PIP4K-IN-a131
Based on 2 publication(s) in Google Scholar
PIP4K-IN-a131 is PIP4K lipid kinases inhibitor, with IC50s of 1.9 μM and 0.6 μM for purified PIP4K2A and PIP4Ks, respectively. PIP4K-IN-a131 exhibits cancer-selective lethality via dual blockade of the lipid kinase PIP4Ks and mitotic pathways.
For research use only. We do not sell to patients.
- Purity: 99.42%
- CAS No.: 2055405-95-1
- Formula: C20H13N3
- Molecular Weight:295.34
-
Storage:Powder -20°C, 3 years , 4°C, 2 years
* The compound is unstable in solutions, freshly prepared is recommended.
Publications Citing Use of MedChemExpress (MCE) PIP4K-IN-a131
More
Biological Activity
IC50: 1.9 μM (PIP4K2A), 0.6 μM (PIP4Ks)[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | GI50 |
2 μM
Compound: 4a; A131
|
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
|
[PMID: 30015072] |
| AGS | GI50 |
1.1 μM
Compound: 4a; A131
|
Antiproliferative activity against human AGS cells after 72 hrs by MTT assay
Antiproliferative activity against human AGS cells after 72 hrs by MTT assay
|
[PMID: 30015072] |
| ARPE-19 | GI50 |
>10 μM
Compound: 4a; A131
|
Antiproliferative activity against human ARPE19 cells after 72 hrs by MTT assay
Antiproliferative activity against human ARPE19 cells after 72 hrs by MTT assay
|
[PMID: 30015072] |
| AZ-521 cell line | GI50 |
2.4 μM
Compound: 4a; A131
|
Antiproliferative activity against human AZ-521 cells after 72 hrs by MTT assay
Antiproliferative activity against human AZ-521 cells after 72 hrs by MTT assay
|
[PMID: 30015072] |
| BJ | GI50 |
8.1 μM
Compound: 4a; A131
|
Antiproliferative activity against human BJ cells after 72 hrs by MTT assay
Antiproliferative activity against human BJ cells after 72 hrs by MTT assay
|
[PMID: 30015072] |
| DLD-1 | GI50 |
1.2 μM
Compound: 4a; A131
|
Antiproliferative activity against human DLD1 cells after 72 hrs by MTT assay
Antiproliferative activity against human DLD1 cells after 72 hrs by MTT assay
|
[PMID: 30015072] |
| HCT-116 | GI50 |
1.8 μM
Compound: 4a; A131
|
Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
|
[PMID: 30015072] |
| HCT-15 | GI50 |
0.5 μM
Compound: 4a; A131
|
Antiproliferative activity against human HCT15 cells after 72 hrs by MTT assay
Antiproliferative activity against human HCT15 cells after 72 hrs by MTT assay
|
[PMID: 30015072] |
| HeLa | GI50 |
1.4 μM
Compound: 4a; A131
|
Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay
Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay
|
[PMID: 30015072] |
| HGC-27 | GI50 |
1.2 μM
Compound: 4a; A131
|
Antiproliferative activity against human HGC27 cells after 72 hrs by MTT assay
Antiproliferative activity against human HGC27 cells after 72 hrs by MTT assay
|
[PMID: 30015072] |
| HT-29 | GI50 |
0.9 μM
Compound: 4a; A131
|
Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay
Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay
|
[PMID: 30015072] |
| Huh-7 | GI50 |
1.2 μM
Compound: 4a; A131
|
Antiproliferative activity against human HuH7 cells after 72 hrs by MTT assay
Antiproliferative activity against human HuH7 cells after 72 hrs by MTT assay
|
[PMID: 30015072] |
| IM95 | GI50 |
1 μM
Compound: 4a; A131
|
Antiproliferative activity against human IM95 cells after 72 hrs by MTT assay
Antiproliferative activity against human IM95 cells after 72 hrs by MTT assay
|
[PMID: 30015072] |
| IMR-90 | GI50 |
5.8 μM
Compound: 4a; A131
|
Antiproliferative activity against human IMR90 cells after 72 hrs by MTT assay
Antiproliferative activity against human IMR90 cells after 72 hrs by MTT assay
|
[PMID: 30015072] |
| MCF7 | GI50 |
1.2 μM
Compound: 4a; A131
|
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
|
[PMID: 30015072] |
| MDA-MB-231 | GI50 |
1.1 μM
Compound: 4a; A131
|
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay
|
[PMID: 30015072] |
| MKN-45 | GI50 |
1 μM
Compound: 4a; A131
|
Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay
Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay
|
[PMID: 30015072] |
| NUGC-3 | GI50 |
1 μM
Compound: 4a; A131
|
Antiproliferative activity against human NUGC3 cells after 72 hrs by MTT assay
Antiproliferative activity against human NUGC3 cells after 72 hrs by MTT assay
|
[PMID: 30015072] |
| SCH | GI50 |
1.7 μM
Compound: 4a; A131
|
Antiproliferative activity against human SCH cells after 72 hrs by MTT assay
Antiproliferative activity against human SCH cells after 72 hrs by MTT assay
|
[PMID: 30015072] |
| SNU1 | GI50 |
0.9 μM
Compound: 4a; A131
|
Antiproliferative activity against human SNU1 cells after 72 hrs by MTT assay
Antiproliferative activity against human SNU1 cells after 72 hrs by MTT assay
|
[PMID: 30015072] |
| SNU-16 | GI50 |
1 μM
Compound: 4a; A131
|
Antiproliferative activity against human SNU16 cells after 72 hrs by MTT assay
Antiproliferative activity against human SNU16 cells after 72 hrs by MTT assay
|
[PMID: 30015072] |
| SNU-449 | GI50 |
2.3 μM
Compound: 4a; A131
|
Antiproliferative activity against human SNU449 cells after 72 hrs by MTT assay
Antiproliferative activity against human SNU449 cells after 72 hrs by MTT assay
|
[PMID: 30015072] |
| TERT-RPE1 | GI50 |
5.2 μM
Compound: 4a; A131
|
Antiproliferative activity against human hTERT-RPE1 cells after 72 hrs by MTT assay
Antiproliferative activity against human hTERT-RPE1 cells after 72 hrs by MTT assay
|
[PMID: 30015072] |
| U2OS | GI50 |
1.5 μM
Compound: 4a; A131
|
Antiproliferative activity against human U2OS cells after 72 hrs by MTT assay
Antiproliferative activity against human U2OS cells after 72 hrs by MTT assay
|
[PMID: 30015072] |
| WI-38 | GI50 |
3.4 μM
Compound: 4a; A131
|
Antiproliferative activity against human WI38 cells after 72 hrs by MTT assay
Antiproliferative activity against human WI38 cells after 72 hrs by MTT assay
|
[PMID: 30015072] |
PIP4K-IN-a131 (0-100 μM; 72 hours) is a potent antiproliferative agent with a clear selectivity toward cancer cells killing[1].
PIP4K-IN-a131 eliminates cancer cells via a dual-inhibitory mechanism[1].
PIP4K-IN-a131 causes inhibition of the PI3K/Akt/mTOR pathway only in normal BJ cells, but not in transformed counterparts[1].
Inhibition of PIP4Ks by PIP4K-IN-a131 arrests normal cells at the G1/S phase of the cell cycle by suppressing the PI3K/Akt/mTOR signaling pathway via transcriptional upregulation of PIK3IP1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Normal and transformed BJ cells
-
Concentration:0-100 μM (MTT assay)
-
Incubation Time:72 hours
-
Result:Selective killed cancer cells.
-
Cell Line:BJ cells
-
Concentration:5 µM
-
Incubation Time:24 hours
-
Result:Induced the upregulation of PIK3IP1 mRNA levels.
Chemical Information
-
CAS No. 2055405-95-1
-
Appearance Solid
-
Molecular Weight 295.34
-
Formula C20H13N3
-
Color Light yellow to yellow
-
SMILES
N#C/C(C1=CNC2=C1C=CC=C2)=C\C3=CC=CC4=C3C=CN=C4
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years * The compound is unstable in solutions, freshly prepared is recommended.
Publications (2)
-
Journal Impact Factor
-
Most Recent
-
Nat Commun
PIP4K2B is mechanoresponsive and controls heterochromatin-driven nuclear softening through UHRF1. [Abstract]2023 Mar 14;14(1):1432. PMID: 36918565 -
Solvent & Solubility
DMSO : 62.5 mg/mL (211.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (7.04 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (7.04 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * The compound is unstable in solutions, freshly prepared is recommended.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
-
Data Sheet (280 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3859 mL | 16.9296 mL | 33.8593 mL | 84.6482 mL |
| 5 mM | 0.6772 mL | 3.3859 mL | 6.7719 mL | 16.9296 mL | |
| 10 mM | 0.3386 mL | 1.6930 mL | 3.3859 mL | 8.4648 mL | |
| 15 mM | 0.2257 mL | 1.1286 mL | 2.2573 mL | 5.6432 mL | |
| 20 mM | 0.1693 mL | 0.8465 mL | 1.6930 mL | 4.2324 mL | |
| 25 mM | 0.1354 mL | 0.6772 mL | 1.3544 mL | 3.3859 mL | |
| 30 mM | 0.1129 mL | 0.5643 mL | 1.1286 mL | 2.8216 mL | |
| 40 mM | 0.0846 mL | 0.4232 mL | 0.8465 mL | 2.1162 mL | |
| 50 mM | 0.0677 mL | 0.3386 mL | 0.6772 mL | 1.6930 mL | |
| 60 mM | 0.0564 mL | 0.2822 mL | 0.5643 mL | 1.4108 mL | |
| 80 mM | 0.0423 mL | 0.2116 mL | 0.4232 mL | 1.0581 mL | |
| 100 mM | 0.0339 mL | 0.1693 mL | 0.3386 mL | 0.8465 mL |