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18

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T9973	FAK-IN-7	FAK	Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
	FAK-IN-7 有潜在的抗增殖活性，是一种 FAK 抑制剂。
T27371	FR-167356 FR167356,FR 167356	ATPase	Membrane transporter/Ion channel
	FR-167356 是 a3 异构体液泡型 H+-ATPase 的特异性抑制剂，对破骨细胞质膜、肾刷状缘膜和巨噬细胞微粒体的 IC50 分别为 170 nM、370 nM 和 220 nM。 FR-167356 减少 B16-F10 细胞的骨转移。
T36460	CAY10736 CAY10736
	CAY10736 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.827-9.89 μM). CAY10736 inhibits migration and epithelial-to-mesenchymal transition (EMT) of A375 and B16/F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16/F10 cells (IC50s = 2.4 and 1.59 μM, respectively) and increases the production of reactive oxygen species (ROS) in these cells in a ...
T36497	CAY10735 CAY10735
	CAY10735 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.674-11.56 μM). CAY10735 inhibits migration of and the epithelial-to-mesenchymal transition (EMT) in A375 and B16/F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16/F10 cells (IC50s = 3.04 and 1.24 μM, respectively) and increases production of reactive oxygen species (ROS) in these cells ...
T37586	DMHAPC-Chol
	DMHAPC-Chol is a cationic cholesterol. Liposomes containing DMHAPC-chol have been used for DNA plasmid delivery in vitro and in vivo in a B16-F10 mouse xenograft model. Liposomes containing DMHAPC-chol are cytotoxic to B16-F10 cells when used at lipid concentrations greater than 20 μM. DMHAPC-Chol, as part of a lipoplex with DOPE , has also been used to deliver DNA into mouse lung via intratracheal injection, resulting in a heterogeneous distribution in the bronchi and bronchioles, and to delive...
T79528	SWS1	PD-1/PD-L1	Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation
	SWS1为d-(+)-生物素缀合的PD-L1抑制剂(IC50: 1.8 nM)，显示出抗癌潜力。该化合物能提高肿瘤浸润淋巴细胞数量，并在B16-F10小鼠模型中展现抗肿瘤效果(TGI=66.1%)。
T78958	Anticancer agent 106	Apoptosis	Apoptosis
	Anticanceragent 106（化合物 10ic）是一款能诱导B16-F10黑色素瘤细胞发生凋亡(apoptosis)的抗癌剂。此外，Anticanceragent 106在抑制肺转移性黑色素瘤小鼠模型的转移性结节方面也显示出有效性。该化合物主要应用于癌症研究，特别是针对肺转移性黑色素瘤。
T79705	LP23	PD-1/PD-L1	Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation
	LP23为非芳基甲胺类PD-1/PD-L1抑制剂(IC50：16.7 nM)，展现出抗肿瘤效果。能恢复HepG2/Jurkat T细胞的免疫功能并促进HepG2细胞凋亡。在B16-F10肿瘤模型中，LP23表现出体内活性，在剂量为30 mg/kg时TGI达到88.6%。
T83886	icFSP1 TFA
	icFSP1是一种抑制剂，针对的是铁死亡抑制蛋白1（FSP1）。在2.5 µM的浓度下使用时，能够引发FSP1在细胞中的凝聚和相分离，但在无细胞测试中并不抑制FSP1的酶活性（IC50 = > 30 µM）。icFSP1以浓度依赖的方式诱导HT-1080纤维肉瘤细胞的铁死亡。在体内，icFSP1（50 mg/kg）通过使用人类过表达FSP1，Gpx4-/-Fsp1-/-的B16/F10细胞，在B16/F10鼠黑色素瘤模型中减少肿瘤体积和重量。
T79711	Antitumor photosensitizer-4	Apoptosis	Apoptosis
	Antitumor photosensitizer-4 (compound 10b) 是靶向ABCG2酪氨酸激酶抑制剂(TKI)的有效代表，由达沙替尼与伊马替尼构成的光敏剂(PS)。该化合物能够诱发细胞凋亡(apoptosis)及ROS生成，在HepG2和B16-F10细胞上展现出显著的光毒性作用。
T36138	BMP-22
	BMP-22 is an inhibitor of autotaxin (IC50 = 170 nM). It is selective for autotaxin over the phosphodiesterases NPP6 and NPP7 at 10 μM. BMP-22 (0.1-1,000 nM) inhibits autotaxin-mediated production of lysophosphatidic acid (LPA) from lysophosphatidylcholine in vitro in a concentration-dependent manner. It inhibits LPC-dependent MM1 cell invasion of a human umbilical vein endothelial cell (HUVEC) monolayer. BMP-22 (0.5 mg/kg per day) decreases the number of lung metastatic foci in a B16/F10 syngene...
T78855	Anticancer agent 157	NO Synthase	Immunology/Inflammation
	Anticanceragent 157（compound 15）是一种NO抑制剂，具有抗炎和抗癌特性，IC50值为0.62 μg/mL。它能够与iNOS和caspase 8结合，进而导致核断裂和染色质浓缩，从而诱导细胞凋亡。此外，Anticanceragent 157在不同癌细胞系中展现出显著的抑制活性，对HT29结肠癌细胞的IC50为2.45 μg/mL，对Hep-G2肝癌细胞的IC50为3.25 μg/mL，以及对B16-F10鼠黑色素瘤细胞的IC50为3.84 μg/mL。
T38320	93-O17S 93-O17S
	93-O17S is a chalcogen-containing cationic lipidoid.1It has been used in the synthesis of lipid nanoparticles (LPNs) for the delivery of Cre recombinase and ribonucleoproteins for genome editing in mice. LPNs containing 93-O17S have been used for the intratumoral delivery of cGAMP to enhance cross-presentation of tumor antigens and stimulation of interferon genes (STING) activation in a B16/F10 murine melanoma model.2 1.Li, Y., Yang, T., Yu, Y., et al.Combinatorial library of chalcogen-containin...
T36181	Quinaldopeptin
	Quinaldopeptin is a quinomycin antibiotic. It is active against a variety of bacteria, including S. pyogenes, S. aureus, C. perfringens, S. faecalis, E. coli, and K. pneumoniae (MICs = 0.2, 0.4, 0.8, 1.6, 3.1 and 6.3 μg/ml, respectively). It is cytotoxic to B16/F10 and Moser cells (IC50s = 0.0008 and 0.04 μg/ml, respectively) and increases survival in a P388 leukemia mouse model. Quinaldopeptin is a bis-intercalator depsipeptide (NPBID) that binds to and intercalates into DNA (Kd = 32 nM).
T36645	CAY10763 CAY10763
	CAY10763 is a dual inhibitor of indolamine 2,3-dioxygenase 1 (IDO1; IC50= 46 nM) and STAT3 activation.1It binds to STAT3 (Kd= 530 nM) and selectively reduces the levels of STAT3 phosphorylated at the tyrosine in position 705 (STAT3Y705) over phosphorylated STAT3S727, STAT1, and STAT5 in SKOV3 cells when used at a concentration of 500 nM. It also inhibits STAT3 nuclear translocation in SKOV3 cells. CAY10763 is cytotoxic to HCT116, SKOV3, A549, and HepG2 cancer cells (IC50s = 37, 28, 33, and 12 nM...
T37722	Diprovocim-1
	Diprovocim-1 is an agonist of the toll-like receptor 1/2 heterodimer.1It induces TNF-α release in THP-1 cells (EC50= 110 pM), an effect that can be inhibited by anti-TLR1 or anti-TLR2 antibodies. Diprovocim-1 (10 mg/kg) increases the production of ovalbumin-specific IgG1 in wild-type, but notTLR2-/-, mice sensitized to ovalbumin.2It also enhances anti-PD-L1 antibody-induced activation of cytotoxic T lymphocytes, reduction of tumor growth, and increases in survival in a B16/F10 murine melanoma mo...
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...
T83775	STING Agonist 12L Stimulator of Interferon Genes Agonist 12L
	STING激动剂12L是一种刺激干扰素基因(STING)的激动剂。它与野生型STING结合(IC50 = 1.15 µM)，以及STING的R232、AQ和Q变体(IC50分别为1.06、0.61和1.12 µM)，并在THP-1和RAW 264.7细胞中诱导报告基因表达(EC50分别为0.38和12.94 µM)。STING激动剂12L (5 µM)在THP-1细胞中诱导IFNB1、CXCL10和IL6 mRNA的表达。在体内，STING激动剂12L (10 mg/kg)提高了血浆IFN-β水平，并且在B16/F10小鼠黑色素瘤模型中减少了肿瘤体积和肺转移灶的数量。

化合物

Cat.No: T9973

Target: FAK

Cat.No: T27371

Synonym: FR167356,FR 167356

Target: ATPase

Cat.No: T36460

Synonym: CAY10736

Cat.No: T36497

Synonym: CAY10735

Cat.No: T37586

Cat.No: T79528

Target: PD-1/PD-L1

Anticancer agent 106

Cat.No: T78958

Target: Apoptosis

Cat.No: T79705

Target: PD-1/PD-L1

Cat.No: T83886

Antitumor photosensitizer-4

Cat.No: T79711

Target: Apoptosis

Cat.No: T36138

Anticancer agent 157

Cat.No: T78855

Target: NO Synthase

Cat.No: T38320

Synonym: 93-O17S

Cat.No: T36181

Cat.No: T36645

Synonym: CAY10763

Cat.No: T37722

Cat.No: T83765

Synonym: DDA

STING Agonist 12L

Cat.No: T83775

Synonym: Stimulator of Interferon Genes Agonist 12L

Cat. No.	Product Name	Target	Signaling Pathways
TN5212	Uvedalin	Others	Others
	Uvedalin shows cytotoxicity against HeLa, HL-60, and Murine B16-F10 melanoma cell lines.
TN6054	Norglaucine hydrochloride
	(+)-Norglaucine shows cytotoxic activity toward the tumor cell lines B16-F10 (mouse melanoma), HepG2 (human hepatocellular carcinoma), K562 (human chronic myelocytic leukemia) and HL-60 (human promyelocytic leukemia) and non-tumor peripheral blood mononuc
TN2792	2-Oxopomolic acid
	2-Oxopomolic acid shows cytotoxic activity, it shows a significant decrease in intracellular melanin content in B16-F10 cells, and in culture media melanin. 2-Oxopomolic acid shows radical-scavenging activities similar to that of the reference antioxidant
TN4085	Fupenzic acid	Others	Others
	Fupenzic acid shows a significant decrease in intracellular melanin content in B16-F10 cells, and in culture media melanin.

天然产物

Cat.No: TN5212

Target: Others

Norglaucine hydrochloride

Cat.No: TN6054

2-Oxopomolic acid

Cat.No: TN2792

Cat.No: TN4085

Target: Others

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