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SKLB-0124

Catalog No. TYD-04834 Copy Product Info
🥰Excellent
SKLB-0124 is a potent degrader of PRMT6, exhibiting DC50 values of 15.4 μM in HCC827 cells and 16.4 μM in MDA-MB-435 cells. It does not degrade PRMT1 or PRMT8. SKLB-0124 has an IC50 value of 1.6 μM for PRMT6. It induces proteasome-dependent degradation of PRMT6 and significantly inhibits cell proliferation. Additionally, SKLB-0124 effectively induces apoptosis and cell cycle arrest, making it suitable for research in lung cancer and breast cancer.

SKLB-0124

Copy Product Info
🥰Excellent
Catalog No. TYD-04834

SKLB-0124 is a potent degrader of PRMT6, exhibiting DC50 values of 15.4 μM in HCC827 cells and 16.4 μM in MDA-MB-435 cells. It does not degrade PRMT1 or PRMT8. SKLB-0124 has an IC50 value of 1.6 μM for PRMT6. It induces proteasome-dependent degradation of PRMT6 and significantly inhibits cell proliferation. Additionally, SKLB-0124 effectively induces apoptosis and cell cycle arrest, making it suitable for research in lung cancer and breast cancer.

SKLB-0124
Cas No. 3065966-31-3
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For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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Product Introduction

Bioactivity
Description
SKLB-0124 is a potent degrader of PRMT6, exhibiting DC50 values of 15.4 μM in HCC827 cells and 16.4 μM in MDA-MB-435 cells. It does not degrade PRMT1 or PRMT8. SKLB-0124 has an IC50 value of 1.6 μM for PRMT6. It induces proteasome-dependent degradation of PRMT6 and significantly inhibits cell proliferation. Additionally, SKLB-0124 effectively induces apoptosis and cell cycle arrest, making it suitable for research in lung cancer and breast cancer.
Targets&IC50
PRMT6:15.4 nM (DC50)
In vitro
SKLB-0124 demonstrates non-acute degradation kinetics by degrading PRMT6 at an appropriate rate via the ubiquitin-proteasome system (UPS) pathway in MDA-MB-435 and HCC827 cells (1.25-20 μM, 0.5-7 d), without inducing a hook effect. It inhibits cell proliferation, with IC50 values of 6.66 μM and 5.68 μM for HCC827 and MDA-MB-435 cells, respectively, when used at concentrations of 0-10 μM for 6 days. At concentrations of 10-20 μM for 3 days, SKLB-0124 causes G0/G1 phase arrest in MDA-MB-435 and HCC827 cells in a concentration-dependent manner. Additionally, SKLB-0124 exhibits low toxicity towards normal HEK293 and HEK293T cells at concentrations ranging from 15-90 μM over 9 days.
Chemical Properties
Molecular Weight531.75
FormulaC32H45N5O2
Cas No.3065966-31-3
SmilesO=C(NC1=CC=C(C=C1)C=2C=NC=C(C2)CN(C)CCNC)CCCNC(=O)CC34CC5CC(CC(C5)C3)C4
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year

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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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
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2 Enter the in vivo formulation:
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