PROTAC HMGCR Degrader-2
PROTAC HMGCR Degrader-2 is a HMGCR PROTAC degrader with an IC50 value of 0.25 μM. PROTAC degrades HMGCR-2 in Insig-silenced HepG2 cells with a DC50 of 0.12 μM. PROTAC HMGCR Degrader-2 takes PROTAC HMGCR Degrader-1 (HY-171823) as the oral prodrug. PROTAC HMGCR Degrader-2 degrades HMGCR by the VHL-dependent ubiquitin-proteasome system and reduces cellular cholesterol in HepG2 cells. PROTAC CDK2/4/6 Degrader-2 can be used for hyperlipidemia research.
(Pink: HMG-CoA Reductase (HMGCR) ligand (HY-122439); Blue: VHL ligand (HY-125845); Black: linker (HY-W014831)).
For research use only. We do not sell to patients.
- CAS No.: 2715104-46-2
- Formula: C53H79N5O10S
- Molecular Weight:978.29
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Biological Activity
Description
IC50 & Target
[1]|
VHL |
In Vitro
PROTAC HMGCR Degrader-2 (compound 21c) (0.01-3 μM, 16 h) preferentially acts as HMGCR inhibitors over degraders at high doses in HepG2 cells, achieves a maximum degradation (Dmax) of 65% at a high dose of 1 μM[1].
PROTAC HMGCR Degrader-2 (0.1 μM, 24 h) reduces cellular cholesterol in HepG2 cells[1].
PROTAC HMGCR Degrader-2 (0.01-3 μM, 0-48 h) induces PROTAC-mediated HMGCR degradation in In sig-silenced HepG2 cells with a DC50 of 0.12 μM, and achieved a Dmax of 76% at 1 μM[1].
PROTAC HMGCR Degrader-2 (1 μM, 6 h) binds simultaneously to HMGCR and VHL, and subsequently degraded HMGCR by the VHL-dependent ubiquitin-proteasome system in Insig-silenced HepG2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HepG2 cells
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Concentration:0.01, 0.03, 0.1, 0.3, 1 and 3 μM
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Incubation Time:16 h
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Result:Attenuated the upregulation of HMGCR at low doses and increased HMGCR expression at high doses.
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Cell Line:HepG2 cells
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Concentration:0.01 μM
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Incubation Time:24 h
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Result:Reduced cellular cholesterol protein expression.
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Cell Line:Insig-silenced HepG2 cells
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Concentration:0.01, 0.03, 0.1, 0.3, 1 and 3 μM
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Incubation Time:0, 4, 8, 16, 24 and 48 h
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Result:Effectively degraded the HMGCR protein at a dose manner concentration and 16 h.
Elevated HMGCR expression at higher concentration of 3 μM.
Reduced HMGCR protein level in a time-dependent manner at 1 μM.
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Cell Line:HepG2 cells
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Concentration:1 μM
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Incubation Time:16 h
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Result:Effectively attenuated the compensatory upregulation of HMGCR.
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Cell Line:Insig-silenced HepG2 cells
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Concentration:1 μM
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Incubation Time:16 h
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Result:Induced HMGCR degradation, which was significantly blocked by the addition of VHL032 (10 μM) or MG132 (10 μM) (HY-13259).
Induced HMGCR degradation reduced by lovastatin (HY-N0504).
Chemical Information
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CAS No. 2715104-46-2
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Molecular Weight 978.29
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Formula C53H79N5O10S
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SMILES
O=C(N1[C@@H](C[C@H](C1)O)C(NCC2=CC=C(C3=C(N=CS3)C)C=C2)=O)[C@H](C(C)(C)C)NC(CCCCCCCCCCNC(O[C@@H]4[C@@]5([H])C(C=C[C@@H]([C@@H]5CC[C@@H](O)C[C@@H](O)CC(O)=O)C)=C[C@@H](C4)C)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC HMGCR Degrader-2 Related Classifications
HY-181134 Related Classifications
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