mp 10

MP-10 succinate is a potent and specific inhibitor of PDE10A.

[11C]MP 10 (PF-2545920) 是一种特异性且有效的 PDE10A 抑制剂 (IC50=0.37 nM)，其特异性活性是 PDE 的 1000 倍以上。

Oleoylestrone (MP-101) 存在于血浆和脂肪组织中，具有潜在的抗氧化作用，可诱导大鼠体内脂肪的流失，可用于减肥。

CM-352是一种金属蛋白酶抑制剂，可减少脑损伤并改善脑出血大鼠模型的功能恢复。

MMP-9 10-IN-2 (compound 6e) 是 MMP10 和 MMP9 的强效抑制剂，对 MMP10 的 IC50MMP10 为 0.076 μM，对 MMP9 的抑制浓度为 0.5 μM，抑制率达到 93.18%。该化合物在抗肿瘤治疗中具有重要作用。

IMP-1088 是一种人N-肉豆蔻酰基转移酶NMT1和NMT2双重抑制剂，对 HsNMT1 和 HsNMT2 的IC50小于1 nM，对 HsNMT1 的Kd 小于210 pM。它有保护宿主细胞免受病毒感染的细胞毒作用，通过阻断鼻病毒的 N-肉豆蔻酰化蛋白来阻断鼻病毒的复制。

NHC-diphosphate is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) as a diphosphate form[1]. NHC is a pyrimidine ribonucleoside and behaves as a potent anti-virus agent. NHC effectively inhibits the replication of venezuelan equine encephalitis virus (VEEV), Chikungunya virus (CHIKV) and hepatitis C virus (HCV)[1]. Huh-7 cells are incubated with (10-50 μM; 4 h) NHC or a McGuigan phosphoramidate prodrug of NHC.Intracellular levels of the parental compounds and phosphorylated metabolites are measured using LC-MS MS. Small amounts of NHC-monophosphate (MP) and NHC-diphosphate can be observed, while NHC-triphosphate remains the most abundant metabolite.[1].

NHC-triphosphate triammonium is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) as a triphosphate form[1]. NHC-triphosphate triammonium is a weak alternative substrate for the viral polymerase and can be incorporated into HCV replicon RNA[1][2]. In an intracellular metabolism assay, HCV replicon cells are treated with 10 μM 3H-labeled NHC, and intracellular nucleotide levels are determined after 1, 2 and 8 hours incubations. NHC is rapidly convered into the mono-, di-, and triphosphate forms, and NHC-TP reaches up to 71.12 pM after 8 hours[1].NHC-triphosphate triammonium (NHC-TP) (5-40 μM) absence leads to full-length polymerization products, it can be a weak alternative substrate. In addition, incorporation of NHC-TP instead of CTP increases the molecular weight of the polymerization product by 16 (one extra oxygen) for each event and an obvious electrophoretic shift is observed in cell-free HCV NS5B polymerization reactions[1].Huh-7 cells are incubated with (10-50 μM; 4 h) NHC or a McGuigan phosphoramidate prodrug of NHC. Intracellular levels of the parental compounds and phosphorylated metabolites are measured using LC-MS MS. Small amounts of NHC-monophosphate (MP) and NHC-diphosphate (DP) can be observed, while NHC-triphosphate triammonium remains the most abundant metabolite[2].NHC-triphosphate triammonium (NHC-TP) metabolite may directly target the viral polymerase and behave as a nonobligate chain terminator. It plays a prominent role in inhibiting early negative-strand RNA synthesis, either through chain termination or mutagenesis, which may in turn interfere with correct replicase complex formation. [1]. Stuyver LJ,et al. Ribonucleoside analogue that blocks replication of bovine viral diarrhea and hepatitis C viruses in culture.Antimicrob Agents Chemother. 2003 Jan;47(1):244-54. [2]. Maryam Ehteshami, et al. Characterization of β-d- N4-Hydroxycytidine as a Novel Inhibitor of Chikungunya Virus.

XMU-MP-3 is a robust, non-covalent inhibitor of BTK, exhibiting exceptional potency with IC50 values of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation, respectively, in the presence of 10 μM ATP. Moreover, XMU-MP-3 elicits apoptosis.

Mardepodect hydrochloride (Mardepodect HCl) 是一种可穿过血脑屏障且具有口服活性的、选择性和高效性的 PDE10A 抑制剂（IC50 ：0.37 nM）。Mardepodect hydrochloride 可上调编码特定生长因子、转录因子、细胞信号分子和细胞表面蛋白的基因，同时下调广泛的可靶向细胞周期和细胞凋亡相关基因。