2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. 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.

KBD-1

KBD-1 Chemical Structure

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KBD-1 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

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[1]. (Pink: BRD4 ligand (HY-78695); Blue: KLHL41 ligand (HY-184150); Black: linker).

IC50 & Target[1]

BRD4

 

In Vitro

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.

KBD-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: RH30 human rhabdomyosarcoma cells
Concentration: 20 μM
Incubation Time: 12 h
Result: Achieved complete BRD4 degradation at 20 μM after 12 h treatment.

Western Blot Analysis[1]

Cell Line: RD and RH30 human rhabdomyosarcoma cells, OV90, A549, SW480, HeLa non-muscle cancer cell lines
Concentration: 20 μM
Incubation Time: 24 h
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).

Cell Viability Assay[1]

Cell Line: RD and RH30 human rhabdomyosarcoma cells, OV90, A549, SW480, HeLa non-muscle cancer cell lines
Concentration: 40 μM
Incubation Time: 24 h
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.

Western Blot Analysis[1]

Cell Line: RH30 human rhabdomyosarcoma cells (KLHL41 knockdown)
Concentration: 20 μM
Incubation Time: 12 h
Result: Successfully induced BRD4 degradation in RH30 cells prior to KLHL41 knockdown, but BRD4 degradation was disturbed after KLHL41 knockdown.

Western Blot Analysis[1]

Cell Line: HeLa human cervical adenocarcinoma cells (KLHL41 overexpression)
Concentration: 20 μM
Incubation Time: 12 h
Result: Did not induce BRD4 degradation in HeLa cells prior to KLHL41 overexpression, but successfully degraded BRD4 after KLHL41 overexpression.
Molecular Weight

745.33

Formula

C41H41ClN8O2S
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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KBD-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KBD-1KBD1KBD 1PROTACsEpigenetic Reader DomainubiquitinationCullin-RING ligasemyosarcomaproteasomal degradationC2C12 mouse myocytesKLHL41E3 ligaseRD human rhabdomyosarcoma cellsRH30 human rhabdomyosarcoma cellsBRD4Inhibitorinhibitorinhibit

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