Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T9697 |
ASK1-IN-1
|
ASK | Apoptosis |
ASK1-IN-1 是一种凋亡信号调节激酶 1(SK1) 抑制剂,具有良好的效价 (细胞IC50=138 nM; BiochemicalIC50=21 nM)。ASK1-IN-1具有中枢神经系统渗透性。 | |||
T9377 |
ASK1-IN-2
|
Apoptosis; ASK; MAPK | Apoptosis; MAPK |
ASK1-IN-2 是一种口服有活性的凋亡信号调节激酶 1 抑制剂(IC50:32.8 nM)。它可用于研究溃疡性结肠炎。 | |||
T67857 |
ASK1-IN-4
|
ASK | Apoptosis |
ASK1-IN-4 是一种ASK1抑制剂,IC50 = 0.2 μM。 | |||
T61584 |
ASK1-IN-3
|
||
ASK1-IN-3 is a highly potent and selective inhibitor of ASK1 kinase, demonstrating an IC 50 of 33.8 nM. This compound also exhibits inhibitory effects on various cell cycle regulating kinases. ASK1-IN-3 showcases remarkable induction of apoptosis in HepG2 cancer cells and displays potent activity in arresting the cell cycle [1]. | |||
T13099 |
TC ASK 10
|
ASK; MAPK | Apoptosis; MAPK |
TC ASK 10 是选择性的,口服有效的细胞凋亡信号调节激酶 1 抑制剂,IC50为 14 nM。它对其他代表性激酶的抑制活性低于 50%,除 ASK2之外 (IC50为 0.51 μM)。 | |||
T35897 |
ASK120067
|
||
ASK120067 is a potent and orally active inhibitor of EGFRT790M (IC50:0.3 nM) with selectivity over EGFRWT (IC50:6.0 nM). ASK120067 is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC)[1]. In the in vitro kinase assay ASK120067 potently inhibits the EGFR L858R/T790M and EGFR T790M resistant mutants with IC50 values of 0.3 nM and 0.5 nM, respectively, as well as the EGFRexon19del sensitizing mutant (IC50= 0.5 nM). The 50 of ASK120067 against wild-type EGFR (EGFRWT... | |||
T33514 |
MSC 2032964A
MSC-2032964A,MSC2032964A |
ASK | Apoptosis |
MSC 2032964A 是一种有效的选择性 ASK1 抑制剂 (IC50 = 93 nM),具有口服生物利用度和脑渗透性。它在小鼠 EAE 模型中抑制神经炎症,并在培养的小鼠星形胶质细胞中阻断 LPS 诱导的 ASK1 和 p38 磷酸化。 | |||
T5190 |
GS-444217
GS 444217,GS444217 |
Apoptosis; ASK; MAPK | Apoptosis; MAPK |
GS-444217 是一种可口服的选择性 ATP 竞争性凋亡信号调节激酶 1 抑制剂,IC50为 2.87 nM。 | |||
T3101 |
NQDI-1
NQDI1,NQDI 1 |
Apoptosis; ASK; MAPK | Apoptosis; MAPK |
NQDI-1 (NQDI 1) 是一种凋亡信号调节激酶 1 抑制剂,Ki 为 500 nM,IC50为 3 μM。 | |||
T3350 |
Selonsertib
GS-4997 |
Apoptosis; ASK; MAPK | Apoptosis; MAPK |
Selonsertib (GS-4997) 是一种选择性的,具有生物口服可利用的凋亡信号调节激酶1 抑制剂,pIC50为 8.3。它具有潜在的抗炎、抗肿瘤和抗纤维化活性。 | |||
T70893 | K811 | ||
K811 is an ASK1-specific inhibitor that prolongs survival in a mouse model of amyotrophic lateral sclerosis. K811 efficiently prevented cell proliferation in cell lines with high ASK1 expression and in HER2-overexpressing GC cells. Treatment with K811 reduced sizes of xenograft tumors by downregulating proliferation markers. | |||
T70892 |
K812
|
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K812 is an ASK1-specific inhibitor discovered to prolong survival in a mouse model of amyotrophic lateral sclerosis. | |||
T68430 |
BPyO-34
|
||
BPyO-34 is a novel apoptosis signal-regulating kinase 1 (ASK1) inhibitor with IC50 of 0.52μM in vitro in kinase assay. | |||
T73460 |
DDO3711
|
||
DDO3711是通过化学接头将ASK1 (小分子凋亡信号调节激酶1) 抑制剂与PP5 (磷酸酶) 激活剂连接,形成特定于招募PP5的磷酸酶募集嵌合体(PHORC)。该化合物特异性地抑制ASK1 (IC50=164.1 nM),而对ASK2 (IC50>20 μM)无影响。通过募集PP5,DDO3711显著促进p-ASK1T838的去磷酸化,表现出ASK1依赖性的抗增殖活性,显示其抗癌潜力并可用于研究异常磷酸化癌蛋白。 | |||
T70622 | Selonsertib HCl | ||
Selonsertib, also known as GS-4997, is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. GS-4997 targets and binds to the catalytic kinase domain of ASK1 in an ATP-competitive manner, thereby preventing its phosphorylation and activation. GS-4997 prevents the production of inflammatory cytokines, down-regulates the expression of genes involved in fibrosis, suppresses excessive apoptosis ... | |||
TP2127 |
R18
|
||
Antagonist of 14.3.3 proteins (KD ≈80 nM). Competitively inhibits 14.3.3-ligand interactions without requiring phosphorylation. Blocks the ability of 14.3.3 to bind to target proteins such as Raf-1, Bad, ASK1 and exoenzyme S. | |||
T36610 |
(E)-2-(2-Chlorostyryl)-3,5,6-trimethylpyrazine
|
||
(E)-2-(2-Chlorostyryl)-3,5,6-trimethylpyrazine (CSTMP) is a stilbene derivative with antioxidant and anticancer activities. It stimulates proliferation of hydrogen peroxide-damaged ECV-304 cells (EC50 = 24.9 nM). CSTMP reduces hydrogen peroxide-induced release of lactate dehydrogenase (LDH) in and increases viability of human umbilical vein endothelial cells (HUVECs) in a concentration-dependent manner via inhibition of apoptosis. It reverses hydrogen peroxide-induced release of malondialdehyde ... |