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

ZX079 是一种靶向 BRD4 和 CBP 的双靶点 PROTAC 降解剂，其针对 BRD4 的 DC50 值为 0.035 nM，针对 CBP 的 DC50 值为 < 0.02 nM。ZX079 可通过招募 cereblon E3 连接酶，以剂量和时间依赖的方式降解 BRD4 和 CBP 蛋白。ZX079 可诱导 MV4-11 和 MOLM-13 细胞凋亡 (apoptosis)，并在急性髓系白血病异种移植模型中抑制肿瘤生长。ZX079 可用于急性髓系白血病的相关研究。
(粉色: BRD4 (BD1) 和 BRD4 (BD2) 和 CBP 和 p300 配体 (HY-181759)；蓝色: Cereblon 配体 (HY-14658)；黑色: 连接子 (HY-W105740))。

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ZX079

ZX079 Chemical Structure

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ZX079 相关抗体

Top Publications Citing Use of Products

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CBP/p300 GCN5/PCAF TIP60 MOZ/MORF HBO1

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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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

ZX079 (10k) (24 h) 可呈剂量和时间依赖性降解 BRD4 (DC50 = 0.035 nM)、CBP、p300 及 BRD3 (DC50 < 0.02 nM)，而对 BRD2 无显著降解作用[1]。
ZX079 (0.0001-100 μM) 可强效结合 BRD4 (1) (IC50 = 0.9 μM)、BRD4 (2) (IC50 = 0.5 μM) 及 CBP 溴结构域 (IC50 = 1.2 μM)，并可有效促进 BRD4-PROTAC-CRBN 和 CBP-PROTAC-CRBN 三元复合物的组装[1]。
ZX079 (0.02-200 nM; 96 h) 对 MV4-11 细胞 (IC50 = 0.86 nM) 和 MOLM-13 细胞表现出优异的抗增殖活性，而对正常 HUVEC 和 L929 细胞仅表现出极低的细胞毒性 (测试浓度 0.001-10 μM)[1]。
ZX079 (200 nM; 8 h) 可在全蛋白质组水平上选择性消耗 MV4-11 细胞中的 BRD4、BRD3、CBP 和 p300 蛋白[1]。
ZX079 (37-1000 nM; 48 h) 可呈剂量依赖性诱导 MV4-11 和 MOLM-13 细胞发生凋亡，同时伴随 Caspase-3 剪切水平升高；在 2 nM 时，c-Myc 蛋白表达几乎完全被抑制[1]。

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

ZX079 相关抗体:

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.
药代动力学
(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 /
体内研究
(In Vivo)

ZX079 (10k) (2-10 mg/kg；腹腔注射；每周 2 次/每周 1 次；持续 21 天) 在 AML 异种移植模型中展现出强效的体内抗肿瘤活性，通过两种不同的腹腔给药方案实现了 91-93% 的肿瘤生长抑制率，同时保持了耐受性[1]。

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.
分子量

887.99

Formula

C47H56F3N7O7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

ZX079 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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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HY-181854
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