2. PROTAC Protein Tyrosine Kinase/RTK Cell Cycle/DNA Damage Metabolic Enzyme/Protease Stem Cell/Wnt MAPK/ERK Pathway JAK/STAT Signaling PI3K/Akt/mTOR Apoptosis
  3. PROTACs FLT3 HSP ERK STAT Akt Apoptosis
  4. MA191

MA191 是一种 FLT3 PROTAC 降解剂。MA191 可消除因丝裂原活化激酶反弹激活而产生的 FLT3 抑制剂耐药性。MA191 通过一种需要 VHL、Neddylation 和 BIM 的机制介导 FLT3-ITD 的快速降解。MA191 在诱导细胞凋亡 (apoptosis) 之前降低 FLT3-ITD 水平。MA191 可抑制斑马鱼体内 AML 细胞的增殖。MA191 可用于急性髓系白血病 (AML) 的研究。(粉色：FLT3 配体：(HY-175311)，蓝色：E3 连接酶 CRBN 配体 (HY-112078)，黑色：连接子，E3 连接酶配体-接头偶联物：(HY-175312))。

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MA191

MA191 Chemical Structure

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MA191 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

查看 HSP 亚型特异性产品:

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

查看 ERK 亚型特异性产品:

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ERK ERK1 ERK2 ERK5 ERK8

查看 STAT 亚型特异性产品:

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STAT3 STAT5 STAT6 STAT1

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Akt Akt1 Akt2 Akt3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MA191 is a FLT3 PROTAC degrader. MA191 abrogates FLT3 inhibitor resistance from rebound activation of mitogen-activated kinases. MA191 mediates rapid FLT3-ITD degradation through a mechanism requiring VHL, neddylation, and BIM. MA191 reduces FLT3-ITD levels before inducing apoptosis. MA191 halts AML cell proliferation in Danio rerio. MA191 can be used for the study of acute myeloid leukemia (AML) (Pink: FLT3 ligand: (HY-175311), Blue: E3 ligase CRBN Ligand (HY-112078), Black: Linker, E3 ligase ligand-linker conjugate (HY-175312))[1].

体外研究
(In Vitro)

MA191 (0-100 nM, 24-72 h) 可抑制 MV4-11 和 MOLM-13 细胞的生长，其 IC50 值在 9.6 至 11 nM 之间[1]。
MA191 (50 nM, 6-24 h) 可抑制 MV4-11 和 MOLM-13 细胞中 FLT3 的自磷酸化 (pY591) 以及 ERK1/ERK2、STAT5 和 AKT 的磷酸化[1]。
MA191 (10-50 nM, 16-24 h) 以剂量和时间依赖性方式降低 MV4-11 细胞中 FLT3-ITD 和 HSP110 的水平[1]。
MA191 (0-100 nM, 6-24 h) 可在 MV4-11 细胞中诱导 FLT3-ITD 的 BIM 依赖性和类泛素化依赖性降解，在 16 h 时的 DC50 值为 10.5 nM，在 24 h 时为 10 nM[1]。
MA191 (0-1000 nM, 24-48 h) 可诱导携带 FLT3-ITD 的培养型和原代急性髓系白血病细胞凋亡，且不影响正常免疫细胞、造血干细胞和祖细胞[1]。
MA191 (50-200 nM, 24-72 h) 可破坏 AML 细胞对 FLT3 抑制剂的耐药机制[1]。

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

MA191 相关抗体:

Western Blot Analysis[1]

Cell Line: MV4-11 and MOLM-13 cells
Concentration: 50 nM
Incubation Time: 6, 24 h
Result: Inhibited the autophosphorylation of FLT3 (pY591) and phosphorylation of ERK1/ERK2, STAT5 and AKT.
Decreased the FLT3-ITD levels after 24 h, whereas in RS4-11, FLT3 was less affected.
Increased the level of caspase-3.

Western Blot Analysis[1]

Cell Line: MV4-11 cells, BIM-KD-MV4-11 cells and VHL-KD-MV4-11 cells
Concentration: 10, 20, 50 nM
Incubation Time: 6, 16, 24 h
Result: Degraded FLT3-ITD in MV4-11 cells which was inhibited in BIM-KD-MV4-11 cells.
Degraded HSP110, HSP70, HSP27, and HSP90.
Inhibited the phosphorylation of FLT3-ITD.
Attenuated phosphorylated STAT5 dose- and time-dependently.
Showed a time- and dose-dependent accumulation of active caspase-3 and BIM-EL after 16 h.
Rescued the degradation of FLT3 in cells with a KD of VHL.

Apoptosis Analysis[1]

Cell Line: MV4-11 and MOLM-13 cells
Concentration: 100, 200 nM
Incubation Time: 24, 72 h
Result: Did not induce apoptosis in RS4-11 after a 72-h treatment. In MV4-11 cell cultures, the death rate was nearly 100% and in the case of MOLM-13 cell cultures it was 50%.
Induced cell death in MOLM-13, MOLM-13-RES and MOLM-13-RES-AC.
体内研究
(In Vivo)

MA191 (200 nM, 48 h, 单次给药) 在体内斑马鱼幼鱼模型中抑制急性髓细胞白血病细胞增殖且无明显毒性[1]。

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

Animal Model: MV4-11 cells at density of 1×106 cells/mL were injected into the yolk sac of zebrafish wild-type AB line embryos on day 2 post fertilization[1].
Dosage: 200 nM
Administration: 48 h
Result: Halted AML cell proliferation.
Showed no significant toxicity .
分子量

1088.32

Formula

C57H73N11O9S
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

MA191 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

MA191MA 191MA-191PROTACsFLT3HSPERKSTATAktApoptosisCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Heat shock proteinsExtracellular signal regulated kinasesPKBProtein kinase Bacute myeloid leukemiaAKTapoptosisInhibitorinhibitorinhibit

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