Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T36778 |
MK2-IN-1
MK2-IN-1 (MK2 Inhibitor) |
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MK2-IN-1 is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode. | |||
T4442 |
MK2-IN-1 hydrochloride
MK2 Inhibitor,MK 25 |
MAPK | MAPK |
MK2-IN-1 hydrochloride (MK 25) 是一种高效的选择性 MAPKAPK2(MK2)激酶抑制剂,其 IC50值为0.11uM。 | |||
T9034 |
MK2-IN-3
MK2 Inhibitor III |
MAPK | MAPK |
MK2-IN-3 (MK2 Inhibitor III) 是选择性的 MAPKAP-K2 (MK-2)抑制剂(IC50:8.5 nM),能够抑制 U937 细胞及体内 TNFα 的生成。 | |||
T12058 |
MK2-IN-3 hydrate
MK-2 Inhibitor III |
ERK; MAPK; MNK | MAPK |
MK2-IN-3 hydrate (MK-2 Inhibitor III) 是一种口服有活性的、ATP 竞争性的MAPKAP-K2 (MK-2)选择性抑制剂(IC50:0.85 nM)。 | |||
T14988 |
CMPD1
|
MAPK | MAPK |
CMPD1 是非 ATP 竞争性 p38 MAPK 介导的 MK2磷酸化选择性抑制剂(Ki:330 nM)。 | |||
T81783 |
MK2-IN-5
Hsp25 kinase inhibitor,Mk2 pseudosubstrate |
ERK | MAPK |
MK2-IN-5为Mk2的假底物,Ki值为8 μM。该化合物针对MAPK通路内的蛋白相互作用域,并能抑制HSP25与HSP27的磷酸化。 | |||
T16501 |
PF-3644022
|
p38 MAPK; Serine Protease; MAPK | MAPK; Proteases/Proteasome |
PF-3644022 是可口服的,具有 ATP 竞争性的MAPKAPK2 (MK2)选择性抑制剂,IC50为 5.2 nM,Ki 为 3 nM。它有效抑制 TNFα 的产生并具有抗炎作用,还抑制 MK3 和 p38 调节/激活激酶,IC50分别为 53 和 5.0 nM。 | |||
T60657 | (R)-STU104 | TNF; MAPK | Apoptosis; MAPK |
(R)-STU104 是一种新型 TAK1-MKK3 蛋白-蛋白相互作用 (PPI)抑制剂,抑制 TNF-α,通过与 MKK3 结合并破坏TAK1磷酸化MKK3来抑制TAK1/MKK3/p38/MnK1/MK2/elF4E信号通路。(R)-STU104 是治疗溃疡性结肠炎的候选化合物。 | |||
T6940 |
PHA-767491 hydrochloride
CAY10572,PHA-767491,PHA767491 HCl,CAY-10572 hydrochloride |
Apoptosis; GSK-3; CDK | Apoptosis; Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells |
PHA-767491 hydrochloride (CAY-10572 hydrochloride) 是一种Cdc7-Dbf4(DDK)/Cdk9的双重抑制剂,IC50值分别为 10 nM 和 34 nM。 | |||
T39321 |
CC-99677
CC99677,Gamcemetinib,CC 99677 |
HSP; MAPK | Cytoskeletal Signaling; MAPK; Metabolism |
CC-99677 (Gamcemetinib) 是一种一种用于自身免疫性疾病的选择性靶向共价MAPKAPK2(MK2)抑制剂,通过亲核芳族取代(SNAr)机制将生化效力转化为LPS活化的单核细胞THP-27细胞中热休克蛋白27(HSP1)磷酸化的有效抑制所显示的细胞效力。CC-99677 在大鼠实验中展现出在生化(IC 50 =156.3 nM)和细胞检测(EC 50 =89 nM)中均有 | |||
T5494 |
MW-150
MW01-18-150SRM |
p38 MAPK; Autophagy | Autophagy; MAPK |
MW-150 (MW01-18-150SRM) 是一种选择性、CNS 渗透性和口服活性的 p38α MAPK 抑制剂,Ki 为 101 nM。它可抑制内源性 p38α MAPK 在活化的神经胶质中磷酸化内源性底物 MK2 的能力。 | |||
T62110 | MK2-IN-4 | ||
MK2-IN-4 是一种 MAPKAPK2 (MK2) 抑制剂 (IC50: 45 nM)。MK2-IN-4 能够用于癌症、炎症和免疫学的研究。 | |||
T72202 |
Anti-inflammatory agent 33
|
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Anti-inflammatory agent 33,一种有效的p38α抑制剂,抑制NO产生,并抑制LPS诱导的iNOS、COX-2、p-p38α、p-MK2蛋白表达,具有抗炎活性。 | |||
T39126 |
Zunsemetinib
CDD-450,ATI-450 |
||
Zunsemetinib (CDD-450) is a potent and specific inhibitor of the p38α-MK2 pathway, exerting its effects through oral administration. It has proven activity against immuno-inflammatory diseases, making it a valuable tool for research in this area. | |||
T16721 |
Ralimetinib
LY2228820 |
Others | Others |
Ralimetinib selectively inhibits phosphorylation of MK2 (Thr334) and has no effect on phosphorylation of p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc. Ralimetinib is an effective and selective, ATP-competitive inhibitor of p38 MAPK α/β (IC50s: 5.3 and 3. | |||
T39343 |
MW-150 hydrochloride
MW01-18-150SRM hydrochloride,MW-150 hydrochloride |
||
MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a potent and selective inhibitor of p38α MAPK, with a Ki value of 101 nM. It exhibits excellent CNS penetration and oral bioavailability. MW-150 hydrochloride (MW01-18-150SRM hydrochloride) effectively suppresses the phosphorylation of MK2, a substrate of endogenous p38α MAPK, in activated glial cells. | |||
T5487 | MW-150 dihydrochloride dihydrate | ||
MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) 是一种选择性的,可透过神经系统,具有口服活性的的p38α MAPK 抑制剂,Ki 值为 101 nM。MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) 抑制内源性 p38α MAPK 磷酸化活化的神经胶质中内源性底物 MK2 的能力。 | |||
T76242 |
MMI-0100
|
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MMI-0100 是一种细胞渗透性肽抑制剂,抑制丝裂原活化蛋白激酶活化蛋白激酶 II (MK2)。MMI-0100 在体内外减少内膜增生。MMI-0100 抑制IL-6表达而不影响IL-8表达。MMI-0100 抑制纤维化过程,例如静脉移植疾病。 | |||
T35536 |
Tpl2 Kinase Inhibitor (hydrochloride)
|
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Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50= 0.05 μM).1It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 μM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 μM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 μM.2Tpl2 kinase inhibitor (5... |