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10

抑制剂 & 化合物

3

天然产物

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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。

化合物

CYM5442
Cat.No: T2026
Synonym:
Target: S1P Receptor, LPL Receptor
Zibotentan
Cat.No: T6258
Synonym: ZD4054
Target: Apoptosis, Endothelin Receptor
NTP42
Cat.No: T12268
Synonym:
Target: Prostaglandin Receptor, PPAR
SP4206
Cat.No: T12982
Synonym:
Target: IL Receptor
AMP423
Cat.No: T69821
Synonym:
Target:
Olodanrigan
Cat.No: T4431
Synonym: PD-126055,EMA401
Target: RAAS
AG126
Cat.No: T4092
Synonym: Tyrphostin AG126,AG 126
Target: ERK, COX
Ki16425
Cat.No: T6108
Synonym: Debio 0719
Target: LPA Receptor, LPL Receptor
CYM5442 hydrochloride
Cat.No: T41144
Synonym: CYM 5442 hydrochloride
Target:
STO-609 acetate
Cat.No: T3650
Synonym:
Target: CaMK
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.

天然产物

Albofungin
Cat.No: T26590
Synonym: Antibiotic P42-1,Antibiotic P42-C
Target:
Enniatin B
Cat.No: T13679
Synonym:
Target: ERK
Enniatin B1
Cat.No: T13680
Synonym: 恩镰孢菌素 B1
Target: ERK
TargetMol Loading
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