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Search Results for " nonpeptidic "

22

抑制剂 & 化合物

1

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T3146	BMS-202 PD1-PDL1 inhibitor 2,PD-1/PD-L1 inhibitor 2	Apoptosis; PD-1/PD-L1	Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation
	BMS-202 (PD1-PDL1 inhibitor 2) 是一种非肽类 PD-1/PD-L 复合物抑制剂，其 IC50为 18 nM，KD 为 8 μM。它与 PD-L1 直接结合并阻断人类 PD-1/PD-L 的相互作用，具有抗肿瘤活性。
T9292	ALE-0540 ALE0540	Others; Trk receptor	Others; Tyrosine Kinase/Adaptors
	ALE-0540是一种非肽类杂环分子，可抑制NGF 与p75和TrkA 的结合，以及TrkA 受体介导的信号转导和生物反应。
T4236	AR-M 1000390 hydrochloride ARM390 Hydrochloride,ARM-390 HCl	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	AR-M 1000390 hydrochloride (ARM-390 HCl) 是选择性 δ 阿片受体激动剂，EC50为 7.2±0.9 nM。
T70946	SC 51316
	SC 51316 is a nonpeptidic angiotensin II (AII) receptor antagonist.
T33734	NS 11 NS-11,NS11
	NS 11 is an RGD-nonpeptidic mimetic.
T26082	RID-F Ridaifen-F,Ridaifen F
	RID-F is an inhibitor of the nonpeptidic proteasome.
T12072	ML-00253764 hydrochloride	Others	Others
	ML-00253764 hydrochloride is an antagonist of nonpeptidic melanocortin receptor 4 (MC4R) (Ki and IC50 of 0.16 µM and 0.103 µM, respectively).
T26439	A 74273 A-74273,A74273
	A 74273, a nonpeptidic and renin inhibitor, may be used to treat cardiovascular diseases due to renin inhibition.
T14781	Brilacidin PMX 30063	Others	Others
	Brilacidin is a nonpeptidic anti-infective in a new class of defensin mimetics used for the research of eye infections.
T11369	GB-110	Others	Others
	GB-110 selectively induces PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM. GB-110 is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist.
T69170	ATC0065 HCl
	ATC0065 dihydrochloride is a novel nonpeptidic and potent melanin-concentrating hormone receptor 1 (MCHR1) selective antagonist.
T27661	JNJ-10329670
	JNJ 10329670 is a highly potent (Ki of approximately 30 nM), nonpeptidic, noncovalent inhibitor of human cathepsin S with immunosuppressive activity.
T11369L	GB-110 hydrochloride (1252806-70-4 free base) GB-110 hydrochloride	Others	Others
	GB-110 hydrochloride selectively induces PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM. GB-110 hydrochloride is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist.
T16851	SB-267268	Others	Others
	SB-267268 inhibits human and mouse αvβ3 (IC50s: 0.68 and 0.29 nM, respectively). SB-267268 is a selective and nonpeptidic alpha(v)beta3 and alpha(v)beta5 integrins antagonist (Kis: 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respective
T13846	PROTAC RIPK degrader-2	Others	Others
	PROTAC RIPK degrader-2 is a nonpeptidic PROTAC ,and potently targets serine-threonine kinase RIPK2 and has highly selective for RIPK2 degradation.
T11630L	IFN alpha-IFNAR-IN-1	Others	Others
	IFN alpha-IFNAR-IN-1 is a nonpeptidic, low-molecular-weight inhibitor of the interaction between IFN-α and IFNAR. It inhibits MVA-induced IFN-α responses by BM-pDCs (IC50: 2-8 μM).
T73854	GB-110 hydrochloride
	GB-110 hydrochloride 是一种有效的，具有口服活性的，非肽类的 protease activated receptor2 (PAR2)激动剂。GB-110 hydrochloride 选择性诱导 PAR2介导的 HT29 细胞内 Ca2+释放，EC50值为 0.28 μM。
T61210	R-PSOP
	R-PSOP is a potent and selective nonpeptidic NMUR2 antagonist, exhibiting binding affinity to human and rat NMUR2 with Ki values of 52 nM and 32 nM, respectively. This compound demonstrates moderate central nervous system (CNS) penetration and is valuable in the study of eating disorders, obesity, pain, and stress-related disorders [1].
T21786	Apogossypolone (ApoG2)
	Apogossypolone (ApoG2) 是一种具有口服活性的Bcl-2 家族蛋白抑制剂，对 Bcl-2, Mcl-1 和 Bcl-XL 的Ki 值分别为 35, 25 和 660 nM。Apogossypolone 具有抗肿瘤活性，可诱导细胞凋亡 (apoptosis) 和自噬 (autophagy)。Apogossypolone 具有抗真菌活性。
T79455	SARS-CoV-2 Mpro-IN-9	SARS-CoV	Microbiology/Virology
	SARS-CoV-2 Mpro-IN-9 (compound c7) 是非肽类、非共价型SARS-CoV-2 Mpro抑制剂，IC50值为0.085 μM，展现出改进的物化特性和药物代谢及药动学 (DMPK) 性质。在Vero E6 细胞中，对SARS-CoV-2感染显示抑制效果，EC50为1.10 μM，同时具备低细胞毒性（CC50>50 μM）。
T38372	2-Fluoro-4-iodo benzonitrile
	2-Fluoro-4-iodo benzonitrile is a building block.1,2It has been used in the synthesis ofL. infantumtrypanothione reductase (Li-TryR) dimerization and oxidoreductase activity inhibitors.12-Fluoro-4-iodo benzonitrile has also been used in the synthesis of transient receptor potential ankyrin 1 (TRPA1) antagonists.2 1.Revuelto, A., Ruiz-Santaquiteria, M., de Lucio, H., et al.Pyrrolopyrimidine vs imidazole-phenyl-thiazole scaffolds in nonpeptidic dimerization inhibitors of Leishmania infantum trypan...
T36393	CAY10727
	CAY10727 is an inhibitor of protein arginine deiminase 3 (PAD3; kinact/KI= 15,600 M-1min-1).1It is selective for PAD3 over PAD1, -2, and -4 (kinact/KIs = 360, 1,110, and 1,460 M-1min-1, respectively). 1.Jamali, H., Khan, H.A., Stringer, J.R., et al.Identification of multiple structurally distinct, nonpeptidic small molecule inhibitors of protein arginine deiminase 3 using a substrate-based fragment methodJ. Am. Chem. Soc.137(10)3616-3621(2015)

化合物

Cat.No: T3146

Synonym: PD1-PDL1 inhibitor 2,PD-1/PD-L1 inhibitor 2

Target: Apoptosis, PD-1/PD-L1

Cat.No: T9292

Synonym: ALE0540

Target: Others, Trk receptor

AR-M 1000390 hydrochloride

Cat.No: T4236

Synonym: ARM390 Hydrochloride,ARM-390 HCl

Target: Opioid Receptor

Cat.No: T70946

Cat.No: T33734

Synonym: NS-11,NS11

Cat.No: T26082

Synonym: Ridaifen-F,Ridaifen F

ML-00253764 hydrochloride

Cat.No: T12072

Target: Others

Cat.No: T26439

Synonym: A-74273,A74273

Cat.No: T14781

Synonym: PMX 30063

Target: Others

Cat.No: T11369

Target: Others

Cat.No: T69170

Cat.No: T27661

GB-110 hydrochloride (1252806-70-4 free base)

Cat.No: T11369L

Synonym: GB-110 hydrochloride

Target: Others

Cat.No: T16851

Target: Others

PROTAC RIPK degrader-2

Cat.No: T13846

Target: Others

IFN alpha-IFNAR-IN-1

Cat.No: T11630L

Target: Others

GB-110 hydrochloride

Cat.No: T73854

Cat.No: T61210

Apogossypolone (ApoG2)

Cat.No: T21786

SARS-CoV-2 Mpro-IN-9

Cat.No: T79455

Target: SARS-CoV

2-Fluoro-4-iodo benzonitrile

Cat.No: T38372

Cat.No: T36393

Cat. No.	Product Name	Target	Signaling Pathways
T6485	Embelin NSC 91874,恩贝酸,恩贝酸/恩贝灵,Emberine,Embelic acid	Apoptosis; NF-κB; Lipoxygenase; IAP; Prostaglandin Receptor; Autophagy	Apoptosis; Autophagy; GPCR/G Protein; Immunology/Inflammation; Metabolism; NF-κB
	Embelin (Embelic acid) 是从日本 Ardisia 草药中分离出来的一种非肽类细胞渗透性XIAP 抑制剂，诱导口腔鳞癌细胞自噬和凋亡。它阻断 NF-kappaB 信号通路，从而抑制 NF-kappaB 调节的抗凋亡和转移基因产物。在高水平 XIAP 的前列腺癌细胞中抑制细胞生长，诱导凋亡，并激活 caspase-9。

天然产物

Cat.No: T6485

Synonym: NSC 91874,恩贝酸,恩贝酸/恩贝灵,Emberine,Embelic acid

Target: Apoptosis, NF-κB, Lipoxygenase, IAP, Prostaglandin Receptor, Autophagy

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