2. PROTAC Epigenetics Apoptosis Cell Cycle/DNA Damage
  3. PROTACs Epigenetic Reader Domain Apoptosis c-Myc CDK PARP
  4. PROTAC BET Degrader-15

PROTAC BET Degrader-15 is a BET PROTAC degrader with DC50 values of <0.10 nM, <0.01 nM, and <0.01 nM against BRD2, BRD3, and BRD4, respectively. PROTAC BET Degrader-15 induces significant G2/M phase cell cycle arrest and triggers apoptosis. PROTAC BET Degrader-15 causes marked downregulation of c-Myc, accompanied by upregulation of the cell cycle inhibitory protein p21, downregulation of CDK6, and an increase in the apoptosis marker cleaved PARP. PROTAC BET Degrader-15 is applicable to the research of hematologic malignancies and lung cancer.
(Pink: BRD2 and BRD3 and BRD4 ligand (HY-181735); Blue: Cereblon ligand (HY-41547); Black: linker (HY-33846)).

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

PROTAC BET Degrader-15

PROTAC BET Degrader-15 Chemical Structure

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PROTAC BET Degrader-15 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Description

PROTAC BET Degrader-15 is a BET PROTAC degrader with DC50 values of <0.10 nM, <0.01 nM, and <0.01 nM against BRD2, BRD3, and BRD4, respectively. PROTAC BET Degrader-15 induces significant G2/M phase cell cycle arrest and triggers apoptosis. PROTAC BET Degrader-15 causes marked downregulation of c-Myc, accompanied by upregulation of the cell cycle inhibitory protein p21, downregulation of CDK6, and an increase in the apoptosis marker cleaved PARP. PROTAC BET Degrader-15 is applicable to the research of hematologic malignancies and lung cancer[1]. (Pink: BRD2 and BRD3 and BRD4 ligand (HY-181735); Blue: Cereblon ligand (HY-41547); Black: linker (HY-33846)).

IC50 & Target[1]

BRD2

＜0.10 nM (DC50)

BRD3

＜0.01 nM (DC50)

BRD4

＜0.01 nM (DC50)

CDK6

 

In Vitro

PROTAC BET Degrader-15 (Compound CR10) (72 h) potently inhibits the proliferation of MV4-11, Molm-13, and HL-60 acute myeloid leukemia cells, with IC50 values of 1.21, 2.14, and 0.69 nM respectively[1].
PROTAC BET Degrader-15 (72 h) potently inhibits the proliferation of multiple solid tumor cell lines, with IC50 values ranging from 2.83 nM (MDA-MB-231) to 254.2 nM (A549)[1].
PROTAC BET Degrader-15 (5-20 nM; 2 h) induces degradation of BRD2, BRD3, and BRD4 in MV4-11 and A549 cells via a ubiquitin-proteasome system-dependent mechanism that relies on CRBN and BET protein binding[1].
PROTAC BET Degrader-15 (1 h) binds to BRD2, BRD3, and BRD4 bromodomains with nanomolar affinity, with IC50 values ranging from 22 nM (BRD3(1)) to 61 nM (BRD4(2))[1].
PROTAC BET Degrader-15 (1-50 nM; 24 h) dose-dependently arrests MV4-11 cells at the G2/M phase of the cell cycle after 24 h of treatment[1].
PROTAC BET Degrader-15 (1-20 nM; 24 h) dose-dependently induces apoptosis in MV4-11 cells, with significant apoptosis observed at concentrations as low as 1 nM after 24 h of treatment[1].
PROTAC BET Degrader-15 (3.3-1000 nM; 24 h) modulates key proteins involved in proliferation, cell cycle regulation, and apoptosis in MV4-11, A549, and MDA-MB-231 cells, including downregulating C-Myc and CDK6, upregulating P21, and inducing PARP cleavage[1].
PROTAC BET Degrader-15 (4-50 nM; 8 d) potently inhibits the colony-forming ability of A549 and MDA-MB-231 solid tumor cells, with near-complete inhibition observed at 10 nM[1].
PROTAC BET Degrader-15 (50-100 nM; 0-12 h) potently inhibits the migratory capacity of MDA-MB-231 breast cancer cells at concentrations of 50 and 100 nM[1].

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

PROTAC BET Degrader-15 Related Antibodies

Western Blot Analysis[1]

Cell Line: MV4-11 and A549 cells
Concentration: 5 nM (MV4-11 cells, 2 h); 20 nM (A549 cells, 2 h); 10 μM MG132, 10 μM Pomalidomide, 10 μM MLN4924, 100 nM compound 10 (2 h pretreatment)
Incubation Time: 2 h (PROTAC BET Degrader-15 treatment); 2 h (pretreatment prior to PROTAC BET Degrader-15 addition)
Result: Had induced degradation of BRD2, BRD3, and BRD4 completely abolished by pretreatment with MG132, Pomalidomide, MLN4924, or compound 10 in both MV4-11 and A549 cells.

Cell Cycle Analysis[1]

Cell Line: MV4-11 cells
Concentration: 1, 5, 20 and 50 nM
Incubation Time: 24 h
Result: Induced a significant, dose-dependent arrest at the G2/M phase of the cell cycle.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 1, 5 and 20 nM
Incubation Time: 24 h
Result: Elicited pronounced pro-apoptotic effects starting at 1 nM, with apoptosis increasing in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: MV4-11, A549, and MDA-MB-231 cells
Concentration: 3.3, 10, 100, 200 and 1000 nM
Incubation Time: 24 h
Result: Caused dose-dependent downregulation of C-Myc and CDK6, upregulation of P21, and an increase in cleaved-PARP levels (with a corresponding decrease in full-length PARP) in all three cell lines.

Cell Migration Assay [1]

Cell Line: MDA-MB-231 breast cancer cells
Concentration: 50 and 100 nM
Incubation Time: 0, 6, 12 h post-treatment monitoring
Result: Significantly suppressed cell migration relative to controls, as measured by reduced wound closure over time.
Parmacokinetics
Species Dose Route T1/2 Cmax Vss MRT0-inf CL AUC0-t AUC0-∞ Tmax CL/F Vz/F Bioavailability
Mice[1] 1 mg/kg i.v. 1.88 h 207.14 ng/mL 0.75 L/kg 2.62 h 0.28 L/h/kg 204.05 ng·h/mL 215.32 ng·h/mL / / / /
Mice[1] 20 mg/kg i.p. 4.26 h 778.68 ng/mL / 5.10 h / 4571.49 ng·h/mL 4662.67 ng·h/mL 2.00 h 3.98 mL/min/kg 1.45 L/kg 108.27 %
Mice[1] 20 mg/kg p.o. 0.92 h 350.49 ng/mL / 1.38 h / 496.20 ng·h/mL 529.67 ng·h/mL 0.33 h 40.02 mL/min/kg 3.13 L/kg 12.30 %
In Vivo

PROTAC BET Degrader-15 (Compound CR10) (1-2 mg/kg; i.p.; once every 4 days for 21 days) induces dose-dependent tumor growth inhibition in A549 xenograft mice[1].
PROTAC BET Degrader-15 (1-2 mg/kg; i.p.; once every 4 days for 17 days total) induces dose-dependent tumor growth inhibition in MV4-11 xenograft mice[1].

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

Animal Model: BALB/c nude (female, 6-8 weeks old)[1]
Dosage: 1 mg/kg; 2 mg/kg
Administration: i.p.; every 4 days; 21 days
Result: Induced tumor growth inhibition rate of 54.74% at 1 mg/kg and 72.97% at 2 mg/kg, which were notably higher than the positive control dBet1.
Maintained largely unchanged body weights throughout the study.
Showed no obvious lesions in major organs (heart, liver, spleen, lung, kidney) via histopathological examination.
Showed no significant abnormalities in hematological and biochemical analyses.
Animal Model: BALB/c nude (female, 6-8 weeks old)[1]
Dosage: 1 mg/kg; 2 mg/kg
Administration: i.p.; every 4 days; 17 days
Result: Induced tumor growth inhibition rates of 44.26% at 1 mg/kg and 63.19% at 2 mg/kg, which were higher than the positive control dBet1.
Maintained largely unchanged body weights throughout the study.
Showed no obvious lesions in major organs (heart, liver, spleen, lung, kidney) via histopathological examination.
Showed no significant abnormalities in hematological and biochemical analyses.
Molecular Weight

795.88

Formula

C44H45N9O6
SMILES

COC1=C(C2=C(C)ON=C2C)C=C3C(C(N([C@@H](C4=CC=CC=C4)C)C(CN5CCN(CCNC6=C7C(C(N(C8CCC(NC8=O)=O)C7=O)=O)=CC=C6)CC5)=N9)=C9C=N3)=C1
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 BET Degrader-15 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 BET Degrader-15PROTAC BET Degrader15PROTAC BET Degrader 15PROTACsEpigenetic Reader DomainApoptosisc-MycCDKPARPMycCyclin dependent kinasepoly ADP ribose polymerasexenograft tumorsBRD3BRD4ubiquitin-proteasome systemMV4-11 cellshematologic malignancieslung cancerMolm-13 cellsBRD2HL-60 cellsInhibitorinhibitorinhibit

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