2. Metabolic Enzyme/Protease
  3. Ser/Thr Protease
  4. PCSK9 degrader 1

PCSK9 degrader 1 (Compound 16) is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows high affinity to PCSK9 with a Ki of 107 nM. PCSK9 degrader 1 can involve in a protein-protein interaction with the low-density lipoprotein (LDL) receptor.

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PCSK9 degrader 1 Chemical Structure

PCSK9 degrader 1 Chemical Structure

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Based on 1 publication(s) in Google Scholar

PCSK9 degrader 1 Related Antibodies

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Description

PCSK9 degrader 1 (Compound 16) is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows high affinity to PCSK9 with a Ki of 107 nM. PCSK9 degrader 1 can involve in a protein-protein interaction with the low-density lipoprotein (LDL) receptor[1].

IC50 & Target

Ki: 107 nM (PCSK9)[1]
In Vitro

PCSK9 degrader 1 (Compound 16; 1.25-20 μM; 24 hours; HEK293 cells) treatment shows a clear concentration-dependent degradation of both the pro and mature form of PCSK9 yielding a half-maximal degradation concentration of 4.8 and 3.4 μM, as well as a maximum percentage of degradation at 20 μM of 58% and 61%, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PCSK9 degrader 1 Related Antibodies

Western Blot Analysis[1]

Cell Line: HEK293 cells
Concentration: 1.25 μM, 2.5 μM, 5 μM, 10 μM or 20 μM
Incubation Time: 24 hours
Result: Showed a clear concentration-dependent degradation of both the pro and mature form of PCSK9 yielding a half-maximal degradation concentration of 4.8 and 3.4 μM, as well as a maximum percentage of degradation at 20 μM of 58% and 61%, respectively.
Molecular Weight

1077.22

Formula

C53H69FN8O13S
Appearance

Solid

Color

White to off-white

SMILES

OC(C(C=C1)=CC=C1C(C(F)=C2)=CC=C2OC(C(OCCOCCNC([C@@H](NC(OC(C)(C)C)=O)CCCN/C(NC(OC(C)(C)C)=O)=N/C(OC(C)(C)C)=O)=O)=C3)=CC4=C3CCN[C@]4(C)CC(NC5=NC=CS5)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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PCSK9 degrader 1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PCSK9 degrader 1Ser/Thr ProteaseSerine proteasesSerine endopeptidasesThreonine proteasesInhibitorinhibitorinhibit

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