2. PROTAC Cell Cycle/DNA Damage Apoptosis
  3. PROTACs Checkpoint Kinase (Chk) DNA/RNA Synthesis Apoptosis Bcl-2 Family Caspase
  4. MA203

MA203 是一种高效且选择性的 PROTAC 降解剂，靶向 CHK1。MA203 可加速实体瘤细胞和急性白血病细胞中 CHK1 的 CRBN 依赖性蛋白酶体降解。MA203 可诱导 DNA 复制应激。MA203 可阻断细胞周期进程并诱导肿瘤细胞凋亡 (apoptosis)。MA203 不会损伤健康的已分化和原始造血细胞、基质细胞以及视网膜上皮细胞。MA203 可用于 CHK1 依赖性癌症的研究。
(粉色: Chk1 靶蛋白配体；蓝色: Cereblon 配体 (HY-41547)；黑色: 连接子 (HY-22391))。

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MA203

MA203 Chemical Structure

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MA203 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Chk1 Chk2 BUBR1

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3

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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

MA203 is a highly efficient and selective PROTAC degrader targeting CHK1. MA203 accelerates CRBN-dependent proteasomal degradation of CHK1 in solid tumor-derived cells and acute leukemia cells. MA203 induces DNA replication stress. MA203 blocks cell cycle progression and triggers tumor cell apoptosis. MA203 does not damage healthy differentiated and primitive hematopoietic cells, stromal cells, and retinal epithelial cells. MA203 can be used for the study of CHK1-dependent cancers[1]. (Pink: Chk1 Target protein ligand; Blue: Cereblon ligand (HY-41547); Black: linker (HY-22391)).

IC50 & Target[1]

Chk1

 

Bax

 

Bcl-xL

 

体外研究
(In Vitro)

MA203 (PROTAC 41) 在 5 µM 浓度下可使 MIA PaCa-2 胰腺导管腺癌 (PDAC) 细胞中 CHK1 水平降低约 50%，并且与 CHK1 具有很强的亲和力 (在 1.0 µM 浓度下结合率为 97%)[1]。
MA203 (2 µM，24 小时) 可显著降低 Hydroxyurea (HY-B0313) (HU) 处理的 MIA PaCa-2 和 MOLT-4 细胞中 CHK1 水平，分别降低高达 80% 和 50%[1]。
MA203 (2 μM，3-24 小时) 介导的 CHK1 降解是一个时间依赖性过程，并伴有 MIA PaCa-2 细胞中磷酸化状态的改变，表明该降解增强了 DNA 损伤信号[1]。
MA203联合 HU 可显著降低 MOLT-4 细胞、MOLM-13 细胞、RS4-11 细胞和 HCT116 细胞中 CHK1 的表达水平至未处理细胞的 50%-40%，并减弱 MOLM-13 细胞中 CHK1 的表达[1]。
在 MIA PaCa-2 细胞中，MA203 (1-5 µM，24 h) 与5 µM Irinotecan (HY-16562) 联合使用时，其剂量依赖性地减弱CHK1表达的效果优于单独使用[1]。
在MOLT-4细胞中，MA203 (0.5-10 µM，24 h) 与2 µM Cytarabine (HY-13605) 联合使用时，其达到半数最大CHK1降解浓度 (DC50 = 387.4 nM) 显著低于单独使用时的DC50 (DC50 = 3.86 µM)[1]。
MA203 (0.5–10 μM，24 小时) 增强 HU 诱导的 DNA 复制应激，导致 MIA PaCa-2 和 MOLT-4 细胞中 DNA 双链断裂和复制灾难[1]。
MA203 (2 μM，24-48 小时) + HU 显著增加 MIA PaCa-2 和 MOLT-4 细胞中早期和晚期凋亡细胞的比例[1]。
MA203 (2 μM，24 小时) 单独使用或与 HU 联合使用均能促进树突状细胞的存活[1]。
MA203 (2 μM，24 小时) 显著增强 Ara-C 介导的细胞死亡，表现为 MOLT-4 细胞中杀死 50% 细胞所需的 Ara-C 浓度 (IC50) 降低了 62%[1]。
MA203 (2 µM，24 小时) + HU 处理 24 小时后，MIA PaCa-2 细胞中多种关键蛋白的表达显著降低，这些蛋白调控肿瘤发生和 DNA 损伤修复，包括转录因子 7 (TCF7)、细胞周期相关蛋白 7 (CDCA7)、起始点识别复合物亚基 1 (ORC1) 和 Werner 综合征 RecQ 样解旋酶 (WRN)，同时 RRM2 水平略有升高[1]。
MA203 (2 µM，24-48 小时) + HU 处理可导致更显著的 G1/S 期阻滞；诱导更高的细胞凋亡率，并伴有 BAX/BIM 的上调和 BCL-XL/XIAP 的下调；线粒体膜电位更显著的丧失以及更强的 caspase 激活[1]。

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

MA203 相关抗体:

Western Blot Analysis[1]

Cell Line: MIA PaCa-2 cells, MOLT-4 cells
Concentration: 2 µM
Incubation Time: 24 h
Result: Specifically degraded CHK1, and this degradation is enhanced by HU-induced CHK1 activation.
Did not affect other checkpoint kinases or common CRBN substrates.

Western Blot Analysis[1]

Cell Line: MIA PaCa-2 cells
Concentration: 2 µM
Incubation Time: 3 h, 6 h, 10 h, 16 h, 24 h
Result: Illustrated that the degradation of CHK1 started already after 3 h in MIA PaCa-2 cells, to yield a 50%-70% reduction of CHK1 after 10-16 h.
Suppressed the HU-induced hyperphosphorylation of CHK1 at S296 but augmented its HU-induced hyperphosphorylation at S345.
Did not alter CHK2 levels over different time points.

Western Blot Analysis[1]

Cell Line: MIA PaCa-2, MOLT-4
Concentration: 0.5 μM, 1 μM, 2 μM, 5 μM, 10μM
Incubation Time: 24 h
Result: Significantly increased γH2AX levels (4.2-fold).
Achieved a Dmax of 92% at a DC50 of 1.51 µM in MIA PaCa-2 cells, and a Dmax of 93.2% at a DC50 of 5.35 µM in MOLT-4 cells.
Significant 15.7-fold induction of ATM phosphorylation at S1981.

Apoptosis Analysis[1]

Cell Line: MIA PaCa-2 cells, HCT116 cells, MOLT-4 cells, MOLM-13 cells
Concentration: 2 μM
Incubation Time: 24 h, 48 h
Result: After 48 h, the percentages of early and late apoptotic cells significantly increased to 15% and 14% in MIA PaCa-2 cell cultures; A significant rise in the early apoptotic cell population to 33% was observed.
In HCT116 cells, caused early and late apoptosis were significantly increased when combined with 0.5 mM HU for 48 h. An accumulation of late apoptotic cells (30%) occurred upon treatment.
Significantly augmented cell populations in early apoptosis to 19% and in late apoptosis to 15% after 24 h in MOLT-4 cells. In the presence of 1 mM HU, triggered early (48%) and late (24%) apoptotic cell death.
In MOLM-13 cells, triggered a significant accumulation of early apoptotic cells (33%), enhanced late apoptosis of MOLM-13 cells to 50%.
Normal human cells did not exhibit any significant impairment in viability upon treatment.
体内研究
(In Vivo)

MA203 (PROTAC 41) (12 μM，48 小时) 能显著抑制斑马鱼幼体中人类白血病细胞的增殖，且在有效剂量下对斑马鱼幼体无明显毒性[1]。

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

755.82

Formula

C38H45N9O8
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

MA203 相关分类

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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:

MA203MA 203MA-203PROTACsCheckpoint Kinase (Chk)DNA/RNA SynthesisApoptosisBcl-2 FamilyCaspaseRPOTACCHK1CereblonMIA PaCa-2 cellsMOLT-4MOLM-13RS4-11Inhibitorinhibitorinhibit

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