PI3K/HDAC-IN-5
PI3K/HDAC-IN-5 is a dual PI3K/HDAC inhibitor. PI3K/HDAC-IN-5 inhibits PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ (IC50 values of 25.41, 134.52, 166.75, and 41.58 nM, respectively) and inhibits downstream PI3K/AKT signaling. PI3K/HDAC-IN-5 inhibits HDAC6, HDAC8, and HDAC11 (IC50 values of 29.35, 157.27, and 382.26 nM, respectively), increases α-tubulin and SMC3 acetylation, while not affecting histone H3/H4 acetylation. PI3K/HDAC-IN-5 induces S phase cell cycle arrest and apoptosis, and inhibits the proliferation of cervical cancer cell lines. PI3K/HDAC-IN-5 can be used for research on cervical cancer.
For research use only. We do not sell to patients.
- CAS No.: 3133922-71-8
- Formula: C22H20N6O3S
- Molecular Weight:448.50
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
PI3Kα 25.41 nM (IC50) |
PI3Kβ 134.52 nM (IC50) |
PI3Kγ 166.75 nM (IC50) |
PI3Kδ 41.58 nM (IC50) |
HDAC6 29.35 nM (IC50) |
HDAC8 157.27 nM (IC50) |
HDAC11 382.26 nM (IC50) |
α-Tubulin |
SMC3 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
2.26 μM
|
Antiproliferative activity against human HeLa cervical cancer cells assessed as viability reduction incubated 48 hrs by CCK-8 assay.
Antiproliferative activity against human HeLa cervical cancer cells assessed as viability reduction incubated 48 hrs by CCK-8 assay.
|
42715866 |
| SiHa | IC50 |
2.66 μM
|
Antiproliferative activity against human SiHa cervical cancer cells assessed as viability reduction incubated 48 hrs by CCK-8 assay.
Antiproliferative activity against human SiHa cervical cancer cells assessed as viability reduction incubated 48 hrs by CCK-8 assay.
|
42715866 |
| Ca-Ski | IC50 |
4.06 μM
|
Antiproliferative activity against human Ca-Ski cervical cancer cells assessed as viability reduction incubated 48 hrs by CCK-8 assay.
Antiproliferative activity against human Ca-Ski cervical cancer cells assessed as viability reduction incubated 48 hrs by CCK-8 assay.
|
42715866 |
| ME-180 | IC50 |
4.61 μM
|
Antiproliferative activity against human ME-180 cervical cancer cells assessed as viability reduction incubated 48 hrs by CCK-8 assay.
Antiproliferative activity against human ME-180 cervical cancer cells assessed as viability reduction incubated 48 hrs by CCK-8 assay.
|
42715866 |
| HEK-293T | IC50 |
16.32 μM
|
Cytotoxicity against human HEK-293T normal cells assessed as viability reduction incubated 48 hrs by CCK-8 assay.
Cytotoxicity against human HEK-293T normal cells assessed as viability reduction incubated 48 hrs by CCK-8 assay.
|
42715866 |
In Vitro
PI3K/HDAC-IN-5 (1.25-5 μM; 48 h) inhibits PI3K/AKT signaling and HDAC6/8 function in HeLa cells without altering histone H3/H4 acetylation[1].
PI3K/HDAC-IN-5 (15 min) preferentially inhibits HDAC6 with an IC50 of 29.35 nM in the cell-free fluorescent HDAC assay[1].
PI3K/HDAC-IN-5 (1 μM; 0-60 min) is rapidly metabolized in mouse liver microsomes with a t1/2 of 14.67 min[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:HeLa cells
-
Concentration:1.25, 2.5, 5 μM
-
Incubation Time:48 h
-
Result:S-phase fraction increased from 31.6% in control to 39.7% at 1.25 μM, 42.8% at 2.5 μM, and 43.6% at 5.0 μM.
G0/G1 fraction decreased from 55.4% in control to 47.6% at 1.25 μM, 44.0% at 2.5 μM, and 41.2% at 5.0 μM.
G2/M fraction was 13.0% in control, 12.7% at 1.25 μM, 13.2% at 2.5 μM, and 15.2% at 5.0 μM.
-
Cell Line:HeLa cells
-
Concentration:1.25, 2.5, 5 μM
-
Incubation Time:48 h
-
Result:Total apoptotic population increased from 3.66% in control to 12.91% at 1.25 μM, 28.84% at 2.5 μM, and 70.40% at 5 μM.
At 5 μM, late apoptosis was 56.60%.
-
Cell Line:HeLa cells
-
Concentration:1.25, 2.5, 5 μM
-
Incubation Time:48 h
-
Result:Markedly reduced phosphorylated PI3K and AKT levels, whereas total PI3K and AKT levels remained unchanged.
Dose-dependently upregulated acetylated SMC3 (Ac-SMC3) and acetylated α-tubulin (Ac-Tubulin).
Acetylation levels of histone H3 (Ac-H3) and H4 (Ac-H4) remained unaltered.
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Apoptosis Solutions
- Protocol for Cell Cycle
- Cell Viability Determination by MTT Colorimetric Assay
Parmacokinetics
Chemical Information
-
CAS No. 3133922-71-8
-
Molecular Weight 448.50
-
Formula C22H20N6O3S
-
SMILES
NC1=CC(C2=NC(C(C3=CC=CC(C(NO)=O)=C3)=CS4)=C4C(N5CCOCC5)=N2)=CN=C1
-
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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PI3K/HDAC-IN-5 Related Classifications
HY-189649 Related Classifications
Powered by Bioz