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)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
4T1 IC50
5.43 μM
Compound: 8t
Antiproliferative activity against mouse 4T1 cells assessed as cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against mouse 4T1 cells assessed as cell viability incubated for 72 hrs by CCK-8 assay
[PMID: 36097406]
ASPC1 IC50
2.31 μM
Compound: 8t
Antiproliferative activity against human ASPC1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human ASPC1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
[PMID: 36097406]
BXPC-3 IC50
1.65 μM
Compound: 8t
Antiproliferative activity against human BXPC-3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human BXPC-3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
[PMID: 36097406]
KYSE-520 cell line IC50
1.95 μM
Compound: 8t
Antiproliferative activity against human KYSE520 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human KYSE520 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
[PMID: 36097406]
MV4-11 IC50
0.07 μM
Compound: 8t
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
[PMID: 36097406]
SW1990 IC50
3.92 μM
Compound: 8t
Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
[PMID: 36097406]
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

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  • 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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