PIP4K-IN-a131

Name: PIP4K-IN-a131
Brand: MedChemExpress
SKU: HY-136310
Rating: 4.5 (1 reviews)

Cat. No.: HY-136310 Purity: 98.92%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

PIP4K-IN-a131 Chemical Structure

CAS No. : 2055405-95-1

Size	Price	Stock	Quantity
5 mg	USD 260	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 410	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1140	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1700	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE PIP4K-IN-a131

•Nat Commun. 2023 Mar 14;14(1):1432. [Abstract]

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Biological Activity
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References
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Description

IC₅₀ & Target

IC50: 1.9 µM (PIP4K2A), 0.6 µM (PIP4Ks)^[1]

Cellular Effect

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]

In Vitro

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 Proliferation Assay^[1]

Cell Line:	Normal and transformed BJ cells
Concentration:	0-100 μM (MTT assay)
Incubation Time:	72 hours
Result:	Selective killed cancer cells.

RT-PCR^[1]

Cell Line:	BJ cells
Concentration:	5 µM
Incubation Time:	24 hours
Result:	Induced the upregulation of PIK3IP1 mRNA levels.

Molecular Weight

295.34

Formula

C₂₀H₁₃N₃

CAS No.

2055405-95-1

Appearance

Solid

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.

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.3859 mL	16.9296 mL	33.8593 mL
5 mM	0.6772 mL	3.3859 mL	6.7719 mL
10 mM	0.3386 mL	1.6930 mL	3.3859 mL

View the 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: 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.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 98.92%

Select Batch:

Data Sheet (280 KB) SDS (251 KB)

COA (257 KB) LCMS (89 KB)

Handling Instructions (2659 KB)

References

[1]. Mayumi Kitagawa, et al. Dual Blockade of the Lipid Kinase PIP4Ks and Mitotic Pathways Leads to Cancer-Selective Lethality. Nat Commun. 2017 Dec 19;8(1):2200. [Content Brief]

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

PIP4K-IN-a131 Related Classifications

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:

PIP4K-IN-a1312055405-95-1OthersIP4Klipidkinasescancer-selectivemitoticPI3K/Akt/mTORRas/Raf/MEK/ERKRasInhibitorinhibitorinhibit

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PIP4K-IN-a131

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PIP4K-IN-a131 Related Antibodies

1 Publications Citing Use of MCE PIP4K-IN-a131

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Complete Stock Solution Preparation Table

PIP4K-IN-a131 Related Classifications

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