PROTAC BTK Degrader-13
PROTAC BTK Degrader-13 is a reagent targeting BTK, with a DC50 of 0.27 μM. PROTAC BTK Degrader-13 degrades BTK in a proteasome-dependent manner and inhibits BTK-mediated downstream signaling pathways by reducing the phosphorylation levels of BTK and p38 MAPK. PROTAC BTK Degrader-13 exerts selective cytotoxic effects on BTK-overexpressing lymphoma cells and ITK-positive cells. PROTAC BTK Degrader-13 can be used in studies related to B-cell lymphoma.
(Pink: Btk ligand (HY-168965); Blue: Cereblon ligand (HY-103596); Black: linker).
For research use only. We do not sell to patients.
- Formula: C33H30N6O7
- Molecular Weight:622.63
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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
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- References
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Biological Activity
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p38 |
PROTAC BTK Degrader-13 (compound 25) (0-50 μM; 72 h) exhibits cytotoxicity against ITK-positive JURKAT and CCRF-CEM cells, as well as BTK-positive RAMOS cells, with IC50 values of 3.42 μM, 3.81 μM, and 9.79 μM, respectively. However, it shows no cytotoxicity against BTK-positive K562 cells, ITK/BTK-deficient cancer cells, or non-cancerous fibroblasts[1].
PROTAC BTK Degrader-13 (0-20 μM; 24 h) induces proteasome-dependent BTK degradation in RAMOS cells, with a Dmax of 72.84% and a DC50 of 0.27 μM[1].
PROTAC BTK Degrader-13 (0-10 μM; per kit protocol) selectively inhibits BTK kinase activity over ITK, with an IC50 of 0.44 μM against BTK and 2.16 μM against ITK[1].
PROTAC BTK Degrader-13 (0-20 μM; 24 h) has no effect on ITK protein levels in JURKAT cells[1].
PROTAC BTK Degrader-13 (0-20 μM; 24 h pre-incubation) inhibits BTK-mediated downstream signaling pathways in RAMOS cells, and significantly reduces the phosphorylation levels of BTK (Tyr551, Tyr223) and p38 MAPK after stimulation with LPS or IgM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAMOS (B-cell lymphoma, BTK-positive)
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Concentration:0, 20 μM (with/without 10 nM Bortezomib (HY-10227), mechanism validation)
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Incubation Time:24 h
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Result:Completely blocked BTK degradation when co-treated with 10 nM Bortezomib.
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Cell Line:JURKAT (T-cell leukemia, ITK-positive)
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Concentration:0, 5, 10, 20 μM
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Incubation Time:24 h
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Result:Did not reduce ITK protein levels at tested concentrations.
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Cell Line:RAMOS (B-cell lymphoma, BTK-positive)
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Concentration:0, 5, 10, 20 μM (pre-treatment)
1 μg/mL LPS (stimulation); 10 μg/mL anti-human IgM (stimulation) -
Incubation Time:24 h (pre-incubation)
10 min (stimulation) -
Result:Significantly reduced phosphorylation of BTK at Tyr551 and Tyr223, as well as phosphorylation of p38 MAPK, compared to untreated cells following either LPS or IgM stimulation.
Chemical Information
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Molecular Weight 622.63
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Formula C33H30N6O7
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SMILES
O=C1NC2=NC=C(C3=CC=C(OCO4)C4=C3)C=C2C15CCN(CCNC6=C7C(C(N(C8C(NC(CC8)=O)=O)C7=O)=O)=CC=C6)CC5
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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 BTK Degrader-13 Related Classifications
HY-168963 Related Classifications
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