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20

抑制剂 & 化合物

1

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T11831	LDN-27219	Others	Others
	LDN-27219 是一种人组织型转谷氨酰胺酶抑制剂(IC50:600 nM)。
T12909	SID 26681509	Cysteine Protease; Parasite	Microbiology/Virology; Proteases/Proteasome
	SID 26681509 是可逆的，竞争性的人组织蛋白酶 L 选择性抑制剂，IC50为 56 nM。它抑制Plasmodium falciparum 的体外繁殖，IC50为15.4 μM，抑制Leishmania major，IC5012.5 μM。
T25372	EMD57033 EMD-57033,(+)-EMD 57033,EMD 57033	Calcium Channel; Carbonic Anhydrase	Membrane transporter/Ion channel; Metabolism
	EMD57033是一种心脏肌钙蛋白C（cTnC）激活剂，是一种显性的Ca2+增敏剂。EMD57033通过与心脏/慢速骨骼肌钙蛋白C 异构体结合从而发挥促进心脏收缩的功能。
T3193	Pimelic diphenylamide 106 Histone Deacetylase Inhibitor VII,TC-H 106,RGFA-8	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	Pimelic diphenylamide 106 (RGFA-8) 是一种缓慢和紧密结合的I 类HDAC 抑制剂，对HDAC1、 2和3的IC50值分别150、760和370 nM。
TP1570	Cortistatin-14
	Cortistatin 14 is a neuropeptide expressed in inhibitory neurons of the cerebral cortex. Depresses neuronal activity, and induces slow-wave sleep, likely through antagonism of acetylcholine. It is structurally and functionally similar to somatostatin 14.
T61111	UCB-5307	TNF	Apoptosis
	UCB-5307 是一种小分子化合物，可在体外抑制 TNFR1 信号转导和下游功能。人 TNFα 的 KD 为 9 nM。 TNF 直接通过缓慢的结合动力学结合，KD = 6 nM。 UCB-5307 可以通过预制的 hTNF/hTNFR1 复合物。
T6707	Tiotropium Bromide hydrate BA-679 BR hydrate,BA 679BR,噻托溴铵一水合物	AChR	Neuroscience
	Tiotropium Bromide hydrate (BA-679 BR hydrate) 是长效的毒蕈碱受体拮抗剂，可用于治疗慢性阻塞性气道疾病 (COPD)。
T28798	SL-25.1188 SL25.1188
	SL-25.1188 is a monoamine oxidase B (MAO-B) inhibitor. SL-25.1188 is characterized by reversible binding, high brain uptake, and very slow plasma metabolism in vivo.
T38730	Ara-F-NAD+
	Ara-F-NAD+, an arabino analogue of NAD + , is a potent, slow-binding CD38 NADase inhibitor, with a K i of 169 nM.
T24348	L 708286 L708286,L-708286,DFKi
	L 708286 is an agent of peptide-based phenethylcarbamoyldifluoromethylene. It is a slow-binding inhibitor of human leucocyte elastase (HLE).
T15285	FK706	Serine Protease	Proteases/Proteasome
	FK706 is a slow-binding and competitive human neutrophil elastase inhibitor (IC50: 83 nM; Ki: 4.2 nM). FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase (IC50s: 22 nM and 100 nM, respectively). FK706 has an anti-inflammatory ef
T28245	ONO-0300302 ONO 0300302
	ONO-0300302 is a slow tight binding LPA1 antagonist (IC50: 0.16 nM) used to treat Benign Prostatic Hyperplasia. ONO-0300302 inhibits significantly an LPA-induced increase of intraurethral pressure (IUP) in rat (3 mg/kg, p.o.) and dog (1 mg/kg, p.o.) over
T74032	Ara-F-NAD+ sodium
	Ara-F-NAD+ sodium 是一种 NAD+的 arabino 类似物。Ara-F-NAD+ sodium 是一种有效的、可逆的、缓慢结合的CD38NADase 抑制剂。
T38050	CP-609754	Transferase	Metabolism
	CP-609754 是高效的、可逆的法尼基转移酶抑制剂，对重组人 H-Ras 和重组 K-Ras 法尼基化的 IC50分别为 0.57 ng/mL 和 46 ng/mL。CP-609754有潜在的抗癌作用。
T73051	Leritrelvir RAY1216	SARS-CoV	Microbiology/Virology
	Leritrelvir (RAY1216)，一种口服活性SARS-CoV-2主要蛋白酶慢紧抑制剂，其Ki值为8.6 nM。
T29073	UR-2922 UR 2922
	UR-2922 is an oral antagonist of platelet GPIIb/IIIa. UR-2922 possessed a high affinity for the human platelet receptor (K(d) <1 nM) and a slow dissociation rate (k(off)= 90 min) in vitro. UR-2922 induced no ligand-induced binding sites (LIBS) expression
T21681	AACOCF3 Arachidonyl trifluoromethyl ketone,Arachidonyltrifluoromethane	Phospholipase	Metabolism
	AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeable trifluoromethyl ketone analog of arachidonic acid. It is a potent and selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). By blocking the production of arachidonate and 12-hydroxyeicosatetraenoic acid in calcium ionophore-challenged platelets, AACOCF3 hinders their synthesis. Moreover, AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets. Given its diverse applications, AACOCF3 ...
T71000	RO-5328673
	RO-5328673 is a dual NK2/NK3 antagonist. O5328673. [(3)H]RO5328673 bound to a single saturable site on hNK2, hNK3 and gpNK3 with high-affinity. RO5328673 acted as an insurmountable antagonist at both human and guinea-pig NK3 receptors in the [(3)H]IP accumulation assay. In binding kinetic analyses, [(3)H]RO5328673 had fast association and dissociation rates at hNK2 while it had a fast association rate and a remarkably slow dissociation rate at gp and hNK3. In electrophysiological recordings of g...
T37492	11-trans Leukotriene C4 11-trans Leukotriene C4
	11-trans Leukotriene C4 (11-trans LTC4) is a C-11 double bond isomer of LTC4. LTC4 undergoes slow temperature-dependent isomerization to 11-trans LTC4 during storage. 11-trans LTC4 is produced in smaller amounts relative to LTC4 in ionophore-stimulated HMC-1 cells (a human mast cell line) and equine eosinophils, but not in human neutrophils or RBL-1 cells. It is nearly equipotent with LTC4 for contraction of guinea pig parenchymal and ileum. In a radioligand binding assay using guinea pig ileum ...
T71618	Oxocarbazate
	Oxocarbazate, also known as CID23631927, is an inhibitor of human cathepsin L. In the cathepsin L inhibition assay, The oxocarbazate caused a time-dependent 17-fold drop in IC50 from 6.9 nM (no preincubation) to 0.4 nM (4-h preincubation). Slowly reversible inhibition was demonstrated in a dilution assay. CID23631927 demonstrate activity in blocking both SARS-CoV (IC50 = 273 nM) and Ebola virus (IC50 = 193 nM) entry into human embryonic. CID 23631927 was a subnanomolar, slow-binding, reversible...

化合物

Cat.No: T11831

Target: Others

Cat.No: T12909

Target: Cysteine Protease, Parasite

Cat.No: T25372

Synonym: EMD-57033,(+)-EMD 57033,EMD 57033

Target: Calcium Channel, Carbonic Anhydrase

Pimelic diphenylamide 106

Cat.No: T3193

Synonym: Histone Deacetylase Inhibitor VII,TC-H 106,RGFA-8

Target: HDAC

Cat.No: TP1570

Cat.No: T61111

Target: TNF

Tiotropium Bromide hydrate

Cat.No: T6707

Synonym: BA-679 BR hydrate,BA 679BR,噻托溴铵一水合物

Target: AChR

Cat.No: T28798

Synonym: SL25.1188

Cat.No: T38730

Cat.No: T24348

Synonym: L708286,L-708286,DFKi

Cat.No: T15285

Target: Serine Protease

Cat.No: T28245

Synonym: ONO 0300302

Ara-F-NAD+ sodium

Cat.No: T74032

Cat.No: T38050

Target: Transferase

Cat.No: T73051

Synonym: RAY1216

Target: SARS-CoV

Cat.No: T29073

Synonym: UR 2922

Cat.No: T21681

Synonym: Arachidonyl trifluoromethyl ketone,Arachidonyltrifluoromethane

Target: Phospholipase

Cat.No: T71000

11-trans Leukotriene C4

Cat.No: T37492

Synonym: 11-trans Leukotriene C4

Cat.No: T71618

Cat. No.	Product Name	Target	Signaling Pathways
TN3540	Broussonin C	Tyrosinase; Antifection	Microbiology/Virology; Proteases/Proteasome
	Broussonin C and broussin are antifungal compounds. Broussonin C exerts simple reversible slow-binding inhibition against diphenolase.

天然产物

Cat.No: TN3540

Target: Tyrosinase, Antifection

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