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24

抑制剂 & 化合物

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天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T12927	SK1-IN-1	S1P Receptor	GPCR/G Protein
	SK1-IN-1 is a potent inhibitor of sphingosine kinase 1 (SPHK1)(IC50 of 58 nM).
T4612	NS309	EGFR; Potassium Channel; HER	Angiogenesis; JAK/STAT signaling; Membrane transporter/Ion channel; Tyrosine Kinase/Adaptors
	NS309 是选择性钙依赖性钾离子通道 SK/IK 的激活剂，在 BK 通道上没有激活作用。
T28788	SK-216 SK216.Plasminogen activator inhibitor-1 (PAI-1) inhibitor
	SK-216 is a specific PAI-1 inhibitor. SK-216 reduced the extent of angiogenesis in the tumors and inhibited VEGF-induced migration and tube formation by human umbilical vein endothelial cells in vitro. SK-216 reduced the degree of bleomycin-induced pulmon
T74662	UBA5-IN-1
	UBA5-IN-1 (compound 8.5) 是 UBA5的选择性抑制剂，IC50值为 4.0 μM。UBA5-IN-1 抑制高表达 UBA5 的 Sk-Luci6 癌细胞的增殖。
T74558	SK-575-NEG
	SK-575-NEG（化合物28）是SK-575的甲基化对应物，通过对SK-575中的哌啶-2,6-二酮氨基进行甲基化合成而得，用作对照化合物。SK-575-NEG强效结合PARP1，IC50值仅为2.64 nM。在1 μM浓度下，SK-575-NEG对MDA-MB-436和Capan-1细胞中PARP1的降解完全无效。
T79429	Tubulin polymerization-IN-50
	Tubulin polymerization-IN-50（compound 7n）是一种Tubulin polymerization抑制剂，其在SK-Mel-28细胞中的IC50值为5.05 μM，能够诱导(cell cycle)阻滞在G2/M期。
T74781	UT-11
	UT-11是一种有效且具有脑渗透性的mPGES-1抑制剂，能够降低人类(SK-N-AS)和小鼠(BV2)细胞内PGE2的生成，其IC50s分别是0.10 μM和2.00 μM。
T74491	Antitumor agent-61
	Antitumor agent-61 (Compound 9b)，Irinotecan (Ir)的衍生物，展现出对多种肿瘤细胞（包括SK-OV-3、SK-OV-3/CDDP、U2OS、MCF-7、A549与MG-63）具有显著的抑制效果，其IC50值分别为0.92、1.39、1.75、2.20、3.05和3.23 μM。该化合物主要通过线粒体途径引发SK-OV-3细胞的凋亡。
T80170	Tamapin	Potassium Channel	Membrane transporter/Ion channel
	Tamapin为靶向小电导Ca(2+)激活的K(+) (SK)通道的毒液肽，尤以钾通道SK2为选择性阻断剂。该化合物能够抑制海马锥体神经元SK通道介导的电流，来源于印度红蝎(Mesobuthus tamulus)。
T80924	Tubulin polymerization-IN-51
	Tubulin polymerization-IN-51（compound 7u）是抑制SK-Mel-28细胞微管蛋白聚合的化合物，IC50介于2.55至17.89μM。该化合物适用于癌症研究。
T70789	VPC03090
	VPC03090 is a Sphingosine-1-Phosphate Receptor Inhibitor. VPC03090 is an analog of FTY-720, acts as antagonist for S1PR1 and S1PR3. VPC03090-P, converted from VPC03090 through the phosphorylation by SK-2, causes a reduction in tumor growth in mice with mammary cancer, and its oral bioavailability is determined to be 30 hours.
T80171	Tamapin TFA	Potassium Channel	Membrane transporter/Ion channel
	Tamapin TFA为靶向小电导Ca(2+)激活的K(+) (SK)通道的毒液肽，特异性抑制SK2（钾通道）并阻断海马锥体神经元中SK通道介导的电流。该化合物可从印度红蝎(Mesobuthus tamulus)毒液中提取。
T36427	PACAP (6-27) (human, chicken, mouse, ovine, porcine, rat) (trifluoroacetate salt)	PACAP	GPCR/G Protein
	Pituitary adenylate cyclase-activating peptide (PACAP) (6-27) is a PACAP receptor antagonist with IC50 values of 1,500, 600, and 300 nM, respectively, for rat PAC1, rat VPAC1, and human VPAC2 recombinant receptors expressed in CHO cells. It binds to PACAP receptors on SH-SY5Y and SK-N-MC human neuroblastoma and T47D human breast cancer cells (IC50s = 24.5, 106, and 105 nM, respectively) and inhibits cAMP accumulation induced by PACAP (1-38) (Kis = 457, 102, and 283 nM, respectively, in SH-SY5Y, ...
T35977	6α-hydroxy Cholesterol 6α-hydroxy Cholesterol,6α-OHC
	6α-hydroxy Cholesterol is an oxysterol that increases superoxide anion production in SK-N-BE cells when used at concentrations of 50 and 100 μM.[1]
T76184	Scyllatoxin
	Scyllatoxin (Leiurotoxin I) 为一种从(Leiurus quinquestriatus hebraeus)毒蝎毒液中分离的肽毒素，作为小电导钙激活型钾通道KCa(SK)的阻断剂，有能力增强体内去甲肾上腺素(NE)与肾上腺素(Epi)的释放。
T36468	ARN14988
	ARN14988 is a potent inhibitor of acid ceramidase (IC50 = 12.8 nM for the human enzyme). It inhibits acid ceramidase activity and increases levels of C16 dihydro ceramide and C16 ceramide in A375, G361, M14, MeWo, MNT-1, and SK-MEL-28 melanoma cells. ARN14988 also reduces growth of A375 and G361 melanoma cells (EC50s = 41.8 and 67.7 μM, respectively).
T60603	BRD9500
	BRD9500 是一种具有口服活性的磷酸二酯酶 3 (PDE3) 抑制剂，对PDE3A 和PDE3B 的IC50分别为 10 和 27 nM。BRD9500 在黑色素瘤细胞系 SK-MEL-3 癌症异种移植模型中具有活性。
T37564	C4 Ceramide (d18:1/4:0) C4 Ceramide (d18:1/4:0),Cer(d18:1/4:0)
	C4 Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. [1] [2] [3] It inhibits IL-4 production by 16% in EL4 T cells stimulated with phorbol 12-myristate 13-acetate when used at a concentration of 10 μM. [1] C4 Ceramide is cytotoxic to SK-BR-3 and MCF-7/Adr breast cancer cells (IC50s = 15.9 and 19.9 μM, respectively). [2] C4 Ceramide also increases maturation and stability of cystic fibrosis transmembrane conductance regulator (CFTR) proteins bearing...
T35552	Ganglioside GD3 Mixture (sodium salt)
	Ganglioside GD3 is synthesized by the addition of two sialic acid residues to lactosylceramide and can serve as a precursor to the formation of more complex gangliosides by the action of glycosyl- and sialyltransferases. It induces apoptosis in HuT-78 cutaneous T cell lymphoma cells in a concentration-dependent manner and disrupts the mitochondrial membrane potential when used at a concentration of 200 μM. Expression of ganglioside GD3 in GD3-negative SK-MEL-28-N1 malignant melanoma cells increa...
T36539	Nocardamine
	Nocardamine is a ferrioxamine siderophore that has been found inStreptomycesand has diverse biological activities.1,2,3,4It chelates iron in a chrome azurol S assay (IC50= 9.9 μM).1Nocardamine inhibitsM. smegmatisandM. bovisbiofilm formation (MIC = 10 μM for both), an effect that can be reversed by iron.2It is cytotoxic to T47D, SK-MEL-5, SK-MEL-28, and RPMI-7951 cancer cells (IC50s = 6, 18, 12, and 14 μM, respectively).3Nocardamine also induces morphological changes in BM-N4 insect cells.4 1.Lo...
T35762	MC1742
	MC1742 is an inhibitor of class I histone deacetylases (HDACs; IC50s = 0.1, 0.11, 0.02, and 0.61 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 7 and 40 nM for HDAC6 and HDAC10, respectively).1 It is selective for class I and class IIb over class IIa HDACs (IC50s = >50 μM for HDAC4, -5, -7, and -9). MC1742 reduces proliferation of HOS, MG-63, RD, A204, SK-ES-1, and A673 sarcoma cancer stem cells (CSCs). It increases levels of acetylated histone H3 and acetylated tubulin...
T83894	4A7C-301-Nurr1 Agonist 4A7C-301-Nuclear Receptor-Related 1
	4A7C-301-Nurr1激动剂是一种核受体相关1（Nurr1）的激动剂。它通过与Nurr1配体结合域（LBD；IC50 = 48.22 nM）结合，增加了在使用SK-N-BE(2)C人神经母细胞瘤细胞进行的报告基因测定中Nurr1-LBD和全长Nurr1的转录活性（EC50s = 6.53 和 50-70 µM，分别）。每天5 mg/kg的4A7C-301-Nurr1激动剂能减少在经MPTP神经毒素或α-突触核蛋白过表达诱导的帕金森病鼠模型中纹状体和黑质compacta部分多巴胺能细胞的死亡，并减少运动和嗅觉缺陷，而不诱发类似运动障碍的行为。
T35683	2-deoxy-D-Glucose-13C6 2-deoxy-D-Glucose-13C6
	2-deoxy-D-Glucose-13C6is intended for use as an internal standard for the quantification of 2-deoxy-D-glucose by GC- or LC-MS. 2-deoxy-D-Glucose is a glucose antimetabolite and an inhibitor of glycolysis.1,2It inhibits hexokinase, the enzyme that converts glucose to glucose-6-phosphate, as well as phosphoglucose isomerase, the enzyme that converts glucose-6-phosphate to fructose-6-phosphate.32-deoxy-D-Glucose (16 mM) induces apoptosis in SK-BR-3 cells, as well as inhibits the growth of 143B oste...
T83765	Dendrogenin A DDA
	Dendrogenin A (DDA) 作为一种选择性肝X受体(LXR)调节剂(SLiM)、胆固醇环氧水解酶(ChEH; Ki = 120 nM)的抑制剂及胆固醇的活性代谢产物，通过DDA合成酶将5,6α-环氧胆固醇与组胺结合形成。DDA在非癌性人乳腺上皮细胞和上皮黑色素细胞中存在，但在多种乳腺癌细胞或黑色素瘤细胞中未发现，且在分离的人乳腺肿瘤组织中仅以低水平存在。它抑制22(R)-羟基胆固醇诱导的LXRβ和LXRα激活(分别以IC50 = 76和362 nM)，但也是LXR的部分激动剂，在B16/F10小鼠黑色素瘤细胞中增加Nur77、NOR-1、LC3-I和LC3-II的蛋白水平。DDA选择性调节LXRα和LXRβ，而非孕烯X受体(PXR)、芳香烃受体(AhR)、维生素D受体(VDR)、维甲酸X受体γ(RXRγ)、维甲酸受体α(RARα)、过氧化物酶体增殖物激活受体α(PPARα)、PPARγ、糖皮质激素受体、雄激素受体、雌激素受体α(ERα)及ERβ在2.5 µM下。此外，DDA在2.5和5 µM的浓度下增加B16/F10和SK-MEL-28癌细胞中LC3-II的蛋白水平，并在2...

化合物

Cat.No: T12927

Target: S1P Receptor

Cat.No: T4612

Target: EGFR, Potassium Channel, HER

Cat.No: T28788

Synonym: SK216.Plasminogen activator inhibitor-1 (PAI-1) inhibitor

Cat.No: T74662

Cat.No: T74558

Tubulin polymerization-IN-50

Cat.No: T79429

Cat.No: T74781

Antitumor agent-61

Cat.No: T74491

Cat.No: T80170

Target: Potassium Channel

Tubulin polymerization-IN-51

Cat.No: T80924

Cat.No: T70789

Cat.No: T80171

Target: Potassium Channel

PACAP (6-27) (human, chicken, mouse, ovine, porcine, rat) (trifluoroacetate salt)

Cat.No: T36427

Target: PACAP

6α-hydroxy Cholesterol

Cat.No: T35977

Synonym: 6α-hydroxy Cholesterol,6α-OHC

Cat.No: T76184

Cat.No: T36468

Cat.No: T60603

C4 Ceramide (d18:1/4:0)

Cat.No: T37564

Synonym: C4 Ceramide (d18:1/4:0),Cer(d18:1/4:0)

Ganglioside GD3 Mixture (sodium salt)

Cat.No: T35552

Cat.No: T36539

Cat.No: T35762

4A7C-301-Nurr1 Agonist

Cat.No: T83894

Synonym: 4A7C-301-Nuclear Receptor-Related 1

2-deoxy-D-Glucose-13C6

Cat.No: T35683

Synonym: 2-deoxy-D-Glucose-13C6

Cat.No: T83765

Synonym: DDA

Cat. No.	Product Name	Target	Signaling Pathways
T3S1589	Notoginsenoside Fa	Others	Others
	Notoginsenoside Fa 是一种原人参二醇型皂苷，从P. notoginseng 提取出来得到，有激活和恢复退化脑功能的潜能。
T6S1487	Ginsenoside Rg5 人参皂苷Rg5,人参皂甙 Rg5	NF-κB; COX; IGF-1R	Immunology/Inflammation; Neuroscience; NF-κB; Tyrosine Kinase/Adaptors
	Ginsenoside Rg5 是红参的主要成分，可阻断IGF-1与其受体的结合，IC50约为90 nM。它还通过抑制NF-κB p65的 DNA 结合活性来抑制COX-2的 mRNA 表达。它可促进血管生成和改善高血压，具有抗炎和治疗阿尔茨海默病的潜力。
TN4373	Kaempferol tetraacetate	Antifection	Microbiology/Virology
	Kaempferol tetraacetate is a potent antiplatelet agent. It exhibits significant cytotoxicity in vitro against three human cell lines HL-60, U937 and SK-MEL-1.
TN6014	Norcepharadione B 鱼腥草
	Norcepharadione B shows good inhibitory activity against the replication of HSV-1, it also shows antimalarial activity with EC50 values of 7.5mug/ml. Norcepharadione B exhibits significant cytotoxicity against five human tumor cell lines (A-549, SK-OV-3,
T36749	Herboxidiene
	Herboxidiene is a polyketide originally isolated from S. chromofuscus that has diverse biological activities.[1],[2,][3],[4],[5] It inhibits growth of HeLa S3, SK-MEL-2, PC3, A549, and EBC-1 cells with GI50 values ranging from 7.4 to 62 nM.3 Herboxidiene is cytostatic against human umbilical vein endothelial cells (HUVECs; (IC50 = 26 nM)) and inhibits VEGF-induced invasion and tube formation of serum-starved HUVECs in a concentration-dependent manner, indicating antiangiogenic activity.[4] Herbo...
T37452	Stephacidin B
	Stephacidin B is a fungal metabolite that has been found inA. ochraceus.1Dimeric stephacidin B is rapidly converted to a monomer, avrainvillamide ,in vitro.2Stephacidin B is cytotoxic to a variety of cancer cells, including testosterone-independent PC3 and -sensitive LNCaP prostate cancer cells (IC50s = 0.37 and 0.06 μM, respectively) and estradiol-independent SK-BR-3 and -sensitive MCF-7 breast cancer cells (IC50s = 0.32 and 0.27 μM, respectively).1It induces apoptosis in HepG2 and Huh7 hepatoc...
T36954	Nemorosone
	Nemorosone is a polycyclic polyprenylated acylphloroglucinol (PPAP) originally isolated from C. rosea that has antiproliferative properties.1 Nemorosone inhibits growth of NB69, Kelly, SK-N-AS, and LAN-1 neuroblastoma cells (IC50s = 3.1-6.3 μM), including several drug-resistant clones, but not MRC-5 human embryonic fibroblasts (IC50 = >40 μM).2 It increases DNA fragmentation in LAN-1 cells in a dose-dependent manner, and decreases N-Myc protein levels and phosphorylation of ERK1/2 by MEK1/2. Nem...

天然产物

Notoginsenoside Fa

Cat.No: T3S1589

Target: Others

Ginsenoside Rg5

Cat.No: T6S1487

Synonym: 人参皂苷Rg5,人参皂甙 Rg5

Target: NF-κB, COX, IGF-1R

Kaempferol tetraacetate

Cat.No: TN4373

Target: Antifection

Norcepharadione B

Cat.No: TN6014

Synonym: 鱼腥草

Cat.No: T36749

Cat.No: T37452

Cat.No: T36954

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