2. PROTAC Epigenetics Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  3. PROTACs Epigenetic Reader Domain HSP
  4. PROTAC BRD4 Degrader-21

PROTAC BRD4 Degrader-21 is a BRD4-targeting PROTAC degrader with an IC50 value of 59 nM. PROTAC BRD4 Degrader-21 induces ubiquitination of BRD4, leading to its degradation via the proteasome. PROTAC BRD4 Degrader-21 binds to recombinant HSP90α protein with moderate affinity, having an IC50 of 100-1000 nM. PROTAC BRD4 Degrader-21 induces cancer cell death. PROTAC BRD4 Degrader-21 inhibits tumor growth in xenograft mouse models. PROTAC BRD4 Degrader-21 can be used for the research of acute myeloid leukemia, diffuse large B-cell lymphoma.
(Pink: BRD4 ligand (HY-78695); Blue: MDM2 E3 ligase ligand; Black: linker).

For research use only. We do not sell to patients.

PROTAC BRD4 Degrader-21

PROTAC BRD4 Degrader-21 Chemical Structure

CAS No. : 2503036-46-0

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PROTAC BRD4 Degrader-21 Related Antibodies

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Description

PROTAC BRD4 Degrader-21 is a BRD4-targeting PROTAC degrader with an IC50 value of 59 nM. PROTAC BRD4 Degrader-21 induces ubiquitination of BRD4, leading to its degradation via the proteasome. PROTAC BRD4 Degrader-21 binds to recombinant HSP90α protein with moderate affinity, having an IC50 of 100-1000 nM. PROTAC BRD4 Degrader-21 induces cancer cell death. PROTAC BRD4 Degrader-21 inhibits tumor growth in xenograft mouse models. PROTAC BRD4 Degrader-21 can be used for the research of acute myeloid leukemia, diffuse large B-cell lymphoma[1]. (Pink: BRD4 ligand (HY-78695); Blue: MDM2 E3 ligase ligand; Black: linker).

IC50 & Target[1]

BRD4

59 nM (IC50)

HSP90α

100-1000 nM (IC50)

In Vitro

PROTAC BRD4 Degrader-21 (compound 074) (40 μM to 2.0 nM) binds to recombinant HSP90α protein with moderate affinity, having an IC50 of 100-1000 nM in a fluorescent polarization assay[1].
PROTAC BRD4 Degrader-21 (10 μM; 1 hr) binds specifically to bromodomains of the BET family proteins, showing strong competition for ligand binding to BRD2, BRD3, BRD4, and BRDT bromodomains at 10 μM, while displaying minimal binding to non-BET bromodomains[1].
PROTAC BRD4 Degrader-21 (40 μM to 2.0 nM; 2 hr) binds to recombinant BRD4 (BD1+BD2) protein with moderate affinity, having an IC50 of 100-1000 nM in a homogeneous time resolved fluorescence assay[1].
PROTAC BRD4 Degrader-21 (100-300 nM; 24 hr) induces degradation of BRD4 protein in MV4-11 acute myeloid leukemia cells when treated at 100 nM and 300 nM for 24 hr[1].
PROTAC BRD4 Degrader-21 (24 hr) reduces MYC protein expression in MV4-11 acute myeloid leukemia cells with an IC50 <100 nM after 24 hr of treatment[1].
PROTAC BRD4 Degrader-21 selectively degrades BRD4 over HSP90 client proteins, with its IC50 for BRD4 degradation (59 nM in MV4-11 cells) being 6- to 18-fold lower than its IC50 values for degradation of ERBB2, IGF1R, EGFR, and RAF1[1].
PROTAC BRD4 Degrader-21 (72 hr) potently inhibits the growth of MV4-11 acute myeloid leukemia cells, with an IC50 <100 nM in a 72-hr CCK-8 cytotoxicity assay[1].
PROTAC BRD4 Degrader-21 degradates HSP90 client proteins, with IC50 values of 340 nM, 1055 nM, 405 nM, 762 nM for ERBB2, IGF1R, EGFR and RAF1, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PROTAC BRD4 Degrader-21 Related Antibodies

Western Blot Analysis[1]

Cell Line: MV4-11 acute myeloid leukemia cells
Concentration: 3 nM, 10 nM, 30 nM, 100 nM, 300 nM
Incubation Time: 24 hr
Result: Induced degradation of BRD4 protein in MV4-11 cells at 100 nM and 300 nM.
Had its induced BRD4 degradation blocked when cells were co-treated with proteasome inhibitor Bortezomib.
Parmacokinetics
Species Dose Route T1/2 Tmax (Plasma) Cmax AUC0-∞
Mice[1] 5 mg/kg i.v. 3.92 h 1.00 h 497.95 ng/mL 3015.79 ng·h/mL
In Vivo

PROTAC BRD4 Degrader-21 (compound 074) (25-100 mg/kg; i.v.; once weekly; 3 weeks) induces significant tumor growth inhibition in a MV4-11 acute myeloid leukemia xenograft model, with complete tumor regression in some animals[1].
PROTAC BRD4 Degrader-21 (compound 074) (50-100 mg/kg; i.v.; once weekly; 4 weeks) induces significant tumor growth inhibition in a SU-DHL-4 diffuse large B-cell lymphoma xenograft model[1].
PROTAC BRD4 Degrader-21 (compound 074) (5 mg/kg; i.v.; single dose) displays tumor-selective retention in a MV4-11 acute myeloid leukemia xenograft model, with a tumor half-life 4.6-9.5-times longer than in plasma and normal organs[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude (male) injected with MV4-11 cells[1]
Dosage: 25 mg/kg; 50 mg/kg; 100 mg/kg
Administration: i.v.; once weekly; 3 weeks
Result: Induced significant tumor growth inhibition in 50 mg/kg and 100 mg/kg groups.
Achieved complete tumor regression in 1 out of 6 animals (50 mg/kg group) and 4 out of 6 animals (100 mg/kg group).
Caused no significant effects on body weights in any dose group.
Molecular Weight

925.97

Formula

C47H54Cl2N10O4S
CAS No.
SMILES

CC1=C(C)SC2=C1C(C3=CC=C(C=C3)Cl)=N[C@@H](CC(N4CCC(CC4)CN5CCN(CC5)CC6=CC=C(N7C(C8=CC(C(C)C)=C(C=C8O)O)=NNC7=O)C=C6)=O)C9=NN=C(C)N29.Cl
Shipping

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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PROTAC BRD4 Degrader-21 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:

PROTAC BRD4 Degrader-212503036-46-0PROTACsEpigenetic Reader DomainHSPHeat shock proteinsdiffuse large B-cell lymphomaSU-DHL-4 diffuse large B-cell lymphomaproteasomeacute myeloid leukemiaBRD4HSP90αMV4-11 acute myeloid leukemia cellsxenograft mouse modelsbromodomainsBET family proteinsInhibitorinhibitorinhibit

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