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23

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T21679	4'-bromo-Resveratrol	Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair
	4'-Bromo-resveratrol 是Sirtuin-1和Sirtuin-3的双重抑制剂。它通过线粒体代谢重编程，使黑色素瘤细胞的生长受到抑制。它通过代谢重编程、影响细胞周期以及细胞凋亡的信号传导，使其在黑色素瘤细胞中发挥抗增殖作用。
T10104	3,4-Dihydroxybenzylamine hydrobromide NSC 263475 hydrobromide,3,4-二羟基苄胺·氢溴酸	Others; DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Others
	3,4-Dihydroxybenzylamine hydrobromide (NSC-263475 hydrobromide) 抑制黑色素瘤细胞中的 DNA 聚合酶活性，并在具有不同程度酪氨酸酶活性的黑色素瘤细胞系中显示出生长抑制活性。
T28206	NSC49652 NSC 49652,NSC-49652	Apoptosis	Apoptosis
	NSC49652 在神经元和黑色素瘤细胞中触发依赖于 p75NTR 和 JNK 活性的凋亡细胞死亡，并抑制黑色素瘤小鼠模型中的肿瘤生长。
T17195	UC-112	Others	Others
	UC-112是凋亡抑制蛋白IAP 新型高效抑制剂，癌细胞IC50值0.7-3.4uM。
T11209	EOAI3402143	DUB	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Ubiquitination
	EOAI3402143 是一种去泛素化酶抑制剂，以剂量依赖性抑制 Usp9x/Usp24和 Usp5，增加肿瘤细胞凋亡。
T28145	ND-322 HCl ND 322 Hydrochloride,ND322 Hydrochloride,ND-322 Hydrochloride,ND322 HCl	MMP	Proteases/Proteasome
	ND-322 HCl (ND 322 Hydrochloride) 是 MT1-MMP 和 MMP2 的选择性抑制剂，可减少体外黑色素瘤细胞的生长、迁移和侵袭。
T17228	Sabizabulin ABI-231,VERU-111	Microtubule Associated	Cytoskeletal Signaling
	Sabizabulin (ABI-231) 是一种有效且具有口服生物利用度的 α 和 β 微管蛋白抑制剂，可对抗黑色素瘤和前列腺癌细胞系。 Sabizabulin 通过靶向 HPV E6 和 E7 抑制宫颈癌细胞的肿瘤生长和转移表型。 Sabizabulin 显示出抗增殖活性，可用于前列腺癌研究。
T36674	DMU-212	Apoptosis; ERK	Apoptosis; MAPK
	DMU-212 是具有口服活性的白藜芦醇的甲基化衍生物，表现出抗分裂、抗增殖、抗氧化和促进细胞凋亡的活性。它通过诱导凋亡和激活ERK1/2蛋白阻止有丝分裂。
T29973	AMG-628 AMG628,AMG 628,CHEMBL226574,UNII-28J966TN3X
	AMG-628 is an effective and ATP-competitive RAF kinase inhibitor. AMG-628 has been shown to inhibit growth and induce cell cycle arrest and apoptosis in colon and melanoma cell lines with B-RAFV600E mutations.
T12003	Mensacarcin	Others	Others
	Mensacarcin, a highly complex polyketide compound, exhibits multifaceted effects on cellular processes. Specifically, it targets mitochondria, perturbs energy metabolism within these organelles, and activates caspase-dependent apoptotic pathways. Functionally, Mensacarcin can serve as a cytotoxic constituent in antibody-drug conjugates (ADCs). Furthermore, this antibiotic compound displays broad-spectrum inhibition of cell growth across various cancer cell lines and demonstrates potent induction...
T71736	AMG-628, (R)-
	AMG-628, (R)- is the R isomer of AMG-628 --- a potent, ATP-competitive inhibitor of Raf kinases. AMG-628 displays selectivity for Raf kinases and inhibits activation of tyrosine protein kinases such as VEGFR2, Lyn, Flt1 and Fms. AMG-628 has shown to inhibit growth, and induces cell cycle arrest and apoptosis in colon and melanoma cell lines with the B-RafV600E mutation.
T68523	AMG-628, (S)-
	AMG-628, (S)-, is the S isomer of AMG-628 --- a potent, ATP-competitive inhibitor of Raf kinases. AMG-628 displays selectivity for Raf kinases and inhibits activation of tyrosine protein kinases such as VEGFR2, Lyn, Flt1 and Fms. AMG-628 has shown to inhibit growth, and induces cell cycle arrest and apoptosis in colon and melanoma cell lines with the B-RafV600E mutation.
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 ...
T60821	ACA-28
	ACA-28 (compound 2a) 是ERK MAPK 信号的有效调节剂，可通过过度激活 ERK 诱导细胞凋亡，从而选择性抑制癌细胞生长。ACA-28 对黑色素瘤细胞 (SK-MEL-28) 和正常黑色素细胞 (NHEM) 细胞生长的IC50值分别为 5.3 和 10.1 μM。
T72188	Nicotinamide Hydrochloride Niacinamide Hydrochloride,Nicotinic acid amide Hydrochloride,Niacinamide Hydrochloride ; Nicotinic acid amide Hydrochloride
	Nicotinamide Hydrochloride 是维生素 B3 或烟酸的一种形式，可抑制SIRT2的体外活性，其EC50值为 2 μM。 Nicotinamide Hydrochloride 可抑制 90% 的黑色素瘤细胞数量，并增加细胞内 NAD+、ATP、ROS 水平。Nicotinamide Hydrochloride 抑制黑色素瘤小鼠的肿瘤生长并提高生存率，可用于黑色素瘤等皮肤癌相关的研究。
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 ...
T79143	MS934	MEK	MAPK
	MS934是一种VHL招募MEK1/2降解剂，能够有效抑制HT-29细胞生长，表现出抗增殖效果，其GI50值达到0.023 μM。该化合物适用于包括黑色素瘤、非小细胞肺癌(NSCLC)、结直肠癌、原发性脑肿瘤和肝细胞癌在内的多种人类癌症研究。
T83756	S1H TFA Site 1-binding Helix
	S1H是一种人造肽类模拟物，模仿人类生长激素的第36至51个氨基酸，且为生长激素受体的拮抗剂。在溶液中呈现α-螺旋结构，并在100和200纳摩尔（nM）的浓度下，能降低SK-MEL-28和MALME-3M黑色素瘤细胞系以及IM-9 B细胞淋巴细胞中，由人类生长激素及泌乳素诱导的STAT5磷酸化。
T37561	BX-320
	BX-320 is an inhibitor of the serine/threonine kinase 3-phosphoinositide-dependent protein kinase 1 (PDK1; IC50= 30 nM).1It is selective for PDK1 over a panel of 10 additional kinases (IC50s = >820 nM for all). BX-320 inhibits Akt and p70S6K1 phosphorylation in PC3 cells (IC50s = 1-3 μM). It induces apoptosis in, and inhibits the growth of, MDA-MB-468 breast cancer cells (IC50s = 0.5 and 0.6 μM, respectively), as well as inhibits cell growth in a panel of cancer cells (IC50s = 0.12-1.2 μM). BX-3...
T82605	DB21, Galectin-1 Antagonist	Galectin	Immunology/Inflammation
	DB21, Galectin-1 Antagonist 是一种用于抑制galectin-1 (GAL1)与细胞表面聚糖结合的二苯并呋喃缀合肽模拟物。在黑色素瘤、肺腺癌和卵巢癌模型中，该化合物能增强血管生成和肿瘤生长的抑制效果。
T36846	Chromomycin A2
	Chromomycin A2 is an aureolic acid that has been found in several marine actinomycetes and has antibacterial and anticancer activities. Chromomycin A2 inhibits the growth of B. subtilis in an agar diffusion assay. It also inhibits the growth of human SGC7901 gastric cancer, HepG2 hepatocellular carcinoma, A549 lung epithelial adenocarcinoma, HCT116 colon cancer, and COC1 ovarian cancer cells, as well as human umbilical vein endothelial cells (HUVECs; IC50s = 4, 0.5, 3, 5, 5, and 8 nM, respective...
T35573	Adenosine 5’-methylenediphosphate (hydrate)
	Adenosine 5’-methylenediphosphate is an inhibitor of ecto-5’-nucleotidase, also known as CD73, with a Kivalue of 37 nM.1It inhibits cAMP accumulation induced by adenosine 5’-monophosphate , adenosine 5’-diphosphate , or adenosine 5’-triphosphate but not adenosine in VA-13 human fibroblasts when used at a concentration of 100 μM. Adenosine 5’-methylenediphosphate reduces proliferation of U138MG glioma cells, as well as inhibits the invasion and migration of MHCC97H hepatocellular carcinoma (HCC) ...
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

4'-bromo-Resveratrol

Cat.No: T21679

Target: Sirtuin

3,4-Dihydroxybenzylamine hydrobromide

Cat.No: T10104

Synonym: NSC 263475 hydrobromide,3,4-二羟基苄胺·氢溴酸

Target: Others, DNA/RNA Synthesis

Cat.No: T28206

Synonym: NSC 49652,NSC-49652

Target: Apoptosis

Cat.No: T17195

Target: Others

Cat.No: T11209

Target: DUB

Cat.No: T28145

Synonym: ND 322 Hydrochloride,ND322 Hydrochloride,ND-322 Hydrochloride,ND322 HCl

Target: MMP

Cat.No: T17228

Synonym: ABI-231,VERU-111

Target: Microtubule Associated

Cat.No: T36674

Target: Apoptosis, ERK

Cat.No: T29973

Synonym: AMG628,AMG 628,CHEMBL226574,UNII-28J966TN3X

Cat.No: T12003

Target: Others

Cat.No: T71736

Cat.No: T68523

Cat.No: T36460

Synonym: CAY10736

Cat.No: T60821

Nicotinamide Hydrochloride

Cat.No: T72188

Synonym: Niacinamide Hydrochloride,Nicotinic acid amide Hydrochloride,Niacinamide Hydrochloride ; Nicotinic acid amide Hydrochloride

Cat.No: T36497

Synonym: CAY10735

Cat.No: T79143

Target: MEK

Cat.No: T83756

Synonym: Site 1-binding Helix

Cat.No: T37561

DB21, Galectin-1 Antagonist

Cat.No: T82605

Target: Galectin

Cat.No: T36846

Adenosine 5’-methylenediphosphate (hydrate)

Cat.No: T35573

Cat.No: T83765

Synonym: DDA

Cat. No.	Product Name	Target	Signaling Pathways
T3229	Cytochalasin D	ATPase; p38 MAPK; Calcium Channel; Akt; PI3K	Cytoskeletal Signaling; MAPK; Membrane transporter/Ion channel; Metabolism; PI3K/Akt/mTOR signaling
	Cytochalasin D is an actin inhibitor, the removal of actin stress fibers is crucial for the chondrogenic differentiation. It may be an inhibitor of some fertilization processes such as sperm penetration or sperm head decondensation. Cytochalasin D inhibit
T81201	Sartorypyrone B
	Sartorypyrone B为Chevalone C的2β-乙酰氧基衍生物，由海绵源真菌Neosartorya tsunodae(KUFC 9213)的培养物中乙酸乙酯提取得到。该化合物对MCF-7、NCI-H460和A375-C5细胞系展示出较强的生长抑制活性，GI50s值分别为17.8、20.5和25.0 μM，显示其在乳腺癌、非小细胞肺癌和黑色素瘤研究中的应用潜力。
T35624	Ajoene
	Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities, including antibacterial, anticancer, antiplatelet, and antioxidant properties.1,2,3,4It is active against Gram-positive (MICs = 5-160 &#181g/ml) and Gram-negative bacteria (MICs = 136-200 &#181g/ml), as well as yeasts (MICs = 10-20 &#181g/ml).1Ajoene is cytotoxic to mouse melanoma cells (IC50= 18 &#181M), as well as human colon, lung, mammary, and pancreatic cancer cells (IC50s = 7-41 &#181M).2It reduces...

天然产物

Cat.No: T3229

Target: ATPase, p38 MAPK, Calcium Channel, Akt, PI3K

Sartorypyrone B

Cat.No: T81201

Cat.No: T35624

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