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GEM144

Name: GEM144
Brand: TargetMol
SKU: T62916
Price: 61 USD
Availability: InStock
Rating: 5 (10 reviews)

Catalog No. T62916 Copy Product Info

Purity: 98.10%

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GEM144 is a dual inhibitor of DNA polymerase α (POLA1) and HDAC 11. GEM144 induces p53 acetylation, activates p21, arrests the cell cycle in the G1/S phase, and induces apoptosis.

GEM144

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Catalog No. T62916

GEM144 is a dual inhibitor of DNA polymerase α (POLA1) and HDAC 11. GEM144 induces p53 acetylation, activates p21, arrests the cell cycle in the G1/S phase, and induces apoptosis.

Cas No. 2487526-28-1

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Pack Size	Price	USA Stock	Global Stock
1 mg	$61	-	In Stock
5 mg	$97	-	In Stock
10 mg	$143	-	In Stock
25 mg	$242	-	In Stock
50 mg	$378	-	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:98.10%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	GEM144 is a dual inhibitor of DNA polymerase α (POLA1) and HDAC 11. GEM144 induces p53 acetylation, activates p21, arrests the cell cycle in the G1/S phase, and induces apoptosis.
Targets&IC50	H2AX:0.1–0.4 μM, NCI-H460 cells:0.26 μM, MM473 cells:1.4 μM, A2780 cells:0.95 μM, HDAC11:8.23 μM
In vitro	GEM144 (0-10 μM; 24 hours) exhibits antiproliferative activity in tested cancer cell lines with IC50s of 0.26 ~ 2.2 μM[1]. GEM144 (0.1 - 0.4 μM; 24 hours) strongly increases levels of H2AX phosphorylation on Ser 39 (γH2AX), and strongly upregulates p21 expression in a dose-dependent manner[1]. GEM144 (0.26 μM in NCI-H4609, 0.95 μM in A2780 and 1.4 μM in MM473; 72 hours) induced G1/S cell cycle arrest[1]
In vivo	GEM144 (50 mg/kg; p.o., bid, 5 days a week, for 3-4 weeks) significantly reduces tumor burden of MM487 with TGI of 72% in xenografts mice[1].

Chemical Properties

Molecular Weight	461.55
Formula	C₂₈H₃₁NO₅
Cas No.	2487526-28-1
Smiles	O(C(C(NO)=O)C)C1=C(C23CC4CC(C2)CC(C3)C4)C=C(C=C1)C5=CC=C(/C=C/C(O)=O)C=C5

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 200 mg/mL (433.32 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1666 mL	10.8331 mL	21.6661 mL	108.3306 mL
5 mM	0.4333 mL	2.1666 mL	4.3332 mL	21.6661 mL
10 mM	0.2167 mL	1.0833 mL	2.1666 mL	10.8331 mL
20 mM	0.1083 mL	0.5417 mL	1.0833 mL	5.4165 mL
50 mM	0.0433 mL	0.2167 mL	0.4333 mL	2.1666 mL
100 mM	0.0217 mL	0.1083 mL	0.2167 mL	1.0833 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

GEM144

GEM144

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