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23

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T1290	Oxiconazole nitrate 硝酸奥昔康唑,Ro 13-8996	Others; Antibiotic; Antifection; Antifungal	Microbiology/Virology; Others
	Oxiconazole nitrate (Ro 13-8996) 是广谱抗真菌药物，抑制T. tonsurans 和T.rubrum 的生长，MIC90值分别为 0.25 和 0.5 μg/mL。
T9317	TAK-041 NBI-1065846	GPR	Endocrinology/Hormones; GPCR/G Protein
	TAK-041 (NBI-1065846) 是一种选择性 GPR139激动剂，EC50为 22 nM，有用于精神分裂症阴性症状的研究潜力。
T8825	Capmatinib 2HCl.H2O INCB28060 2HCl.H2O,INC-280 2HCl.H2O,NVP-INC280 2HCl.H2O	c-Met/HGFR	Tyrosine Kinase/Adaptors
	Capmatinib 2HCl.H2O (NVP-INC280 2HCl.H2O) 是一种具有潜在抗肿瘤活性的原癌基因 c-Met (HGFR) 的口服生物可利用抑制剂。
T8416	Capmatinib xHCl INCB28060,Capmatinib hydrochloride(free base),INC280	c-Met/HGFR	Tyrosine Kinase/Adaptors
	Capmatinib xHCl (INCB28060) 是一种有效的、口服活性的、选择性的和 ATP 竞争性 c-Met 激酶抑制剂，有效地阻断体外激酶活性 (IC50 = 0.13 nM) 以及在细胞中的组成型或 HGF 刺激活性(IC50 值范围从 0.3 到1.1纳米)。
T1963	Capmatinib NVP-INC280,INC-280,卡马替尼,INCB28060	Apoptosis; c-Met/HGFR	Apoptosis; Tyrosine Kinase/Adaptors
	Capmatinib (INCB28060) 是一种具有口服活性的，选择性的，ATP 竞争性的c-Met 激酶抑制剂，IC50值为0.13 nM。它有效抑制 c-Met 依赖性肿瘤细胞的增殖和迁移，可诱导细胞凋亡，有抗肿瘤活性。
T4260	Capmatinib 2HCl INC-280 2HCl,INCB28060盐酸盐,INCB28060 2HCl	c-Met/HGFR	Tyrosine Kinase/Adaptors
	Capmatinib 2HCl (INC-280 2HCl) 是一种新型的 ATP 竞争性 c-MET 激酶抑制剂，IC50 为 0.13 nM。它具有皮摩尔酶效，对 c-MET 具有高度特异性，选择性超过 10, 000 倍一大组人类激酶。该抑制剂在 c-MET 依赖性肿瘤细胞系中有效阻断 c-MET 磷酸化和其关键下游效应子的激活。因此，它在体外有效抑制 c-MET 依赖性肿瘤细胞增殖和迁移，并有效诱导细胞凋亡。
T68166L	Traxanox TFA Traxanox TFA(58712-69-9 Free base)	Others	Others
	Traxanox TFA 是一种可口服的利尿剂。Traxanox TFA 在体外增强小鼠腹膜巨噬细胞或大鼠腹膜多形核白细胞对酵母颗粒的吞噬作用。Traxanox TFA 对抑制BALB/c小鼠抗体产生的恢复作用。
T68166	Traxanox	Others	Others
	Traxanox 是一种可口服的利尿剂。Traxanox 在体外增强小鼠腹膜巨噬细胞或大鼠腹膜多形核白细胞对酵母颗粒的吞噬作用。Traxanox 对抑制BALB/c小鼠抗体产生的恢复作用。
T78000	OVA Peptide (323-339)
	OVA Peptide (323-339) 是卵清蛋白(OVA)的T和B细胞表位，对BALB/c小鼠的瞬时超敏反应生成与发展至关重要。
T63945	Antitubercular agent-19
	Antitubercular agent-19 是一种抗结核剂。Antitubercular agent-19 对 MTB H37Rv 和 MDR-MTB 表现出良好的抗结核效果 (MIC＜0.016 μg/ml)。Antitubercular agent-19 在 BALB/c 小鼠中表现出较低的细胞毒性和相对较高的急性致死毒性。
T64045	Antitubercular agent-20
	Antitubercular agent-20 是口服具有活力的抗结核剂。Antitubercular agent-20 对 MTB H37Rv 和 MDR-MTB 表现出良好的抗结核效果，其 MIC＜0.016 μg/ml。在 BALB/c 小鼠中，Antitubercular agent-20 表现出较低的细胞毒性和较好的耐受性。
T61532	Tubulin polymerization-IN-6
	Tubulin polymerization-IN-6 (compound 5f) is a potent inhibitor of tubulin polymerization, with an IC50 of 1.09 μM. It not only inhibits cell migration and tube formation but also has anti-angiogenic properties. Additionally, Tubulin polymerization-IN-6 has been found to effectively hinder tumor growth in HT29 xenograft Balb/c nude mice [1].
TP1339	OVA Peptide 323-339
	OVA Peptide (323-339) represents a T and B cell epitope of Ovalbumin (Ova), which play an important role in the development and development of immediate hypersensitivity in BALB/c mice.
T34278	Redaporfin F 2BMet,F2BMet,F-2BMet,LUZ11,LUZ 11,LUZ-11
	Redaporfin, also known as F-2BMet or LUZ-11, is a photosensitizer for Photodynamic Therapy (PDT) of cancer. Redaporfin showed a high efficacy in the treatment of male BALB/c mice with subcutaneously implanted colon (CT26) tumours. Vascular-PDT with 1.5 mg
T37423	Reveromycin D
	Reveromycin D is a bacterial metabolite originally isolated from Streptomyces. It inhibits EGF-induced mitogenic activity in Balb/MK cells and has pH-dependent antifungal activity against C. albicans (MICs = 2 and >500 μg/ml at pH 3 and 7.4, respectively). Reveromycin D also inhibits proliferation of KB and K562 cells (IC50s = 1.6 and 1.3 μg/ml, respectively).
T38044	Reveromycin B
	Reveromycin B is a spiroketal bacterial metabolite originally isolated from Streptomyces. It inhibits EGF-induced mitogenic activity in Balb/MK cells (IC50 = 6 μg/ml) and exhibits pH-dependent antifungal activity against C. albicans (MICs = 15.6 and >500 μg/ml at pH 3.0 and 7.4, respectively). Unlike reveromycin A and reveromycin C , reveromycin B does not inhibit proliferation of KB and K562 cells.
T68875	Xylocydine
	Xylocydine is a novel Cdk inhibitor, which is an effective inducer of apoptosis in hepatocellular carcinoma cells in vitro and in vivo. Xylocydine also strongly inhibits the activity of Cdk7 and Cdk9, in vitro as well as in cell cultures, that is temporally associated with apoptotic cell death in xylocydine-induced HCC cells. Xylocydine can effectively suppress the growth of HCC xenografts in Balb/C-nude mice by preferentially inducing apoptosis in the xenografts, whereas the drug did not cause...
TP1935	RAGE antagonist peptide
	Receptor for advanced glycation end products (RAGE) antagonist. Blocks S100P, S100A4 and HMGB-1 mediated RAGE activation in vitro and in vivo. Inhibits growth and metastasis of rat glioma tumors. Reduces cell growth and RAGE-mediated NF-κB activity in hum
T71382	KRC-108
	KRC-108 is a multiple kinase inhibitor. KRC-108 is a potent inhibitor of Ron, Flt3 and TrkA as well as c-Met. KRC-108 inhibited oncogenic c-Met M1250T and Y1230D more strongly than wild type c-Met. The anti-proliferative activity of KRC-108 was measured by performing a cytotoxicity assay on a panel of cancer cell lines. The GI(50) values (i.e., 50% inhibition of cell growth) for KRC-108 ranged from 0.01 to 4.22 μM for these cancer cell lines. KRC-108 was also effective for the inhibition of tumo...
T69831	RPR-200765A Mesylayte
	RPR-200765A is a potent and selective inhibitor of p38 MAP kinase (IC50 = 50 nM). It inhibits LPS-stimulated TNFalpha release both in vitro, from human monocytes (EC50 = 110 nM), and in vivo in Balb/c mice (ED50 = 6 mg/kg). At oral doses between 10 and 30 mg/kg/day it reduces the incidence and progression in the rat streptococcal cell wall (SCW) arthritis model when administered in either prophylactic or therapeutic dosing regimens. The compound, which is a mesylate salt and exists as a stable m...
T35491	3,5-dimethyl PIT-1
	PtdIns-(3,4,5)-P3 (PIP3) serves as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains such as phosphatidylinositol 3-kinase (PI3K) or PTEN. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking and initiates an intricate signaling cascade that has been implicated in cancer. 3,5-dimethyl PIT-1 is a dimethyl analog of PIT-1, the selective inhibitor of PIP3/Akt PH domain binding, that is designed for more favorab...
T38269	Purfalcamine
	Purfalcamine is an orally active, selective Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC50 of 17 nM and an EC50 of 230 nM. Purfalcamine has antimalarial activity and causes malaria parasites developmental arrest at the schizont stage[1][2]. Purfalcamine has low activity against Toxoplasma gondii calcium-dependent protein kinase 3 (TgCDPK3)[1]. Purfalcamine (225, 450 nM) has no effect on the parasitemia in the first 32 hours. After about 40 hours, paras...
T36486	Benpyrine
	Benpyrine is a highly specific and orally active TNF-α inhibitor with a KD value of 82.1 μM. Benpyrine tightly binds to TNF-α and blocks its interaction with TNFR1, with an IC50 value of 0.109 μM. Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research[1]. Benpyrine (5-20 μM; 14 hours; RAW264.7 cells) pretreatment results in a dose-dependent decrease in the phosphorylation of IκBα in RAW264.7 cells (stimulated with 10 ng/mL TNF-α or 1 μg/mL LPS). Benpyrine abo...

化合物

Oxiconazole nitrate

Cat.No: T1290

Synonym: 硝酸奥昔康唑,Ro 13-8996

Target: Others, Antibiotic, Antifection, Antifungal

Cat.No: T9317

Synonym: NBI-1065846

Target: GPR

Capmatinib 2HCl.H2O

Cat.No: T8825

Synonym: INCB28060 2HCl.H2O,INC-280 2HCl.H2O,NVP-INC280 2HCl.H2O

Target: c-Met/HGFR

Capmatinib xHCl

Cat.No: T8416

Synonym: INCB28060,Capmatinib hydrochloride(free base),INC280

Target: c-Met/HGFR

Cat.No: T1963

Synonym: NVP-INC280,INC-280,卡马替尼,INCB28060

Target: Apoptosis, c-Met/HGFR

Capmatinib 2HCl

Cat.No: T4260

Synonym: INC-280 2HCl,INCB28060盐酸盐,INCB28060 2HCl

Target: c-Met/HGFR

Cat.No: T68166L

Synonym: Traxanox TFA(58712-69-9 Free base)

Target: Others

Cat.No: T68166

Target: Others

OVA Peptide (323-339)

Cat.No: T78000

Antitubercular agent-19

Cat.No: T63945

Antitubercular agent-20

Cat.No: T64045

Tubulin polymerization-IN-6

Cat.No: T61532

OVA Peptide 323-339

Cat.No: TP1339

Cat.No: T34278

Synonym: F 2BMet,F2BMet,F-2BMet,LUZ11,LUZ 11,LUZ-11

Cat.No: T37423

Cat.No: T38044

Cat.No: T68875

RAGE antagonist peptide

Cat.No: TP1935

Cat.No: T71382

RPR-200765A Mesylayte

Cat.No: T69831

3,5-dimethyl PIT-1

Cat.No: T35491

Cat.No: T38269

Cat.No: T36486

Cat. No.	Product Name	Target	Signaling Pathways
TN4470	Lyoniside	Antifection	Microbiology/Virology
	Lyoniside and saracoside are cytotoxic to promastigotes and intracellular amastigotes, they demonstrate strong anti-leishmanial efficacies in BALB/c mice model of leishmaniasis, suggests that these two compounds potential anti-leishmanial candidates. The
T37008	Reveromycin A
	Reveromycin A is the major component of a complex of spiroketal antibiotics isolated from Streptomyces sp. It inhibits the mitogenic activity of epidermal growth factor in Balb/MK cells (IC50 = 0.7 μg/ml), displays antiproliferative activity against human KB and K562 tumor cell lines (IC50s = 1.9 and 1.6 μg/ml, respectively), and demonstrates antifungal activity against C. albicans (MIC = 2 μg/ml at pH 3). Reveromycin A also has been shown to inhibit bone resorption by inducing apoptosis in oste...

天然产物

Cat.No: TN4470

Target: Antifection

Cat.No: T37008

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