2. PI3K/Akt/mTOR Apoptosis
  3. PI3K Akt Apoptosis
  4. DHW-208

PI3K-IN-4 是一种强效的泛 PI3K 抑制剂。PI3K-IN-4 对三种 PI3K 亚型均具有高活性，IC50 值为皮摩尔级。PI3K-IN-4 对 PI3Kα (IC50 = 0.20 nM)、PI3Kβ (IC50 = 2.99 nM)、PI3Kδ (IC50 = 0.48 nM) 和 PI3Kγ (IC50 = 0.58 nM) 表现出优异的抑制活性，而对 EGFR 没有显著活性。PI3K-IN-4 通过 PI3K/Akt 信号通路抑制癌细胞生长，进而抑制集落形成并诱导细胞凋亡 (apoptosis)。PI3K-IN-4 可用于肺癌、结肠癌和乳腺癌的相关研究。

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DHW-208

DHW-208 Chemical Structure

CAS No. : 2269470-35-9

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DHW-208 相关抗体

Top Publications Citing Use of Products

查看 PI3K 亚型特异性产品:

查看所有亚型
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

查看 Akt 亚型特异性产品:

查看所有亚型
Akt Akt1 Akt2 Akt3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PI3K-IN-4 is a potent Pan-PI3K inhibitor. PI3K-IN-4 has high activity for three PI3K isoforms with the IC50 values of picomole. PI3K-IN-4 shows superior inhibitory activity against PI3Kα (IC50 = 0.20 nM), PI3Kβ (IC50 = 2.99 nM), PI3Kδ (IC50 = 0.48 nM) and PI3Kγ (IC50 = 0.58 nM) and has no significant activity against EGFR. PI3K-IN-4 inhibits cancer cell growth though PI3K/Akt signaling pathway, leading to the inhibition of colony formation and the induction of apoptosis. PI3K-IN-4 can be used for lung, colon and breast cancer research[1].

IC50 & Target[1]

PI3Kα

0.20 nM (IC50)

PI3Kβ

2.99 nM (IC50)

PI3Kγ

0.58 nM (IC50)

PI3Kδ

0.48 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
3.1 μM
Compound: 7b
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
[PMID: 31097403]
HCT-116 IC50
0.33 μM
Compound: 7b
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
[PMID: 31097403]
HUVEC IC50
19.6 μM
Compound: 7b
Cytotoxicity against HUVEC cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
Cytotoxicity against HUVEC cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
[PMID: 31097403]
L02 IC50
60 μM
Compound: 7b
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
[PMID: 31097403]
MCF7 IC50
0.22 μM
Compound: 7b
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
[PMID: 31097403]
体外研究
(In Vitro)

PI3K-IN-4 (compound 7b) (72 小时) 对典型人类癌细胞表现出抗增殖活性，IC50 值分别为 3.10 μM (A549)、0.33 μM (HCT116) 和 0.22 μM (MCF-7)，且在 HUVEC (IC50 = 19.6 μM) 和 HL7702 正常细胞 (IC50 = 60.0 μM) 中表现出更低的细胞毒性[1]。
PI3K-IN-4 (0.1-10 μM) 能剂量依赖性地降低 Akt 蛋白在 S473 位点的磷酸化水平，并下调 p-Akt/Akt 比率，表明其可能通过 PI3K/Akt 信号通路抑制 MCF-7 细胞生长[1]。
PI3K-IN-4 (0.2-0.8 μM，72 小时) 以剂量依赖性方式抑制 MCF-7 细胞集落形成和增殖[1]。
PI3K-IN-4 (0.2-0.8 μM，48 小时) 诱导 MCF-7 细胞凋亡，并伴有明显的核碎裂和染色质凝聚[1]。
PI3K-IN-4 与 PI3K 形成四个关键氢键，比 Omipalisib (HY-10297) 多一个，这可能有助于其获得更佳的结合稳定性和活性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

DHW-208 相关抗体:

Cell Proliferation Assay[1]

Cell Line: MCF-7 cells
Concentration: 0.2, 0.4 and 0.8 μM
Incubation Time: 72 h
Result: Inhibited the cell proliferation in a dose-dependent manner.
Significantly inhibit colony formation at a concentration of 0.8 μM.

Apoptosis Analysis[1]

Cell Line: MCF-7 cells
Concentration: 0.2, 0.4 and 0.8 μM
Incubation Time: 48 h
Result: Induced cell apoptosis with the highest apoptosis percentage of 27.5 % at 0.8 μM.
Resulted in nuclear fragmentation and condensation of chromatin.
分子量

553.54

Formula

C25H21F2N7O4S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

DHW-208 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DHW-2082269470-35-9DHW208DHW 208PI3KAktApoptosisPhosphoinositide 3-kinasePKBProtein kinase BPan-PI3KPI3KαPI3K/AktapoptosisA549HCT116MCF-7lungcolonbreast cancerInhibitorinhibitorinhibit

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