10
3
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2026 |
CYM5442
|
S1P Receptor; LPL Receptor | GPCR/G Protein |
CYM5442 是高选择性和口服活性的鞘氨醇 1-磷酸受体激动剂,EC50为 1.35 nM。它激活依赖 S1P1的 p42/p44-MAPK 磷酸化,具有视网膜神经保护作用,可轻松穿过中枢神经系统。 | |||
T6258 |
Zibotentan
ZD4054 |
Apoptosis; Endothelin Receptor | Apoptosis; GPCR/G Protein |
Zibotentan (ZD4054) 是一种选择性的,具有口服活性的内皮素 A (ETA) 受体拮抗剂,Ki 为 13 nM。它具有抗癌作用,可研究去势抵抗性前列腺癌。 | |||
T12268 |
NTP42
|
Prostaglandin Receptor; PPAR | DNA Damage/DNA Repair; GPCR/G Protein; Immunology/Inflammation; Metabolism |
NTP42 是血栓素 A2 (TXA2) 受体的拮抗剂,IC50为 3.278 nM,可用于肺动脉高压的相关研究。 | |||
T12982 |
SP4206
|
IL Receptor | Immunology/Inflammation |
SP4206 is an interaction inhibitor of IL-2/IL-2Rα (IL-2 and IL-2Rα with Kd of 70 nM and 10 nM,respectively) | |||
T69821 |
AMP423
|
||
AMP423 is a naphthyl derivative of 2-cyanoaziridine-1-carboxamide with structural similarity to the pro-oxidant anti-tumor agent imexon. AMP423 was active in SCID mice bearing 8226/S myeloma and SU-DHL-6 B-cell lymphoma tumors, with a median tumor growth delay (T-C) of 21 days (P = 0.0002) and 5 days (P = 0.004), respectively, and a median tumor growth inhibition (T/C) of 33.3% (P = 0.03) and 82% (P = 0.01), respectively. In non-tumor-bearing mice, AMP423 was not myelosuppressive. | |||
T4431 |
Olodanrigan
PD-126055,EMA401 |
RAAS | Endocrinology/Hormones |
Olodanrigan (EMA401) 是具有口服活性、高选择性及外周受限的血管紧张素 Ⅱ 类型 2 受体(AT2R)拮抗剂。它的缓解疼痛的机制可能是:抑制增强的 AngII/AT2R 诱导的 p38 和 p42/p44 MAPK 激活,进而阻碍 DRG 神经元的过度兴奋性及 DRG 神经元的萌发。它可用于研究神经性疼痛。 | |||
T4092 |
AG126
Tyrphostin AG126,AG 126 |
ERK; COX | Immunology/Inflammation; MAPK; Neuroscience |
AG126 (Tyrphostin AG126) 是一种酪氨酸激酶抑制剂,可阻止丝裂原活化蛋白激酶 p42MAPK(ERK2) 的激活。 | |||
T6108 |
Ki16425
Debio 0719 |
LPA Receptor; LPL Receptor | GPCR/G Protein |
Ki16425 (Debio 0719) 是一种竞争性、有效和可逆的 LPA1、LPA2 和 LPA3 拮抗剂,Ki 分别为 0.34、6.5 和 0.93 μM。它可抑制LPA 诱导的 HEK293A 细胞中 YAP/TAZ 的去磷酸化,降低LPA 诱导的 p42/p44 MAPK 激活。 | |||
T41144 |
CYM5442 hydrochloride
CYM 5442 hydrochloride |
||
CYM 5442 hydrochloride is a potent and selective S1P1agonistin vitro(EC50 = 1.35 nM). Activates S1P1-mediated p42/p44 MAPK phosphorylation in CHO-K1 cells transfected with S1P1. Induces acute lymphopenia in mice. Brain penetrant. | |||
T3650 |
STO-609 acetate
|
CaMK | Neuroscience |
STO-609 acetate 是选择性的、细胞可渗透的 Ca2+-钙调蛋白依赖性蛋白激酶激酶抑制剂(Ki:80/15 ng/ml,对于 CaM-KKα/KKβ);竞争 ATP 结合位点。它比 CaMK1/2/4、PKC、MLCK、PKA 和 p42 MAPK 显示 > 80 倍的选择性。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T26590 |
Albofungin
Antibiotic P42-1,Antibiotic P42-C |
||
Albofungin is a xanthone isolated from A. tumemacerans. | |||
T13679 |
Enniatin B
|
ERK | MAPK |
Enniatins B decreases the activation of ERK (p44/p42). Enniatin B is a Fusarium mycotoxin. Enniatin B inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 113 μM in an enzyme assay using rat liver microsomes. | |||
T13680 |
Enniatin B1
恩镰孢菌素 B1 |
ERK | MAPK |
Enniatin B1 crosss the blood-brain barrier. Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation.Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 73 μM in an enzyme assay using rat liver microsomes. |