MPS1

抑制剂选择性比较

MPS1产品

所有产品(5) MPS1抑制剂(5)

目录号	产品描述	文献引用	实验数据
S2731	AZ 3146 AZ 3146是一种选择性Mps1抑制剂，IC50为35 nM左右，有助于聚集CENP-E(驱动蛋白相关的动力蛋白)，对FAK， JNK1， JNK2和Kit作用效果稍弱。	Nat Cell Biol, 2020, 22(7):856-867 Oncogene, 2020, 39(13):2819-2834 Front Cell Dev Biol, 2020, 8:601972	Dose response curves for the treatment of breast cancer cell lines in the absence or presence of escalating doses of the TTK inhibitor (TTKi) AZ3146. The survival of cells was measured using the CellTitre MTS/MTA assay carried out 6 days after treatment. Percentage survival (n ¼ 3 per dose) was calculated as the percentage of the signal from treated cells to that from control cells.
S8214^New	Empesertib (BAY1161909) Empesertib (BAY1161909, Mps1-IN-5) 是一种三唑并吡啶的衍生物，是 serine/threonine monopolar spindle 1 (Mps1) kinase 的口服生物利用型选择性抑制剂，IC50值 <1 nM。 Empesertib 具有潜在的抗肿瘤活性。
S8215	BAY 1217389 BAY 1217389一种具有生物口服活性的、选择性丝氨酸/苏氨酸激酶monopolar spindle 1 (Mps1)抑制剂，IC50低于10 nM，具有良好的选择性。	Dev Cell, 2020, 52(4):413-428 Nature, 2019, 575(7781):203-209
S7488	MPI-0479605 MPI-0479605 是一种ATP竞争性的选择性的有丝分裂激酶Mps1抑制剂，IC50为1.8 nM, 其选择性超过其他激酶40倍。	Front Pharmacol, 2020, 30;11:543 Curr Biol, 2019, 29(18):3072-3080 Curr Biol, 2019, 29(18):2993-3005
S0426^New	Pim1/AKK1-IN-1 Pim1/AKK1-IN-1 (LKB1/AAK1 dual inhibitor, MDK-2275) is a potent multi-kinase inhibitor with Kd of 35 nM, 53 nM, 75 nM and 380 nM for Pim1, AKK1, MST2 and LKB1, respectively. Pim1/AKK1-IN-1 also inhibits MPSK1 and TNIK.

目录号	产品描述	文献引用	实验数据
S2731	AZ 3146 AZ 3146是一种选择性Mps1抑制剂，IC50为35 nM左右，有助于聚集CENP-E(驱动蛋白相关的动力蛋白)，对FAK， JNK1， JNK2和Kit作用效果稍弱。	Nat Cell Biol,2020, 22(7):856-867 Oncogene,2020, 39(13):2819-2834 Front Cell Dev Biol,2020, 8:601972	Dose response curves for the treatment of breast cancer cell lines in the absence or presence of escalating doses of the TTK inhibitor (TTKi) AZ3146. The survival of cells was measured using the CellTitre MTS/MTA assay carried out 6 days after treatment. Percentage survival (n ¼ 3 per dose) was calculated as the percentage of the signal from treated cells to that from control cells.
S8214^New	Empesertib (BAY1161909) Empesertib (BAY1161909, Mps1-IN-5) 是一种三唑并吡啶的衍生物，是 serine/threonine monopolar spindle 1 (Mps1) kinase 的口服生物利用型选择性抑制剂，IC50值 <1 nM。 Empesertib 具有潜在的抗肿瘤活性。
S8215	BAY 1217389 BAY 1217389一种具有生物口服活性的、选择性丝氨酸/苏氨酸激酶monopolar spindle 1 (Mps1)抑制剂，IC50低于10 nM，具有良好的选择性。	Dev Cell,2020, 52(4):413-428 Nature,2019, 575(7781):203-209
S7488	MPI-0479605 MPI-0479605 是一种ATP竞争性的选择性的有丝分裂激酶Mps1抑制剂，IC50为1.8 nM, 其选择性超过其他激酶40倍。	Front Pharmacol,2020, 30;11:543 Curr Biol,2019, 29(18):3072-3080 Curr Biol,2019, 29(18):2993-3005
S0426^New	Pim1/AKK1-IN-1 Pim1/AKK1-IN-1 (LKB1/AAK1 dual inhibitor, MDK-2275) is a potent multi-kinase inhibitor with Kd of 35 nM, 53 nM, 75 nM and 380 nM for Pim1, AKK1, MST2 and LKB1, respectively. Pim1/AKK1-IN-1 also inhibits MPSK1 and TNIK.