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I3MT-3

CAS No. : 459420-09-8

MCE 站：I3MT-3

产品活性：I3MT-3 (HMPSNE) 是有效、选择性和具有细胞膜渗透性的 3-巯基丙酮酸硫转移酶 (3MST) (IC₅₀=2.7 μM) 的抑制剂，对其他硫化氢/磺胺制硫酶没有活性。I3MT-3 靶向位于 3MST 活性位点的过硫半胱氨酸残基。

研究领域：Stem Cell/Wnt

作用靶点：Hippo (MST)

In Vitro: I3MT-3 (1?μM) is selective for 3MST and shows a high inhibitory activity (80–90%) even at 10?μM in cell lysate of 3MST-overexpressing HEK293 cells. Besides, it is almost inactive towards the other two H2S-producing enzymes even at 100 μM.
I3MT-3 (1?μM) shows a high selectivity for 3MST, it completely suppresses the 3MST activity in COS7 cells living cells.
I3MT-3 produces a concentration-dependent inhibition of the AzMC (the fluorescent H2S probe) signal when incubated with purified human recombinant enzyme, the inhibition of the catalytic activity of 3-MST produces a concentration-dependent inhibition of H2S production with an IC₅₀ of 13.6 ?M.
I3MT-3 shows a dose-dependent inhibition of 3-MST activity from CT26 homogenates, which contain the murine form of the enzyme. The IC₅₀?of HMPSNE for murine 3-MST is calculated as 2.3 ?M with a cozncentration-dependent decrease of AzMC fluorescence.
I3MT-3 (10 ?M-100 ?M; after 3 h probe AzMC) causes a partial inhibition of the signal, while at 100 ?M, HMPSNE causes a complete inhibition of the AzMC-guided H2S fluorescence at 100 ?M, Additionally, HMPSNE is capable of inhibiting its target in situ in CT26 cells (with an IC₅₀?of approximately 30 ?M).
I3MT-3 (0-300 μM; 5-50 hours) does not enhance MTT conversion at 10 ?M, while at 100 and 300 ?M it produces an inhibitory response, without increasing the LDH signal, i.e., without inducing any detectable degree of cell necrosis. It also produces a decreased oxygen consumption rate (OCR) profiles in CT26 cells.
I3MT-3 (0-300 μM; 48 hours) inhibits CT26 cells proliferate with increasing concentrations of I3MT-3. Confluence of cells treated with HMPSNE is recorded each hour for 48 h by the IncuCyte method.

相关产品：Bioactive Compound Library Plus  |  Stem Cell Signaling Compound Library  |  Anti-Aging Compound Library

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