rG4 WT_AHPC_PEG2
rG4 WT_AHPC_PEG2 is a selective RNA G-quadruplex-based DHX36 PROTAC degrader with a Kd value of 79.7 nM. rG4 WT_AHPC_PEG2 degrades DHX36 via a proteasome-dependent mechanism, without significantly degrading other G4-binding proteins including NCL, DHX9, hnRNP, SRSF and FMR1.
(Pink: Target protein ligand; Blue: VHL ligand (HY-125845); Black: linker).
For research use only. We do not sell to patients.
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
VHL |
In Vitro
rG4 WT_AHPC_PEG2 (15.6-500 nM; 24 h) reduces endogenous APP protein levels in HeLa cells in a concentration-dependent manner, correlating with DHX36 degradation[1].
rG4 WT_AHPC_PEG2 (50-200 nM; 24 h) induces proteasome-dependent degradation of DHX36 and concentration-dependent reduction of Gnai2 protein in mouse C2C12 myoblast cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells
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Concentration:3.75-500 nM (dose-dependent assay); 50 nM (time-dependent assay); 50 nM + 1 μM MG132 (proteasome inhibition assay)
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Incubation Time:24 h (dose-dependent assay); 0-48 h (time-dependent assay); 24 h (proteasome inhibition assay)
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Result:Induced dose-dependent degradation of DHX36, with over 90% degradation observed at 62.5 nM after 24 h, followed by a hook effect at higher concentrations.
Reduced DHX36 by >50% within 6 h of 50 nM treatment, with maximal degradation (~95%) at 48 h.
Blocked DHX36 degradation was observed with co-treatment with MG132, confirming proteasome-dependent activity.
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Cell Line:HeLa cells
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Concentration:15.6-500 nM
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Incubation Time:24 h
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Result:Induced concentration-dependent reduction of endogenous APP protein, which correlated with DHX36 degradation (maximal DHX36 and APP reduction at 62.5 nM).
Caused a slight increase in APP levels at higher concentrations, consistent with the hook effect.
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Cell Line:mouse C2C12 myoblast cells
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Concentration:50-200 nM (dose-dependent assay); 200 nM + 1 μM MG132 (proteasome inhibition assay)
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Incubation Time:24 h
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Result:Induced dose-dependent degradation of DHX36, with significant reduction observed at 100 nM, 150 nM, and 200 nM.
Reduced Gnai2 protein levels in parallel with DHX36 degradation, with significant reduction at 100 nM and 200 nM.
Blocked DHX36 degradation and preserved Gnai2 levels were observed with co-treatment with MG132.
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Cell Line:mouse C2C12 myoblast cells, skeletal muscle stem cells (SCs)
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Concentration:200 nM
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Incubation Time:24 h; 3 h (EdU treatment)
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Result:Reduced the percentage of EdU-positive C2C12 cells from 55.06% to 44.33%.
Reduced the percentage of EdU-positive SCs from 3.70% to 2.47%.
Chemical Information
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Appearance Solid
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Color White to off-white
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SMILES
[rG4 WT_AHPC_PEG2]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Purity & Documentation
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Data Sheet (270 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
rG4 WT_AHPC_PEG2 Related Classifications
HY-185723 Related Classifications
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