2. Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease Epigenetics Cell Cycle/DNA Damage
  3. SHP2 Phosphatase HDAC
  4. SHP2/HDAC-IN-1

SHP2/HDAC-IN-1 是一种变构的 SHP2/HDAC 双重抑制剂，IC50 值分别为 20.4 nM (SHP2) 和 25.3 nM ( HDAC1)。SHP2/HDAC-IN-1 通过激活 T 细胞、增强抗原呈递功能和促进细胞因子分泌来触发抗肿瘤免疫反应。SHP2/HDAC-IN-1 可用于癌症的免疫研究。

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SHP2/HDAC-IN-1 Chemical Structure

SHP2/HDAC-IN-1 Chemical Structure

CAS No. : 2831230-38-5

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SHP2/HDAC-IN-1 相关抗体

Top Publications Citing Use of Products

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SHP2/HDAC-IN-1 is a dual allosteric SHP2/HDAC inhibitor with IC50 values of 20.4 nM (SHP2) and 25.3 nM (HDAC1) respectively. SHP2/HDAC-IN-1 triggers efficient antitumor immunity by activating T cells, enhancing the antigen presentation function and promoting cytokine secretion. SHP2/HDAC-IN-1 can be used in the research of cancer immunoresearch[1].

IC50 & Target[1]

HDAC1

25 nM (IC50)

HDAC2

79 nM (IC50)

HDAC3

233 nM (IC50)

HDAC6

27 nM (IC50)

SHP2

20.4 nM (IC50)

体外研究
(In Vitro)

SHP2/HDAC-IN-1 (compound 8t, 0-10 μM approximately, 72 h) inhibits the proliferation of BxPC-3, SW1990, AsPC-1and MV4-11 cells[1].
SHP2/HDAC-IN-1 (0.25-1 μM, 24 h) increases the acetylation of α-tubulin and histone H3 in MV4-11 cells[1].
SHP2/HDAC-IN-1 (0.25 μM, 24 h) inhibits cell cycle progression in the G1 phase of MV4-11 cells[1].
SHP2/HDAC-IN-1 (0.25 and 0.5 μM, 24 h) decreases the mitochondrial membrane potential and activats caspase-3[1].
SHP2/HDAC-IN-1 (2 h) shows good stability in in mouse liver microsome[1].

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

SHP2/HDAC-IN-1 相关抗体:

Cell Proliferation Assay[1]

Cell Line: Pancreatic carcinoma (BxPC-3, SW1990, and AsPC-1), acute monocytic leukemia (MV4-11)
Concentration: 0-10 μM approximately
Incubation Time: 72 h
Result: Inhibited cell proliferation with IC50s range of 0.07 μM-3.92 μM.

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.25, 0.5, 1 μM
Incubation Time: 24 h
Result: Increased the acetylation of α-tubulin and histone H3.
Inhibited the phosphorylation level of ERK.
体内研究
(In Vivo)

SHP2/HDAC-IN-1 (compound 8t, 40 mg/kg, p.o.) inhibits tumor growth in MV4-11 and 4T1 tumor-bearing xenograft mice[1].
SHP2/HDAC-IN-1 (20 mg/kg p.o., 1 mg/kg i.v.) exhibits good maximum plasma concentrations in rats[1].

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

Animal Model: MV4-11 tumor-bearing xenograft mice[1]
Dosage: 40 mg/kg
Administration: Oral adminstration (p.o.), every day for 20 consecutive days.
Result: Delayed tumor progression with a tumor growth inhibition rate (TGI %) value of 64.0%, with no obvious signs of toxicity.
Animal Model: 4T1 murine breast cancer model[1]
Dosage: 40 mg/kg
Administration: Oral adminstration (p.o.), every day for 12 consecutive days.
Result: Significantly decreased tumor burden with a TGI value of 72%.
Increased the proportions of CD4+ T cells and CD8+ T cells in the spleen.
Enhanced the proportion of mDCs in lymph nodes.
Animal Model: Male Sprague-Dawley (SD) rats (Pharmacokinetic assay)[1]
Dosage: 20 mg/kg p.o., 1 mg/kg i.v.
Administration: Oral adminstration (p.o.) or intravenous injection (i.v.)
Result: Pharmacokinetic profile of SHP2/HDAC-IN-1 (compound 8t).
dose (mg/kg) T1/2 (h) Cmax (ng/mL) Cl (mL/h/kg) F (%)
20 (p.o.) 5.32 1835 21.42
1 (i.v.) 6.15 3517 326
分子量

660.59

Formula

C34H35Cl2N7O3
CAS 号
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

SHP2/HDAC-IN-1 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:

SHP2/HDAC-IN-12831230-38-5SHP2PhosphataseHDACSrc homology phosphatase 2PTPN11Histone deacetylasesTumorT cellantigen presentationimmunitycancerMV4-114T1Inhibitorinhibitorinhibit

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