PROTAC hCAII degrader-1
PROTAC hCAII degrader-1 is a potent PROTAC human carbonic anhydrase II (hCAII) degrader with an DC50 of 0.5 nM in HEK293 cells. PROTAC hCAII degrader-1 recruits cereblon (CRBN) E3 ubiquitin ligase to form a ternary complex. PROTAC hCAII degrader-1 enables ubiquitination and subsequent proteasomal degradation of hCAII.
(Pink: CA Ⅱ ligand (HY-B0989); Blue: Cereblon ligand (HY-41547); Black: linker (HY-133388)).
For research use only. We do not sell to patients.
- CAS No.: 2892306-56-6
- Formula: C32H41N5O7S
- Molecular Weight:639.76
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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
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Biological Activity
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hCA II 0.5 nM (DC50) |
PROTAC hCAII degrader-1 (compound Degrader 11) (5 pM-15 μM; 0-48 h) potently degrades hCAII in HEK293 cells with a DC50 of 0.5 nM, DMax of 100%, and sustained activity over 48 h[1].
PROTAC hCAII degrader-1 (50 nM; 6 h) blocks hCAII degradation when co-treated with Lenalidomide (HY-A0003), Acetazolamide (HY-B0782), or MG132 (HY-13259) in HEK293 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells
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Concentration:0.005, 0.05, 0.5, 5, 50, 500, 5000, 10000, 15000 nM
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Incubation Time:0, 2, 6, 12, 24, 48 h
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Result:Resulted in degradation of hCAII at concentrations as low as 50 pM, with near-complete degradation at 5 nM.
Showed no 'hook effect' at concentrations up to 15 μM.
Showed hCAII depletion beginning within 2 h, reaching maximal effect by 6 h, and sustaining degradation for 48 h.
Chemical Information
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CAS No. 2892306-56-6
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Molecular Weight 639.76
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Formula C32H41N5O7S
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SMILES
O=C(C1=CC=C(S(=O)(N)=O)C=C1)NCCCCCCCCCCCCNC2=CC=CC(C(N3C4C(NC(CC4)=O)=O)=O)=C2C3=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 hCAII degrader-1 Related Classifications
HY-179467 Related Classifications
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