PROTAC TBL1X degrader-1
PROTAC TBL1X degrader-1 is a TBL1X PROTAC degrader. PROTAC TBL1X degrader-1 induces TBL1X degradation via the Cereblon-mediated proteasomal pathway. PROTAC TBL1X degrader-1 exerts cytotoxic effects on cancer cells. PROTAC TBL1X degrader-1 can be used in studies related to diffuse large B-cell lymphoma.
(Pink: TBL1X ligand (HY-168191); Blue: Cereblon ligand (HY-41547); Black: linker (HY-168193)).
For research use only. We do not sell to patients.
- Formula: C49H60N8O11S2
- Molecular Weight:1001.18
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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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Biological Activity
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TBL1X |
PROTAC TBL1X degrader-1 (TD11) (0.008-5 μM; 6 h) induces dose-dependent degradation of TBL1X in Riva DLBCL cells, with maximum reduction to 27% of control levels at 0.04 μM, followed by a hook effect at higher concentrations[1].
PROTAC TBL1X degrader-1 (0.2 μM alone or in combination with 1.0 μM tegavivint/pomalidomide/MG-132; 6 h)-induced TBL1X degradation in Riva DLBCL cells is dependent on formation of a TBL1X-PROTAC-CRBN ternary complex and requires proteasome activity, as shown by reversal of degradation with tegavivint, pomalidomide, or MG-132[1].
PROTAC TBL1X degrader-1 (72 h) induces cytotoxicity in Riva DLBCL, Pfeiffer DLBCL, and Granta-519 MCL cells with IC50 values of 795.0 nM, 397.6 nM, and 522.6 nM, respectively, following 72-hour incubation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Riva diffuse large B-cell lymphoma (DLBCL) cells
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Concentration:0.008 μM, 0.04 μM, 0.2 μM, 1 μM, 5 μM
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Incubation Time:6 h
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Result:Reduced TBL1X levels to 40% of the control at 0.008 μM.
Reduced TBL1X levels to 27% of the control at 0.04 μM.
Recovered TBL1X levels to 53% of the control at 0.2 μM.
Recovered TBL1X levels to 61% of the control at 1 μM.
Increased TBL1X levels to 146% of the control at 5 μM.
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Cell Line:Riva DLBCL cells
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Concentration:0.2 μM (this compound alone); 0.2 μM this compound + 1.0 μM Tegavivint; 0.2 μM TD11 + 1.0 μM Pomalidomide; 0.2 μM this compound + 1.0 μM MG-132
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Incubation Time:6 h
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Result:Reduced TBL1X levels to 51% of the control with 0.2 μM this compound alone.
Restored TBL1X levels to 87% of the control with 0.2 μM this compound + 1.0 μM tegavivint.
Restored TBL1X levels to 82% of the control with 0.2 μM this compound + 1.0 μM pomalidomide.
Restored TBL1X levels to 92% of the control with 0.2 μM this compound + 1.0 μM MG-132.
Chemical Information
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Molecular Weight 1001.18
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Formula C49H60N8O11S2
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SMILES
O=S(C1=CC=C2C(/C(C(C=C(S(N3CC(C)CC(C)C3)(=O)=O)C=C4)=C4/C2=N\OCCCNC(CCCCNC5=C(C(N(C6C(NC(CC6)=O)=O)C7=O)=O)C7=CC=C5)=O)=N/O)=C1)(N8CC(C)CC(C)C8)=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 TBL1X degrader-1 Related Classifications
HY-168190 Related Classifications
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