2. PI3K/Akt/mTOR
  3. PI3K
  4. Hit20

Hit20 is a PI3Kα selective inhibitor, inhibits PI3Kα kinase activity, suppresses PI3Kα phosphorylation. Hit20 suppresses proliferation, colony formation, migration, and invasion of colon cancer cells. Hit20 can be used for the research of colon cancer.

For research use only. We do not sell to patients.

Hit20

Hit20 Chemical Structure

CAS No. : 536714-52-0

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Hit20 Related Antibodies

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Description

Hit20 is a PI3Kα selective inhibitor, inhibits PI3Kα kinase activity, suppresses PI3Kα phosphorylation. Hit20 suppresses proliferation, colony formation, migration, and invasion of colon cancer cells. Hit20 can be used for the research of colon cancer[1].

In Vitro

Hit20 (10 μM) inhibits PI3Kα kinase activity in a cell-free assay with 40.24% inhibition at 10 μM[1].
Hit20 (0-100 μM; 48 h) inhibits proliferation of HCT-116, MCF-7, A549, and H1299 cells with the highest potency against HCT-116 cells (IC50 7.26 μM)[1].
Hit20 (1, 3, 6 μM; 48 h treatment, 14 days culture) reduces colony formation of HCT-116 cells in a concentration-dependent manner[1].
Hit20 (1, 3, 6 μM; 48 h) inhibits wound healing of HCT-116 cells in concentration- and time-dependent manners[1].
Hit20 (1, 3, 6 μM; 48 h) inhibits migration and invasion of HCT-116 cells in a concentration-dependent manner[1].
Hit20 (3, 6, 9 μM; 48 h) induces apoptosis of HCT-116 cells in a concentration-dependent manner[1].
Hit20 (3, 6, 9 μM; 48 h) modulates expression of apoptosis-related proteins (Caspase-3/9, cleaved Caspase-3/9, Bcl-2, Bax) in HCT-116 cells in a concentration-dependent manner[1].
Hit20 (3, 6, 9 μM; 48 h) inhibits phosphorylation of PI3Kα and Akt in HCT-116 cells in a concentration-dependent manner, suppressing the PI3K/Akt signaling pathway[1].

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

Hit20 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MCF-7, HCT-116, A549, H1299 cells
Concentration: 7.26 μM (IC50, HCT-116); 27.37 μM (IC50, MCF-7); 13.40 μM (IC50, A549); 12.22 μM (IC50, H1299)
Incubation Time: 48 h
Result: Exhibited the highest anti-proliferative activity against HCT-116 cells with an IC50 of 7.26 μM, while showing weaker activity against MCF-7 (IC50 27.37 μM), A549 (IC50 13.40 μM), and H1299 (IC50 12.22 μM) cells.

Cell Proliferation Assay[1]

Cell Line: HCT-116 cells
Concentration: 1, 3, 6 μM
Incubation Time: 48 h (treatment); 14 days (culture)
Result: Reduced colony formation in a concentration-dependent manner; showed lower colony numbers in Hit20-treated groups compared to the control.

Cell Migration Assay[1]

Cell Line: HCT-116 cells
Concentration: 1, 3, 6 μM
Incubation Time: 48 h
Result: Decreased wound healing rates in a concentration- and time-dependent manner; reached 33.66% (1 μM), 26.61% (3 μM), and 24.90% (6 μM) at 48 h compared to the control.

Apoptosis Analysis[1]

Cell Line: HCT-116 cells
Concentration: 3, 6, 9 μM
Incubation Time: 48 h
Result: Increased total apoptosis rates in a concentration-dependent manner; reached 7.14% (3 μM), 10.51% (6 μM), and 17.89% (9 μM) compared to the control’s 5.86%.

Western Blot Analysis[1]

Cell Line: HCT-116 cells
Concentration: 3, 6, 9 μM
Incubation Time: 48 h
Result: Downregulated expression of Caspase-3/9 and Bcl-2, while upregulated cleaved Caspase-3/9 and Bax in a concentration-dependent manner.\nReduced phosphorylation levels of PI3Kα (p85α) and Akt (Ser473) in a concentration-dependent manner, decreased p-PI3K/PI3K and p-Akt/Akt ratios.
Molecular Weight

496.99

Formula

C22H17ClN6O2S2
CAS No.
SMILES

CCC1=NN=C(S1)NC(CSC2=NC3=C(C(N2C4=CC=C(C=C4)Cl)=O)NC5=CC=CC=C53)=O
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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Hit20 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:

Hit20536714-52-0Hit 20Hit-20PI3KPhosphoinositide 3-kinaseCaspase-3/9colon cancerPI3KαBaxMCF-7PI3Kα/Akt signaling pathwayA549HCT-116colon cancer cellsBcl-2Inhibitorinhibitorinhibit

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