Pim-1 kinase inhibitor 2

Name: Pim-1 kinase inhibitor 2
Brand: MedChemExpress
SKU: HY-147785
Rating: 4.5 (1 reviews)

Cat. No.: HY-147785 Purity: 99.91%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

Pim-1 kinase inhibitor 2 is a PIM-1 kinase inhibitor with a human IC₅₀ of 0.63 μM. Pim-1 kinase inhibitor 2 exhibits high selectivity for cancer cells over normal cells. Pim-1 kinase inhibitor 2 induces apoptosis, increases active caspase-3 levels, upregulates BAX, downregulates Bcl-2, and elevates the Bax/Bcl-2 ratio. Pim-1 kinase inhibitor 2 suppresses cancer cell proliferation and induces cell cycle arrest. Pim-1 kinase inhibitor 2 can be used for the research of prostate carcinoma, hepatocellular carcinoma, and breast adenocarcinoma.

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

Pim-1 kinase inhibitor 2 Chemical Structure

CAS No. : 2543624-91-3

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
200 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE Pim-1 kinase inhibitor 2

•Adv Sci (Weinh). 2025 Jul 6:e03487. [Abstract]

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PIM1 PIM2 PIM3

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

View All Bcl-2 Family Isoform Specific Products:

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

human PIM1

0.63 μM (IC₅₀)

Caspase 3

Bax

Bcl-2

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	IC₅₀	31.07 μM Compound: 27	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38164076]
MCF7	IC₅₀	19.74 μM Compound: 27	Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay	[PMID: 38164076]
PC-3	IC₅₀	33.45 μM Compound: 27	Anticancer activity against human PC-3 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay Anticancer activity against human PC-3 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay	[PMID: 38164076]
PC-3	IC₅₀	4.82 μM Compound: 34	Antiproliferative activity against human PC-3 cells assessed as reduction in cell growth incubated for 48 hrs by SRB assay Antiproliferative activity against human PC-3 cells assessed as reduction in cell growth incubated for 48 hrs by SRB assay	[PMID: 38071792]

In Vitro

Pim-1 kinase inhibitor 2 (compound 13) (24 h) potently inhibits proliferation of PC3, HepG2, and MCF-7 cancer cells with IC₅₀ values of 4.82 μM, 5.19 μM, and 16.33 μM respectively, and exhibits high selectivity for cancer cells over normal WI-38 cells^[1].
Pim-1 kinase inhibitor 2 potently inhibits PIM-1 kinase with an IC₅₀ of 0.63 μM and 76.43% inhibition at 10 μM^[1].
Pim-1 kinase inhibitor 2 (1.96 μM; 24 h) induces G₂/M phase arrest and increases apoptotic Pre-G₁ phase population in PC3 cells^[1].
Pim-1 kinase inhibitor 2 (1.96 μM; 24 h) induces apoptosis in PC3 cells, with 19.64% total apoptotic cells^[1].
Pim-1 kinase inhibitor 2 increases active caspase-3 levels in PC3 cells to 352.9 Pg/mL, indicating induction of apoptosis^[1].
Pim-1 kinase inhibitor 2 (24 h) upregulates BAX, downregulates Bcl-2, and increases the BAX/Bcl-2 ratio to 115.65 in PC3 cells, promoting apoptosis^[1].

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

Cell Cycle Analysis^[1]

Cell Line:	human prostate carcinoma PC3 cells
Concentration:	1.96 μM
Incubation Time:	24 h
Result:	Reduced the proportion of PC3 cells in G0-G1 phase to 33.72% and S phase to 34.29%. Increased the proportion of PC3 cells in G2/M phase to 31.99% and Pre-G1 (apoptotic) phase to 19.64%, compared to control cells (54.77% G0-G1, 36.41% S, 8.82% G2/M, 1.76% Pre-G1).

Apoptosis Analysis^[1]

Cell Line:	human prostate carcinoma PC3 cells
Concentration:	2.04 μM
Incubation Time:	24 h
Result:	Increases active caspase-3 levels in PC3 cells to 352.9 Pg/mL, indicating induction of apoptosis.

Molecular Weight

406.39

Formula

C₂₄H₁₄N₄O₃

CAS No.

2543624-91-3

Appearance

Solid

Color

brownish yellow

SMILES

N#CC1=C(N=C(C=C1C2=CC=CO2)C3=CC=C(C=C3)N4C(C5=CC=CC=C5C4=O)=O)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 12.5 mg/mL (30.76 mM; ultrasonic and warming and heat to 60°C; 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	2.4607 mL	12.3035 mL	24.6069 mL
5 mM	0.4921 mL	2.4607 mL	4.9214 mL
10 mM	0.2461 mL	1.2303 mL	2.4607 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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 90% Corn Oil
Solubility: ≥ 1.25 mg/mL (3.08 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

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 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: 99.91%

Select Batch:

Data Sheet (276 KB) SDS (251 KB)

COA (250 KB) HNMR (144 KB) RP-HPLC (185 KB) LCMS (101 KB)

Handling Instructions (2659 KB)

References

[1]. Farrag AM, et al. New cyanopyridine-based scaffold as PIM-1 inhibitors and apoptotic inducers: Synthesis and SARs study. Bioorg Chem. 2020;105:104378. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4607 mL	12.3035 mL	24.6069 mL	61.5173 mL
	5 mM	0.4921 mL	2.4607 mL	4.9214 mL	12.3035 mL
	10 mM	0.2461 mL	1.2303 mL	2.4607 mL	6.1517 mL
	15 mM	0.1640 mL	0.8202 mL	1.6405 mL	4.1012 mL
	20 mM	0.1230 mL	0.6152 mL	1.2303 mL	3.0759 mL
	25 mM	0.0984 mL	0.4921 mL	0.9843 mL	2.4607 mL
	30 mM	0.0820 mL	0.4101 mL	0.8202 mL	2.0506 mL