the insulin tolerance test (ITT) and glucose tolerance test (GTT), and an increase in glucose production during a pyruvate tolerance test (PTT). [6]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

Inhibition Assays:

The PI3K inhibitor PIK-75 is dissolved at 10 mM in dimethyl sulfoxide and stored at −20°C until use. PI3K enzyme activity is determined in 50 μL of 20 mM HEPES, pH 7.5, and 5 mM MgCl2 containing 180 μM phosphatidyl inositol, with the reaction started by the addition of 100 μM ATP (containing 2.5 μCi of [γ-32P]ATP). After a 30-minute incubation at room temperature, the enzyme reaction is stopped by the addition of 50 μL of 1 M HCl. Phospholipids are then extracted with 100 μL of chloroform/methanol [1:1 (v/v)] and 250 μL of 2 M KCl followed by liquid scintillation counting. Inhibitors are diluted in 20% (v/v) dimethyl sulfoxide to generate a concentration versus inhibition of enzyme activity curve, which is then analyzed with the use of Prism version 5.00 for Windows to calculate the IC50. For kinetic analysis, a luminescent assay measuring ATP consumption is used. PI3K enzyme activity is determined in 50 μL of 20 mM HEPES, pH 7.5, and 5 mM MgCl2 with PI and ATP at various concentrations. After a 60-minute incubation at room temperature, the reaction is stopped by the addition of 50 μL of Kinase-Glo followed by a further 15-minute incubation. Luminescence is then read using a Fluostar plate reader. Results are analyzed using Prism.
細胞試験: [3]
+ 展開
  • 細胞株: A2780, A2780/cp70, 2780AD, HCT116, HT29, WIL, CALU-3, MCF7, PC3 and HS852 cells
  • 濃度: 0-10 μM
  • 反応時間: 48 hours
  • 実験の流れ: Mitochondrial activity is assessed after stimulation with TGFβ with or without inhibitors for 48 hours using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium (MTT) assay. Harvested washed cells are resuspended in DMEM-lO% FCS and aliquoted (500 μL) into 24-well cluster plates prior to serial dilution (1:2) in duplicates. To each well, 100 μL of an appropriate MTT concentration (dissolved in PBS and filtered through a 0.2 μm filter before use to remove any blue formazan product) is added immediately after diluting the cells, which are then incubated for 3.5 hours at 37 °C. The resulting blue formazan product is solubilized overnight (16 hours) at 37 °C by the addition of 500 μL of 10% sodium dodecyl sulfate (SDS) in 0.01 M HCl to each well. A sample (150 μL) from each duplicate well is transferred to a 96-well microplate, and the optical density determinedby automated spectrophotometry against a reagent blank (no cells). Absorbance is measured at a test wavelength of 570 nm and a reference wavelength of 690 nm. For each primary cell culture, results from three to six wells from each treatment are averaged, and data are expressed as absorbance 570 to 690 nm.
    (参考用のみ)
動物試験:[5]
+ 展開
  • 動物モデル: MTLn3 cells are injected into the right fourth mammary fat pad from the head of female severe-combined immunodeficient/NCr mice.
  • 製剤: PIK-75 is dissolved in DMSO and then diluted in PBS.
  • 投薬量: ≤1 μM
  • 投与方法: Administered via i.p.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 4 mg/mL (8.18 mM) warming
Water Insoluble
Ethanol Insoluble

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 488.74
化学式

C16H14BrN5O4S.HCl

CAS No. 372196-77-5
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

PI3K信号経路図

PI3K Inhibitors with Unique Features

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID