KBD-1
KBD-1 is a muscle-specific BRD4 PROTAC degrader with human KDs of 27.04 nM and 37.36 µM against BRD4 and KLHL4L, respectively. KBD-1 recruits the muscle-specific E3 ligase KLHL41, mediating Cullin-RING ligase (CRL)-dependent ubiquitination and proteasome degradation of BRD4. KBD-1 can be used for the research of myosarcoma.
(Pink: BRD4 ligand (HY-78695); Blue: KLHL41 ligand (HY-184150); Black: linker).
For research use only. We do not sell to patients.
- Formula: C41H41ClN8O2S
- Molecular Weight:745.33
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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
- Purity & Documentation
- References
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Biological Activity
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BRD4 |
KBD-1 directly interacts with purified recombinant KLHL41 protein with a KD of 37.36 µM[1].
KBD-1 (20 μM; 12 h) completely degrades BRD4 in RH30 human rhabdomyosarcoma cells[1].
KBD-1 (20 μM) induces BRD4 degradation in RH30 human rhabdomyosarcoma cells via Cullin-RING ligase (CRL)-mediated ubiquitination and proteasomal degradation[1].
KBD-1 (20 μM; 24 h) induces BRD4 degradation specifically in RD and RH30 human rhabdomyosarcoma cells (KLHL41-expressing) but not in OV90, A549, SW480, or HeLa non-muscle cancer cell lines[1].
KBD-1 (40 μM; 24 h) induces cytotoxicity specifically in RD and RH30 human rhabdomyosarcoma cells but not in OV90, A549, SW480, or HeLa non-muscle cancer cell lines, with an IC50 of 20 μM in myosarcoma cells[1].
KBD-1 (20 μM; 12 h)-induced BRD4 degradation in RH30 human rhabdomyosarcoma cells is dependent on KLHL41 expression[1].
KBD-1 (20 μM; 12 h) induces BRD4 degradation in HeLa human cervical adenocarcinoma cells only when KLHL41 is overexpressed, confirming KLHL41-dependent activity[1].
KBD-1 induces BRD4 degradation in differentiated C2C12 mouse myocytes (high KLHL41 expression) but not in undifferentiated C2C12 myoblasts (low KLHL41 expression)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RH30 human rhabdomyosarcoma cells
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Concentration:20 μM
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Incubation Time:12 h
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Result:Achieved complete BRD4 degradation at 20 μM after 12 h treatment.
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Cell Line:RD and RH30 human rhabdomyosarcoma cells, OV90, A549, SW480, HeLa non-muscle cancer cell lines
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Concentration:20 μM
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Incubation Time:24 h
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Result:Induced BRD4 degradation in KLHL41-expressing RD and RH30 myosarcoma cell lines, but did not induce BRD4 degradation in non-muscle related cancer cell lines (OV90, A549, SW480, HeLa).
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Cell Line:RD and RH30 human rhabdomyosarcoma cells, OV90, A549, SW480, HeLa non-muscle cancer cell lines
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Concentration:40 μM
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Incubation Time:24 h
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Result:Exhibited cytotoxicity only in RD and RH30 myosarcoma cell lines at 40 μM, with IC50 values of 20 μM, while showing no cytotoxicity in non-muscle related cancer cell lines even at 40 μM.
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Cell Line:RH30 human rhabdomyosarcoma cells (KLHL41 knockdown)
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Concentration:20 μM
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Incubation Time:12 h
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Result:Successfully induced BRD4 degradation in RH30 cells prior to KLHL41 knockdown, but BRD4 degradation was disturbed after KLHL41 knockdown.
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Cell Line:HeLa human cervical adenocarcinoma cells (KLHL41 overexpression)
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Concentration:20 μM
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Incubation Time:12 h
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Result:Did not induce BRD4 degradation in HeLa cells prior to KLHL41 overexpression, but successfully degraded BRD4 after KLHL41 overexpression.
Chemical Information
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Molecular Weight 745.33
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Formula C41H41ClN8O2S
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SMILES
O=C(NCC1=CC=C([C@@H]2OCC[C@H]2CNCC3=CNN=C3C4=CC=CC=C4)C=C1)C[C@H]5C6=NN=C(C)N6C7=C(C(C)=C(C)S7)C(C8=CC=C(Cl)C=C8)=N5
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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)
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