Bioactivity | 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 immunotherapy[1]. |
Invitro | 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]. Cell Proliferation Assay[1] Cell Line: |
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]. Animal Model: |
Name | SHP2/HDAC-IN-1 |
CAS | 2831230-38-5 |
Formula | C34H35Cl2N7O3 |
Molar Mass | 660.59 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Meng Liu, et al. Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity. J Med Chem. 2022 Sep 22;65(18):12200-12218. |