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Targets Recommended: p38 MAPK Autophagy

抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T2277	Losmapimod GSK-AHAB,GW856553X,6-[5-(环丙基氨基甲酰基)-3-氟-2-甲基苯基]-N-(2,2-二甲基丙基)吡啶-3-甲酰胺,GW856553,洛批莫德,SB856553	p38 MAPK; Autophagy	Autophagy; MAPK
	Losmapimod (GSK-AHAB) 是一种可口服的特异性 p38 MAPK 抑制剂，抑制 p38α 和 p38β 的 pKi 值分别为 8.1 和 7.6。
T13324	VUF11207 fumarate	CXCR; Arrestin	Autophagy; GPCR/G Protein; Immunology/Inflammation
	VUF11207 fumarate 是一种 CXCR7激动剂和高效CXCR7配体，pKi 为 8.1。它可诱导CXCR7的β-arrestin2募集和随后的内在化，pEC50分别为 8.8 和 7.9。
T36084	PKI-179
	PKI-179 is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 shows anti-tumor activity in vivo[1][2]. PKI-179 inhibits the cell proliferation, with IC50s of 22 nM and 29 nM for MDA361 and PC3 cells, respectively[1].PKI-179 shows inhibitory activity against a panel of 361 other ...
TP2096	ELA-21 (human)
	High affinity apelin receptor agonist. Binds apelin receptors in left ventricle from normal and pulmonary arterial hypertensive (PAH) hearts (pKi values are 9.31 and 9.46, respectively). Bioactive fragment of ELA-32. Inhibits forskolin-induced cAMP produc
T75989	Malantide TFA
	Malantide TFA 是一种合成的十二肽，由被磷酸化酶激酶β亚基上的PKA 磷酸化的位点衍生而来。Malantide TFA 是PKA 的高度特异性底物，Km 为 15 μM，并且在各种大鼠组织提取物中显示出 PKI 抑制 > 90％底物磷酸化。Malantide TFA 也是PKC 的有效底物，Km 为 16 μM。
T36085	PKI-179 hydrochloride
	PKI-179 is an orally bioavailable dual inhibitor of PI3K and mammalian target of rapamycin (mTOR). In an in vitro enzymatic assay, it potently inhibits PI3K (IC50s = 8, 24, 17, and 74 nM for isoforms α, β, δ, and γ, respectively), two common PI3Kα mutants, E545K and H1047R (IC50s = 14 and 11 nM, respectively), and mTOR (IC50 = 0.42 nM). PKI-179 is selective for PI3K and mTOR over a panel of 361 other kinases at IC50 values up to 50 μM, hERG (IC50 > 30 μM), and cytochrome P450 (CYP) isoforms (IC5...
T78691	PI3Kδ-IN-12	PI3K	PI3K/Akt/mTOR signaling
	PI3Kδ-IN-12（化合物 13）是一款针对PI3Kδ的选择性抑制剂，具有pIC50值为5.8。该化合物对PI3Kδ/γ/β/α的pKi值分别是8.0、6.5、6.4和6.7，适用于慢性呼吸系统疾病如哮喘及慢性阻塞性肺病（COPD）的研究领域。

化合物

Losmapimod

Cat.No: T2277

Synonym: GSK-AHAB,GW856553X,6-[5-(环丙基氨基甲酰基)-3-氟-2-甲基苯基]-N-(2,2-二甲基丙基)吡啶-3-甲酰胺,GW856553,洛批莫德,SB856553

Target: p38 MAPK, Autophagy

VUF11207 fumarate

Cat.No: T13324

Synonym:

Target: CXCR, Arrestin

PKI-179 hydrochloride

Species：

Expression System：

Tag：

Cat. No.	Product Name	Species	Expression System
TMPJ-01309	PKI-Beta Protein, Human, Recombinant (His) PRKACN2,PKI-beta,PKI-β,cAMP-Depen...	Human	E. coli
	cAMP-Dependent Protein Kinase Inhibitor β (PKI-β) is a member of the PKI family. As a member of the cAMP-dependent protein kinase inhibitor family,It has been shown that PKI-β is an extremely potent competitive inhibitor of cAMP-dependent protein kinase activity; this protein interacts with the catalytic subunit of the enzyme after the cAMP-induced dissociation of its regulatory chains. It may play a role in the protein kinase A (PKA) pathway by interacting with the catalytic subunit of PKA, and...

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PKI-Beta Protein, Human, Recombinant (His)

Cat.No: TMPJ-01309

Species: Human

Expression System: E. coli

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