2. PROTAC Epigenetics Apoptosis
  3. PROTACs Epigenetic Reader Domain Histone Acetyltransferase c-Myc Caspase Apoptosis
  4. ZX079

ZX079 is a dual BRD4 and CBP PROTAC degrader with a BRD4 DC50 value of 0.035 nM and a CBP DC50 value of < 0.02 nM. ZX079 induces dose- and time-dependent degradation of BRD4 and CBP proteins through recruitment of the cereblon E3 ligase. ZX079 induces apoptosis in MV4-11 and MOLM-13 cells, reduces tumor growth in an acute myeloid leukemia xenograft model. ZX079 can be used for the research of acute myeloid leukemia.
(Pink: BRD4 (BD1) and BRD4 (BD2) and CBP and p300 ligand (HY-181759); Blue: Cereblon ligand (HY-14658); Black: linker (HY-W105740)).

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

ZX079

ZX079 Chemical Structure

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ZX079 Related Antibodies

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Description

ZX079 is a dual BRD4 and CBP PROTAC degrader with a BRD4 DC50 value of 0.035 nM and a CBP DC50 value of < 0.02 nM. ZX079 induces dose- and time-dependent degradation of BRD4 and CBP proteins through recruitment of the cereblon E3 ligase. ZX079 induces apoptosis in MV4-11 and MOLM-13 cells, reduces tumor growth in an acute myeloid leukemia xenograft model. ZX079 can be used for the research of acute myeloid leukemia[1]. (Pink: BRD4 (BD1) and BRD4 (BD2) and CBP and p300 ligand (HY-181759); Blue: Cereblon ligand (HY-14658); Black: linker (HY-W105740)).

IC50 & Target[1]

BRD4

0.035 nM (DC50)

BRD4(1)

0.9 μM (IC50)

BRD4(2)

0.5 μM (IC50)

CBP

 

p300

 

Caspase 3

 

Cereblon

 

In Vitro

ZX079 (10k) (24 h) exhibits dose- and time-dependent degradation of BRD4 (DC50 = 0.035 nM), CBP, p300 and BRD3 (DC50 < 0.02 nM) without significant degradation of BRD2[1].
ZX079 (0.0001-100 μM) binds potently to BRD4 (1) (IC50 = 0.9 μM), BRD4 (2) (IC50 = 0.5 μM), and CBP bromodomains (IC50 = 1.2 μM) and effectively promotes BRD4-PROTAC-CRBN and CBP-PROTAC-CRBN ternary complex assembly[1].
ZX079 (0.02-200 nM; 96 h) exerts superior antiproliferative activity against MV4-11 cells (IC50 = 0.86 nM) and MOLM-13 cells, while it shows minimal cytotoxicity against normal HUVEC and L929 cells (tested at 0.001-10 μM)[1].
ZX079 (200 nM; 8 h) selectively depletes BRD4, BRD3, CBP, and p300 proteins in MV4-11 cells at the proteome-wide level.
ZX079 (37-1000 nM; 48 h) induces apoptosis in MV4-11 and MOLM-13 cells in a dose-dependent manner, accompanied by increased cleavage of Caspase-3 and almost complete reduction of c-Myc protein expression at 2 nM[1].

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

ZX079 Related Antibodies

Cell Viability Assay[1]

Cell Line: MV4-11 and MOLM-13 acute myeloid leukemia cells, HUVEC, L929 normal cells
Concentration: 10-6, 10-4, 10-2, 100, 102 μM (MV4-11 and MOLM-13 cells); 0.01, 0.01, 0.1, 1, 10, 100 μM (HUVEC and L929 cells)
Incubation Time: 96 h (MV4-11 and MOLM-13 cells); 48 h (HUVEC and L929 cells)
Result: Exhibited an IC50 of 0.86 nM in MV4-11 cells and 18.93 nM in MOLM-13 cells.
Exhibited minimal cytotoxicity toward HUVEC and L929 cells.

Western Blot Analysis[1]

Cell Line: MV4-11 acute myeloid leukemia cells
Concentration: 0.02, 0.2, 2.0, 20, 200 nM (24 h); 200 nM (time-course); 2 nM, 200 nM (24 h)
Incubation Time: 1 h, 2 h, 4 h, 8 h, 12 h, 24 h (time-course); 24 h (fixed time)
Result: Achieved 95% degradation of BRD4 and 74% degradation of CBP at 2 nM after 24 h.
Achieved 98% degradation of BRD4 and 99% degradation of CBP at 200 nM after 24 h.
Induced rapid degradation of CBP within 2 h, with near-complete depletion by 4 h.
Reduced BRD4 levels in a time-dependent manner over 24 h.
Exhibited a DC50 of 0.035 nM for BRD4, < 0.02 nM for CBP, and < 0.02 nM each for p300 and BRD3.

Apoptosis Analysis[1]

Cell Line: MV4-11 and MOLM-13 acute myeloid leukemia cells
Concentration: 37, 111, 333, 1000 nM
Incubation Time: 48 h
Result: Potently induced apoptosis in a dose-dependent manner, achieving over 60% apoptosis at 37 nM in MV4-11 cells.
Led to markedly increased cleaved caspase-3 levels and almost completely reduced c-Myc protein expression in MV4-11 cells at 20 nM.
Induced dose-dependent apoptosis in MOLM-13 cells.
Parmacokinetics
Species Dose Route AUClast Cmax CL T1/2 F
Rat[1] 10 mg/kg p.o. 43.9 μg/L·h 9.5 μg/L - L/h/kg 2.13 h 1.48 %
Rat[1] 2 mg/kg i.v. 610 μg/L·h 634 μg/L 3.28 L/h/kg 1.74 h /
In Vivo

ZX079 (10k) (2-10 mg/kg; intraperitoneal injection; twice weekly/weekly; 21 days) exhibits potent in vivo antitumor activity in an AML xenograft model, achieving 91-93% tumor growth inhibition with two distinct intraperitoneal dosing regimens, while maintaining tolerability[1].

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

Animal Model: NOD SCID (female, 4 weeks old, subcutaneous xenograft model)[1]
Dosage: 2 mg/kg (twice weekly); 10 mg/kg (weekly)
Administration: intraperitoneal injection; 21 days
Result: Achieved a tumor growth inhibition (TGI) rate of 93% with 2 mg/kg twice-weekly dose.
Achieved a TGI rate of 91% with 10 mg/kg weekly dose.
Caused no significant body weight loss compared to vehicle control.
Induced degradation of BRD4 and CBP proteins in harvested tumors.
Significantly reduced c-Myc protein expression relative to vehicle control.
Molecular Weight

887.99

Formula

C47H56F3N7O7
SMILES

O=C(NC(CC1)=O)C1N(C2=O)C(C(C2=C3)=CC=C3NCCCCCCCCCCCC(N(CC4)CCC4C5=NC6=CC=C(C(C=C7C)=CN(C)C7=O)C=C6N5CCOC(F)(F)F)=O)=O
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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ZX079 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:

ZX079ZX 079ZX-079PROTACsEpigenetic Reader DomainHistone Acetyltransferasec-MycCaspaseApoptosisHATsHATMycCBPCRBNMV4-11 cellsacute myeloid leukemia cellscereblon E3 ligaseacute myeloid leukemia xenograft modelBRD4p300ubiquitin-proteasome systemBRD3Inhibitorinhibitorinhibit

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