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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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
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VHL |
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.
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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.
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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