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15

抑制剂 & 化合物

8

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T6588	Mitoxantrone 米托蒽醌,mitozantrone	Topoisomerase; PKC	Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair
	Mitoxantrone (mitozantrone) 是一种拓扑异构酶 II 的抑制剂，也可抑制蛋白激酶C (PKC)，IC50值为8.5 μM。
T0158	Mitoxantrone dihydrochloride 米托蒽醌二盐酸盐,盐酸米托蒽醌,Mitoxantrone 2HCl,Mitoxantrone hydrochloride,NSC-301739,mitozantrone dihydrochloride	Topoisomerase; PKC	Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair
	Mitoxantrone dihydrochloride (NSC-301739) 是一种拓扑异构酶 II 的抑制剂；也可抑制蛋白激酶C (PKC)，IC50值为8.5 μM。
T12783	RWJ 50271	Integrin	Cytoskeletal Signaling
	RWJ 50271 是具有口服活性的选择性LFA-1/ICAM-1相互作用抑制剂，抑制 LFA-1/ICAM-1 介导的细胞粘附，在细胞HL60中的IC50值为 5.0 μM。
T14946	Ch55 Ch-55,CH 55,3,5-Di-tert-butylchalcone	Retinoid Receptor	Metabolism
	Ch55 (3,5-Di-tert-butylchalcone)是HL60细胞分化的有效诱导剂(EC50 = 200 nM)，与RAR-α和RAR-β受体显示出高亲和力。Ch55可用于有关癌症的研究。
T36963	CAY10503
	CAY10503 is a proapoptotic, antiproliferative compound that is able to arrest cell cycle progression in the G0-G1 phase. CAY10503 inhibits the growth of HL60, multidrug resistant HL60R, and K562 cells with IC50 values of 7.0, 23, and 20 μM, respectively. Accumulation of HL60 cells in G0-G1 occurred within eight hours following treatment with 50 μM CAY10503, whereas 10 μM CAY10503 required 96 hours for cell cycle arrest to appear. CAY10503 also induces differentiation of HL60 cells into the follo...
T10969	DC1SMe	Others	Others
	DC1 is an ADC cytotoxin, similar to the small groove-binding DNA alkylating agent CC-1065. DC1 can be used to synthesize antibody-drug conjugates targeted to the treatment of cancer. DC1Sme is a DC1 derivative with IC50 values of Ramos, Namalwa, HL60 / s
T10975	DC44SMe	Others	Others
	The IC50 of DC44SMe for Ramos, Namalwa and HL60 / s cancer cells was 2.0 nM, 2.8 nM and 1.9 nM, respectively. DC44SMe can be used for targeted treatment of cancer. DC44SMe is a phosphate prodrug of DC44 and can be used in the synthesis of antibody-drug co
T60559	S-(N-PhenethylthiocarbaMoyl)-L-cysteine
	S-(N-PhenethylthiocarbaMoyl)-L-cysteine (PEITC-Cys) 是一种抗癌剂。S-(N-PhenethylthiocarbaMoyl)-L-cysteine 具有抗白血病活性，可抑制 HL60 细胞中的 DNA 合成。S-(N-PhenethylthiocarbaMoyl)-L-cysteine 是P450的抑制剂。
T78068	O-allylvanillin	Others	Others
	O-allylvanillin为o-烯丙基查尔酮衍生物，呈现抗癌活性。该化合物对THP-1、HL60、Hep-G2、MCF-7细胞系生长抑制作用显著，其IC50值依次为74.76 μM、63.52 μM、90.99 μM、90.11 μM。
T78854	WK499
	BCL6-IN-10 (Compound WK499) 是抑制蛋白 BCL6 的化合物。该化合物能干扰 BCL6 与 SMRT 蛋白的结合作用，进而诱导 apoptosis、导致细胞周期阻滞以及 DNA 损伤。针对多种 Acute Myeloid Leukemia (AML) 细胞株，如 OCI-AML3、THP1、MOLM13、HL60, KG1, NB4，BCL6-IN-10 显示出较强的抑制活性，其 IC50s 分别为 0.91、1.63、1.026、7.42、0.87、0.85 μM。
T79478	Anti-inflammatory agent 45	Apoptosis	Apoptosis
	Anti-inflammatory agent 45（化合物2v）作为一种抗癌剂，直接抑制多种血癌细胞系（如白血病、淋巴瘤、骨髓瘤）的生长。该化合物能够诱导HL60白血病细胞发生凋亡，并可抑制NO生成，其半抑制浓度（IC50）为14.7 μM。
T10976	DC4SMe	Others	Others
	The IC50s of DC4SMe on Ramos, Namalwa and HL60 / s cancer cells were 1.9 nM, 2.9 nM and 1.8 nM, respectively. DC4SMe can be used for targeted therapy of tumors. DC4SMe is a phosphate prodrug of the cytotoxic DNA alkylating agent DC4 and can be used in the
T10971	DC10SMe	Others	Others
	DC10SMe is a DNA alkylating agent that can be used in the synthesis of antibody-drug conjugates (ADC). The IC50 of DC10SMe for Ramos, Namalwa and HL60 / s cancer cells were 15 pM, 12 pM and 12 pM, respectively.
T63957	PI3K-IN-29
	PI3K-IN-29 是一种有效的 PI3K 抑制剂。PI3K-IN-29 对 U87MG、HeLa 和 HL60 细胞具有较好的抑制作用，IC50值分别为 0.264、2.04 和 1.14 µM。PI3K-IN-29 通过抑制PI3K 催化的Akt 的磷酸化来抑制PI3K/Akt 通路。
T79683	HDAC/CD13-IN-1	Others	Others
	HDAC/CD13-IN-1 (Compound 12) 作为HDAC/CD13抑制剂, 对hCD13的IC50为0.34 μM, 猪CD13为0.53 μM, 对HDAC1/2/3的IC50分别为0.03、0.06、0.02 μM。此化合物有效抑制MV4-11、K562、Jeko-1 和 HL60细胞增殖, IC50范围为0.25-2.04 μM，并诱导癌细胞凋亡。同时表现出抗转移和抗侵袭的特性。

化合物

Cat.No: T6588

Synonym: 米托蒽醌,mitozantrone

Target: Topoisomerase, PKC

Mitoxantrone dihydrochloride

Cat.No: T0158

Synonym: 米托蒽醌二盐酸盐,盐酸米托蒽醌,Mitoxantrone 2HCl,Mitoxantrone hydrochloride,NSC-301739,mitozantrone dihydrochloride

Target: Topoisomerase, PKC

Cat.No: T12783

Target: Integrin

Cat.No: T14946

Synonym: Ch-55,CH 55,3,5-Di-tert-butylchalcone

Target: Retinoid Receptor

Cat.No: T36963

Cat.No: T10969

Target: Others

Cat.No: T10975

Target: Others

S-(N-PhenethylthiocarbaMoyl)-L-cysteine

Cat.No: T60559

O-allylvanillin

Cat.No: T78068

Target: Others

Cat.No: T78854

Anti-inflammatory agent 45

Cat.No: T79478

Target: Apoptosis

Cat.No: T10976

Target: Others

Cat.No: T10971

Target: Others

Cat.No: T63957

Cat.No: T79683

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
T0974	Novobiocin Sodium Albamycinsodium,新生霉素钠,Cathomycin,Albamycin	Potassium Channel; DNA gyrase; Topoisomerase; Antibacterial; Antibiotic; ABC; Autophagy	Autophagy; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Microbiology/Virology
	Novobiocin Sodium (Albamycinsodium) 是源自 Streptomyces niveus 的抗生素。它的化学结构类似于香豆素。Novobiocin 与 DNA 促旋酶结合并阻断三磷酸腺苷活性。
T3774	Gracillin 山药,纤细薯蓣皂苷	cell cycle arrest	Cell Cycle/Checkpoint
	Gracillin 是一种甾体皂苷，从植物的根里提取得到，有抗肿瘤作用。
T2S0357	6-Hydroxycoumarin 6-hydroxychromen-2-one,6-羟基香豆素	Others; Carbonic Anhydrase	Metabolism; Others
	6-Hydroxycoumarin (6-hydroxychromen-2-one) 是一种香豆素。其中香豆素具有抗炎，支气管扩张，解热，血管扩张，抗氧化，抗菌，抗真菌，抑菌和抗肿瘤作用。
T2924	Phloretin 根皮素,Dihydronaringenin,NSC 407292,RJC 02792	SGLT; transporter; Endogenous Metabolite	GPCR/G Protein; Metabolism
	Phloretin (NSC-407292) 是从苹果树叶中提取的一种查耳酮，具有抗炎、抗氧化和抗癌活性。它是真核尿素转运蛋白抑制剂，可阻断 VacA 介导的尿素和离子转运，有潜力用于类风湿性关节炎和过敏性气道炎症的相关研究。
TN2835	28-Deoxonimbolide	Caspase	Apoptosis; Proteases/Proteasome
	28-Deoxonimbolide exhibits potent cytotoxic activity against HL60 leukemia cells.
T1507	Streptozocin STZ,Streptozotocin,链脲佐菌素,NSC-85998,链脲菌素,U 9889	DNA Alkylator/Crosslinker; DNA Alkylation; DNA/RNA Synthesis; Antibacterial; Antibiotic; Autophagy	Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology
	Streptozocin (NSC-85998) 是一种抗生素，可诱导 DNA 甲基化。Streptozocin 对产生胰岛素的胰岛 B 细胞具有毒性，常用于构建 1 型糖尿病的动物模型。该产品在溶液中不稳定，建议现配现用。
T80995	Theasaponin E2
	Theasaponin E2, 一种从茶树分离得到的化合物，对K562和HL60细胞表现出显著的细胞毒性，其半抑制浓度(IC50)为14.7 μg/mL。
TN2977	3-O-trans-p-Coumaroyltormentic acid	Caspase; Antifection	Apoptosis; Microbiology/Virology; Proteases/Proteasome
	3-O-(E)-p-coumaroyl tormentic acid may be promising lead compound for developing an effective drug for treatment of leukemia, it induces apoptotic cell death in human leukemia (HL60) via mainly mitochondrial pathway by, at least in part, Topo I inhibition. 3-O-trans-p-coumaroyltormentic acid shows cytotoxicity against four human tumor cell lines (A549, SK-OV-3, SK-MEL-2, and HCT-15) in vitro, the IC50 values of 13.72, 14.29,14.61, 14.04 uM, respectively. 3beta-O-cis-p-Coumaroyltormentic acid, an...

天然产物

Novobiocin Sodium

Cat.No: T0974

Synonym: Albamycinsodium,新生霉素钠,Cathomycin,Albamycin

Target: Potassium Channel, DNA gyrase, Topoisomerase, Antibacterial, Antibiotic, ABC, Autophagy

Cat.No: T3774

Synonym: 山药,纤细薯蓣皂苷

Target: cell cycle arrest

6-Hydroxycoumarin

Cat.No: T2S0357

Synonym: 6-hydroxychromen-2-one,6-羟基香豆素

Target: Others, Carbonic Anhydrase

Cat.No: T2924

Synonym: 根皮素,Dihydronaringenin,NSC 407292,RJC 02792

Target: SGLT, transporter, Endogenous Metabolite

28-Deoxonimbolide

Cat.No: TN2835

Target: Caspase

Cat.No: T1507

Synonym: STZ,Streptozotocin,链脲佐菌素,NSC-85998,链脲菌素,U 9889

Target: DNA Alkylator/Crosslinker, DNA Alkylation, DNA/RNA Synthesis, Antibacterial, Antibiotic, Autophagy

Cat.No: T80995

3-O-trans-p-Coumaroyltormentic acid

Cat.No: TN2977

Target: Caspase, Antifection

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