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

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.

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DHW-208

DHW-208 Chemical Structure

CAS No. : 2269470-35-9

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DHW-208 Related Antibodies

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Description

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)

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]
In Vitro

PI3K-IN-4 (compound 7b) (72h) shows antiproliferation activity against typically human cancer cells with IC50 values of 3.10 μM (A549), 0.33 μM (HCT116), and 0.22 μM (MCF-7), and displays much lower cytotoxicity in HUVEC (IC50 = 19.6 μM) and HL7702 normal cells (IC50 = 60.0 μM)[1].
PI3K-IN-4 (0.1-10 μM) decreases the phospho-Akt (S473) in a dose-dependent manner and down-regulated p-Akt/Akt ratio in MCF-7 cells, suggesting it might inhibit MCF-7 cell growth though PI3K/Akt signaling pathway[1].
PI3K-IN-4 (0.2-0.8 μM, 72 h) inhibits colony formation and inhibit the proliferation of MCF-7 cells in a dose-dependent manner[1].
PI3K-IN-4 (0.2-0.8 μM, 48 h) induces apoptosis in MCF-7 cells with markable nuclear fragmentation and condensation of chromatin[1].
PI3K-IN-4 forms four key hydrogen bonds with PI3K, one more than Omipalisib (HY-10297), which may contribute to its superior binding stability and activity[1].

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

DHW-208 Related Antibodies

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.
Molecular Weight

553.54

Formula

C25H21F2N7O4S
CAS No.
SMILES

COC(N=C1)=C(NS(=O)(C2=CC=C(F)C=C2F)=O)C=C1C3=CC=C(N=CN=C4NC5=CN(CCO)N=C5)C4=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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DHW-208 Related Classifications

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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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