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KDM5-IN-1

Catalog No. T15649Cas No. 1628210-26-3

KDM5-IN-1 is an effective and selective inhibitor of KDM5 with an IC50 of 15.1 nM.

KDM5-IN-1

KDM5-IN-1

Purity: 98.08%
Catalog No. T15649Cas No. 1628210-26-3
KDM5-IN-1 is an effective and selective inhibitor of KDM5 with an IC50 of 15.1 nM.
Pack SizePriceAvailabilityQuantity
1 mg$58In Stock
5 mg$196In Stock
10 mg$298In Stock
25 mg$475In Stock
50 mg$678In Stock
100 mg$912In Stock
500 mgInquiryIn Stock
1 mL x 10 mM (in DMSO)$139In Stock
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Purity:98.08%
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Product Introduction

Bioactivity
Description
KDM5-IN-1 is an effective and selective inhibitor of KDM5 with an IC50 of 15.1 nM.
Targets&IC50
PC9 H3K4Me3:(EC50)0.34 μM, KDM5:15.1 nM
In vitro
KDM5-IN-1 is significantly less potent against other KDM enzymes (1A, 2B, 3B, 4C, 5A, 6A, 7B), inhibiting KDM4C the strongest with an IC50 of 1.9 μM. KDM5-IN-1 potently inhibits KDM5B and KDM5C isoforms (IC50 of 4.7 and 65.5 nM, respectively)[1].
In vivo
KDM5-IN-1(50 mg/kg; oral) shows an unbound maximal plasma concentration Cmax>15-fold over its cell EC50 in vivo[1].
Chemical Properties
Molecular Weight324.38
FormulaC17H20N6O
Cas No.1628210-26-3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 30 mg/mL (92.48 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.0828 mL15.4140 mL30.8280 mL154.1402 mL
5 mM0.6166 mL3.0828 mL6.1656 mL30.8280 mL
10 mM0.3083 mL1.5414 mL3.0828 mL15.4140 mL
20 mM0.1541 mL0.7707 mL1.5414 mL7.7070 mL
50 mM0.0617 mL0.3083 mL0.6166 mL3.0828 mL

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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 mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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