PROTAC IRAK3 degrader-1
PROTAC IRAK3 degrader-1 is a potent and selective IRAK3 degrader with a DC50 of 0.002 μM. PROTAC IRAK3 degrader-1 induces proteasome-dependent degradation of IRAK3 via ternary complex formation with IRAK3 and CRBN. PROTAC IRAK3 degrader-1 can be used for cancer research.
(Pink: IRAK3 Target protein ligand; Blue: Cereblon ligand (HY-14658); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 2712600-00-3
- Formula: C47H63N11O6
- Molecular Weight:878.07
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
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IRAK3 5 nM (IC50) |
IRAK4 1.4 μM (IC50) |
PROTAC IRAK3 degrader-1 (compound 23) potently and selectively binds to recombinant IRAK3 with an IC50 of 5 nM, with 280-fold selectivity over IRAK4[1].
PROTAC IRAK3 degrader-1 binds to recombinant CRBN with an IC50 of 460 nM[1].
PROTAC IRAK3 degrader-1 shows primary selectivity for recombinant IRAK3 in a 400-kinase panel, with weaker inhibition of CDK11, CDK8, TRKC, and GSG2[1].
PROTAC IRAK3 degrader-1 selectively binds to IRAK3 in a chemoproteomic assay, with an apparent binding constant of 34 nM and >20-fold selectivity over all other detected targets[1].
PROTAC IRAK3 degrader-1 (0.0003-10 μM; 2-48 h) potently degrades IRAK3 in THP1 cells, sustained degradation[1].
PROTAC IRAK3 degrader-1 (0.1 μM; 8 h) selectively decreases IRAK3 protein levels in THP1 cells, with only minimal off-target effects on DHCR24 and no degradation of IKZF1, GSPT1, IRAK1, or IRAK4[1].
PROTAC IRAK3 degrader-1 (0.3 μM; 8-32 h) induces significant, sustained IRAK3 degradation in primary human macrophages, and this activity is unaffected by LPS stimulation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP1 monocytic cancer cells
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Concentration:0.0003; 0.001; 0.003; 0.01; 0.03; 0.1; 0.3; 1; 3; 10 μM
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Incubation Time:2; 4; 6; 8; 16; 24; 48 h
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Result:Induced potent IRAK3 degradation with a DC50 of 2 nM and maximum degradation (Dmax) of 98% after 16 h.
Achieved maximal degradation at 0.1 μM after 24 h.
Detected degradation as early as 2 h after treatment with 0.1 μM, which persisted up to 48 h.
Allowed full IRAK3 recovery 24 h after compound washout.
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Cell Line:THP1 monocytic cancer cells
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Concentration:0.1; 0.3; 1; 3; 10 μM
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Incubation Time:6; 24 h
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Result:Fully rescued IRAK3 degradation when cells were pretreated with proteasome inhibitor MG132 or NEDD8-activating enzyme inhibitor MLN4924.
Prevented IRAK3 degradation when cells were pretreated with excess IRAK3 ligand 5 or thalidomide.
Chemical Information
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CAS No. 2712600-00-3
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Molecular Weight 878.07
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Formula C47H63N11O6
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SMILES
O=C1C2=CC(N3CCN(CC3)CCC4CCN(CC4)C(CCC(N5CCN([C@@]6([H])CC[C@H](CC6)NC7=NC=NN8C7=C(C(C)C)C=C8)CC5)=O)=O)=CC=C2C(N1C9C(NC(CC9)=O)=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 IRAK3 degrader-1 Related Classifications
HY-142662 Related Classifications
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