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20

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T40711	H-D-Phe-Pip-Arg-pNA dihydrochloride S-2238 dihydrochloride,H-D-Phe-Pip-Arg-pNA dihydrochloride	Others	Others
	H-D-Phe-Pip-Arg-pNA dihydrochloride (S-2238 dihydrochloride), a chromogenic substrate, mimics the N-terminal fragment of the A alpha chain of fibrinogen, the native substrate of thrombin. Specifically designed for thrombin detection, H-D-Phe-Pip-Arg-pNA dihydrochloride is employed for the quantification of antithrombin-heparin cofactor (AT-III). The AT-III assay utilizing this substrate is characterized by its sensitivity, accuracy, and ease of implementation.
T9011	VU0155094 ML 397,ML-397,VU 0155094,VU-0155094	GluR	Neuroscience
	VU0155094 (ML 397) 是一种正变构调节剂，对各种 III 组 mGluR 具有不同的活性
T27444	GSK 932121 GSK-932121,GSK932121
	GSK 932121 is a potent antimalarial agent. GSK 932121 inhibits selectively the electron-transport chain in P. falciparum at the cytochrome bc1 level (complex III).
T39066	H-D-Phe-Pip-Arg-pNA hydrochloride S-2238 hydrochloride,H-D-Phe-Pip-Arg-pNA hydrochloride
	H-D-Phe-Pip-Arg-pNA hydrochloride, a chromogenic substrate, mimics the N-terminal segment of the A alpha chain of fibrinogen, the native substrate of thrombin. It displays specificity towards thrombin and is employed for quantifying antithrombin-heparin cofactor (AT-III). The utilization of H-D-Phe-Pip-Arg-pNA hydrochloride in the AT-III assay enables a sensitive, accurate, and straightforward measurement process.
T37851	Chlorido[N,N'-disalicylidene-1,2-phenylenediamine]iron(III)
	Chlorido[N,N'-disalicylidene-1,2-phenylenediamine]iron(III) is an inducer of ferroptosis.1 It induces ferroptosis, but not apoptosis or necroptosis, in NB1 cancer cells when used at a concentration of 3 μM.1 Chlorido[N,N'-disalicylidene-1,2-phenylenediamine]iron(III) inhibits proliferation of BJAB, NALM-6, Jurkat, MelHO, and MCF-7 cancer cells (IC50s = 0.07, 2.5, 1.5, 3, and 5 μM, respectively), as well as NALM-6 cells resistant to daunorubicin and vincristine when used at concentrations ranging...
T35966	Mn(III)TMPyP
	Mn(III)TMPyP is a manganese-porphyrin which acts as a superoxide dismutase (SOD) mimetic and peroxynitrite decomposition catalyst. SOD mimetics described to date are unstable and are capable of catalyzing undesired side-reactions in addition to the dismutation of the superoxide radical (O2-). Mn(III)TMPyP is an SOD mimetic with increased stability to pH and hydrogen peroxide. The rate constant for superoxide dismutation and peroxynitrite decomposition are 3.9 x 107 M-1s-1 and ~2 x 106 M-1s-1, re...
T37498	Antimycin A4
	Antimycin A4 is an active component of the antimycin A antibiotic complex that is more polar than antimycin A1 , antimycin A2 , and antimycin A3 . Antimycin A4 inhibits ATP-citrate lyase with a Ki value of 64.8 μM. The antimycin A complex is a mixture of antimycins A1, A2, A3, and A4 that demonstrates antifungal, insecticidal, nematocidal, and piscicidal properties. It blocks mitochondrial respiration and can deplete cellular levels of ATP via inhibition of complex III of the mitochondrial elect...
T35821	CAY10721
	CAY10721 is an inhibitor of sirtuin 3 (SIRT3), a class III HDAC (39% SIRT3 inhibition at 200 μM). Upregulation of SIRT3 transcription is associated with oral squamous cell carcinoma (OSCC) and breast cancer with lymph node involvement, while SIRT3 down-regulation inhibits the growth of OSCC cells and sensitizes them to radiation and chemotherapy.
T83663	Mn(III) Protoporphyrin IX Chloride Manganese(III) Protoporphyrin IX Chloride
	Mn(III) protoporphyrin IX chloride是一种金属卟啉，当浓度为10 µM时，能在鸡胚肝细胞中诱导δ-氨基酮戊二酸合成酶和血红素加氧酶(HO)基因的mRNA表达，这些酶分别催化血红素生物合成和降解的限速步骤。Mn(III) protoporphyrin IX chloride含纳米仿生物已被用于体外纤维蛋白凝块的磁共振成像(MRI)研究。此外，它还被用于Mn(III) protoporphyrin IX-6(7)-甘氨酰-甘氨酰-L-组氨酸甲酯(MnGGH)的合成，MnGGH是一种具有微过氧化物酶活性的金属卟啉衍生物。
T62123	FNDR-20123
	FNDR-20123 是一个安全的、有效的抗疟疾 HDAC 抑制剂，能够作用于疟原虫 HDAC (IC50: 31 nM) 和人类 HDAC (IC50: 3 nM)。FNDR-20123 对恶性疟原虫 (Plasmodium falciparum) 无性期和性血期 (雄性配子体) 都显示出抗疟疾效果，其 IC50 值分别为 41 nM 和 190 nM。FNDR-20123 能够抑制 HDAC1 (IC50: 25 nM)、HDAC2 (IC50: 29 nM)、HDAC3 (IC50: 2 nM)、HDAC6 (IC50: 11 nM)、HDAC8 (IC50: 282 nM)，而且在纳摩尔浓度下可以抑制 III 类 HDAC 亚型。
T68297	Dilmapimod tosylate
	Dilmapimod tosylate is a potent p38 mitogen-activated protein kinase (MAPK) inhibitor. It was investigated for its anti-inflammatory effect in non-head injury trauma patients at risk for developing acute respiratory distress syndrome. IL-1β was identified as a gene regulated by dilmapimod that could influence c-reactive protein levels. Dilmapimod had been in phase III clinical trials by GlaxoSmithKline for the treatment of rheumatoid arthritis, neuropathic pain, coronary artery disease (CAD) and...
T35822	CAY10722
	CAY10722 is an inhibitor of sirtuin 3 (SIRT3), a class III HDAC (71% inhibition at 200 μM). SIRT3 is involved in modulating metabolic homeostasis as a NAD+-dependent protein deacetylase in the mitochondria. SIRT3 functions as either an oncogene or tumor suppressor, depending on cancer cell type. High SIRT3 expression in patient-derived esophageal cancer tissues is associated with shorter survival and, in mice, downregulation leads to a lower tumor load. In contrast, low SIRT3 expression in patie...
T35428	β-Rubromycin
	β-Rubromycin is a bacterial metabolite originally isolated from Streptomyces that has diverse biological activities.1 It inhibits the growth of HMO2, KATO-III, and MCF-7 cells with GI50 values of 0.5, 0.84, and <0.1 μM, respectively. β-rubromycin inhibits HIV-1 reverse transcriptase activity by 39.7% when used at a concentration of 10 μM. It also has antibacterial activity against Gram-positive bacteria. The structure of β-rubromycin was originally described as containing an ortho-quinone group,...
T37127	L-AP4 monohydrate L-AP4 monohydrate
	L-AP4 (L-APB) monohydrate is a potent and specific agonist for the group III mGluRs, with EC50s of 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively[1][2]. L-AP4 (5-30 μg, intrathecal inhection 4-5 days) significantly increases the paw withdrawal threshold in response to application of von Frey filaments in eight nerve-ligated rats in a dose-dependent manner. Intrathecal administration of different doses of L-AP4 is not associated with any evident motor dysfunctio...
T71401	Oxaliplatin-d10
	Oxaliplatin-d10 is intended for use as an internal standard for the quantification of oxaliplatin by GC- or LC-MS. Oxaliplatin is a platinum-containing DNA-crosslinking agent. It induces the formation of DNA inter- and intrastrand crosslinks and DNA-protein adducts, inhibits DNA and RNA synthesis, and induces apoptosis in cancer cells. Oxaliplatin is cytotoxic to cisplatin-sensitive A2780(1A9) and KB-3-1 cells and cisplatin-resistant A2780-E(80) and KB-CP20 cells (IC50s = 0.12, 0.39, 4.7, and 2....
T10372	ARQ 069	Others	Others
	ARQ 069 (3.8-60 μM; for 2 hours) reduces the degree of phosphorylation of FGFR (predominantly FGFR2) in a concentration-dependent manner, without decreasing β-actin. ARQ 069 shows an affinity for FGFR2 of 5.2 μM. ARQ 069 inhibits FGFR phosphorylation in K
T35687	Collismycin A
	Collismycin A is a bacterial metabolite originally isolated from Streptomyces that has diverse biological activities, including antibacterial, antiproliferative, and neuroprotective properties. It is active against a variety of bacteria (MICs = 6.25 and 100 μg/ml) and fungi (MICs = 12.5-100 μg/ml). It inhibits proliferation of A549 lung, HCT116 colon, and HeLa cervical cancer cells (IC50s = 0.3, 0.6, and 0.3 μM, respectively) and NIH373 fibroblasts (IC50 = 56.6 μM) but not MDA-MD-231 breast canc...
T83865	HP661
	HP661是一种针对线粒体复合物I（也称为NADH脱氢酶）的抑制剂，对复合物I具有选择性，以1 µM的浓度抑制其77.6%，而对复合物III抑制率为28.1%，对复合物II和IV则无抑制作用。HP661特异性降低具有高水平氧化磷酸化作用的人类肺癌细胞H460、NCI H441及对trametinib耐药的A549细胞的生存能力（IC50分别为10.6、29.7和15.1 nM），相较于氧化磷酸化水平低的NCI H358人类肺癌细胞（IC50 >10,000 nM）以及非癌性人类胰腺正常上皮细胞（HPNE）和MRC-5人类胎肺成纤维细胞（两者的IC50均>10,000 nM）。当以每天两次，每次30 mg/kg的剂量给药时，HP661在H460小鼠异种移植模型中减少肿瘤体积，并对trametinib引导的肿瘤生长减少产生加成效应。
T36373	Urocortin II (mouse) (trifluoroacetate salt)
	Urocortin II is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin III , frog sauvagine, and piscine urotensin I.1 Mouse urocortin II shares 34 and 42% sequence homology with rat CRF and urocortin . It is expressed in mouse paraventricular, supraoptic, and arcuate nuclei of the hypothalamus, the locus coeruleus, and in motor nuclei of the brainstem and spinal ventral horn. Urocortin II selectively binds to CRF...
T83727	Tat-NTS Peptide TFA Tat-Nuclear Translocation Signal Peptide
	Tat-NTS肽是一种能穿透细胞的肽，由HIV-1 Tat蛋白的转导域与对应于脂联素A1重复III域残基228-237的10个氨基酸肽链接而成，扮演核转运信号（NTS）的角色。它通过阻断脂联素A1与进口素β之间的蛋白质-蛋白质相互作用，阻止脂联素A1在初级鼠海马神经元中的核内转运。Tat-NTS抑制初级鼠海马神经元在葡萄糖-氧剥夺及再灌注诱导的细胞凋亡。在体内，Tat-NTS（10 mg/kg）有效减少了由中脑动脉闭塞（MCAO）引起的缺血-再灌注损伤模型小鼠的梗塞体积和神经元凋亡，并缩短了在Morris水迷宫测试中达到平台的时间。

化合物

H-D-Phe-Pip-Arg-pNA dihydrochloride

Cat.No: T40711

Synonym: S-2238 dihydrochloride,H-D-Phe-Pip-Arg-pNA dihydrochloride

Target: Others

Cat.No: T9011

Synonym: ML 397,ML-397,VU 0155094,VU-0155094

Target: GluR

Cat.No: T27444

Synonym: GSK-932121,GSK932121

H-D-Phe-Pip-Arg-pNA hydrochloride

Cat.No: T39066

Synonym: S-2238 hydrochloride,H-D-Phe-Pip-Arg-pNA hydrochloride

Chlorido[N,N'-disalicylidene-1,2-phenylenediamine]iron(III)

Cat.No: T37851

Cat.No: T35966

Cat.No: T37498

Cat.No: T35821

Mn(III) Protoporphyrin IX Chloride

Cat.No: T83663

Synonym: Manganese(III) Protoporphyrin IX Chloride

Cat.No: T62123

Dilmapimod tosylate

Cat.No: T68297

Cat.No: T35822

Cat.No: T35428

L-AP4 monohydrate

Cat.No: T37127

Synonym: L-AP4 monohydrate

Oxaliplatin-d10

Cat.No: T71401

Cat.No: T10372

Target: Others

Cat.No: T35687

Cat.No: T83865

Urocortin II (mouse) (trifluoroacetate salt)

Cat.No: T36373

Tat-NTS Peptide TFA

Cat.No: T83727

Synonym: Tat-Nuclear Translocation Signal Peptide

Cat. No.	Product Name	Target	Signaling Pathways
TL0007	Bisdemethoxycurcumin 双去甲氧基姜黄素,Curcumin III,Didemethoxycurcumin	Epigenetic Reader Domain; Wnt/beta-catenin	Chromatin/Epigenetic; Cytoskeletal Signaling; Stem Cells
	Bisdemethoxycurcumin (Curcumin III) 是一种具有抗炎及抗氧化作用的姜黄素。
T36227	Beauveriolide III
	Beauveriolide III is a cyclodepsipeptide that has been found inBeauveriaand an inhibitor of lipid droplet formation.1It inhibits lipid droplet formation when used at concentrations of 3 and 10 μM, as well as inhibits cholesterol synthesis (IC50= 0.41 μM), in primary mouse peritoneal macrophages.1,2Beauveriolide III also inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT) activity in mouse macrophage membranes (IC50= 5.5 μM).2Beauveriolide III (25 and 50 mg/kg) reduces the size of aortic ...
T83471	10-Deacetyl-13-oxobaccatin III
	10-Deacetyl-13-oxobaccatin III是一款从Taxus sumatrana分离的紫杉烷。在30 μg/mL的浓度下，对A498、NCI-H226、A549、PC-3细胞系展现细胞毒性作用，其抑制率分别达到29.7%、49.2%、43.9%、65.3%。
T83435	19-Hydroxy-10-deacetylbaccatin III
	19-Hydroxy-10-deacetylbaccatin III (compound 13) 是紫杉烷类化合物，显示出潜在的抗肿瘤作用。在 A498 和 NCI-H226 细胞系中，此化合物表现出轻微的细胞毒性效应。研究指出，当浓度为 30 μg/mL 时，19-Hydroxy-10-deacetylbaccatin III 对 A498 细胞和 NCI-H226 细胞的抑制率为 16.6% 和 32%。
T75540	Ipomoeassin F
	Ipomoeassin F 是一种高效且具有选择性的内质网(ER)蛋白转位抑制剂，它通过作用于ER膜上的Sec61复合物（Sec61α）的成孔亚基来实现其功能。此化合物能特异性抑制SARS-CoV-2蛋白在ER膜上的转位，同时阻碍分泌蛋白和I型跨膜蛋白（TMP）的ER转运，但对III型TMP的转运不产生影响。

天然产物

Bisdemethoxycurcumin

Cat.No: TL0007

Synonym: 双去甲氧基姜黄素,Curcumin III,Didemethoxycurcumin

Target: Epigenetic Reader Domain, Wnt/beta-catenin

Beauveriolide III

Cat.No: T36227

10-Deacetyl-13-oxobaccatin III

Cat.No: T83471

19-Hydroxy-10-deacetylbaccatin III

Cat.No: T83435

Cat.No: T75540

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