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20

抑制剂 & 化合物

22

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T13224	Tubulin inhibitor 6 iHAP1	Microtubule Associated	Cytoskeletal Signaling
	Tubulin inhibitor 6 (iHAP1) 是一种微管蛋白抑制剂，抑制微管蛋白聚合，IC50为 0.87 μM。它抑制多种癌细胞系，抑制 K562 细胞生长，IC50为 840 nM。
T2394	Pixantrone dimaleate 匹克生琼来酸盐,BBR-2778,Pixantrone Maleate,BBR 2778 dimaleate,马来酸匹衫琼	Topoisomerase	DNA Damage/DNA Repair
	Pixantrone dimaleate (Pixantrone Maleate) 是一种拓扑异构酶 II 的抑制剂和 DNA 嵌入剂，是一种实验性抗肿瘤药物。
T13226	Tubulin inhibitor 8	Microtubule Associated	Cytoskeletal Signaling
	Tubulin inhibitor 8是管蛋白和多种癌症细胞系的抑制剂，对管蛋白聚合和K562细胞生长具有抑制作用，IC50分别为0.73μM 和14nM。
T12926	SJB3-019A	Others; DUB	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Others; Ubiquitination
	SJB3-019A 是一种有效的、有效的和新型的泛素特异性蛋白酶1（USP1）抑制剂，在 K562细胞中促进 ID1降解和细胞毒性的作用是 SJB2-043的5倍，IC50为0.0781 μM。SJB3-019A 抑制细胞增殖，使细胞凋亡。
T1937	Spautin-1 Spautin 1	Apoptosis; DUB; Autophagy	Apoptosis; Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Ubiquitination
	Spautin-1是一种特异性自噬抑制剂，可抑制泛素特异性肽酶 USP10和 USP13，IC50s 约为0.6到0.7 μM。
T1817	GNF-2 GNF2	SARS-CoV; Bcr-Abl	Angiogenesis; Cytoskeletal Signaling; Microbiology/Virology; Tyrosine Kinase/Adaptors
	GNF-2 是一种高选择性的非 ATP 竞争性 Bcr-Abl 抑制剂。它抑制 Ba/F3.p210 增殖，IC50为 138 nM。
T63932	BCR-ABL-IN-4
	BCR-ABL-IN-4 是 BCR-ABLL 抑制剂，表现出抗癌活性。BCR-ABL-IN-4 对癌细胞生长具有抑制作用，能够作用于 K562 细胞 (IC50: 0.67 nM) 和 BCR-ABL T315I 转染的 Ba/F3 细胞 (IC50: 16 nM)。
T13225	Tubulin inhibitor 7	Microtubule Associated	Cytoskeletal Signaling
	Tubulin inhibitor 7 is an inhibitor of tubulin and a potent inhibitor of multiple cancer cell lines (tubulin polymerization (IC50: 0.52 μM), K562 cell growth (IC50: 11 nM)).
T78815	MOZ-IN-3	Histone Acetyltransferase	Chromatin/Epigenetic
	MOZ-IN-3 (Compound 6j) 是KAT6A (MOZ) 乙酰转移酶的抑制剂，IC50值为30 nM。该化合物在四种髓系白血病细胞系（HL-60、U937、SKNO-1、K562）上展现了抗肿瘤活性，并且显示出良好的代谢稳定性及药代动力学特性。
T82715	Cisplatin-resistant cells-IN-1
	Cisplatin-resistant cells-IN-1（化合物8）对顽固的铂类药物抗性细胞具有较高的细胞毒性。在低纳摩尔浓度范围内（IC50：0.14–1.79 μM in A549/A549-R, K562/K562-R, and MCF-7/MCF-7TamR cells），该化合物能有效降低代谢活性。
T62217	Tubulin polymerization-IN-9
	Tubulin polymerization-IN-9 是一种微管蛋白 (tubulin) 的有效抑制剂 (IC50: 1.82 μM)。Tubulin polymerization-IN-9 能够将 K562 细胞的细胞周期停滞在 G2/M 期，并诱导其凋亡 (apoptosis) 及线粒体去极化。Tubulin polymerization-IN-9 表现出强大的抗血管和抗肿瘤作用。
T28092	MPT0B206
	MPT0B206 is a novel tubulin polymerization inhibitor. MPT0B206 induced G2/M cell cycle arrest and the appearance of the mitotic marker MPM-2 in K562 and K562R cells, which is associated with the upregulation of cyclin B1 and the dephosphorylation of Cdc2.
T78843	MET/PDGFRA-IN-1	c-Met/HGFR	Tyrosine Kinase/Adaptors
	MET/PDGFRA-IN-1 (compound 8c) 作为MET和PDGFRA蛋白的抑制剂，以36 μM对MET的IC50值显示活性。该化合物能够抑制MET磷酸化并触发细胞凋亡(apoptosis)。此外，MET/PDGFRA-IN-1有效抑止了多种MET阳性细胞系的增殖，包括AsPc-1、EBC-1、MKN-45、Mia-Paca-2、HT-29和K562，其IC50s分别为15.3、19.0、22.0、25.6、21.0、31.5 μM。
T79322	Antiproliferative agent-30
	Antiproliferative agent-30 (Compound 8g) 抑制微管蛋白组装且可抑制FLT3及Abl1。该化合物展现出对血管的破坏活性，并对多种癌细胞系表现出强效的抗增殖能力，包括HCT-116、K562及MV-4-11细胞（IC50值分别为0.054 nM、0.008 nM、0.144 nM）。此外，Antiproliferative agent-30 亦对携带FLT3-ITD-TKD突变的AML显示出抗癌效果。
T79754	JNK-IN-14	JNK	MAPK
	JNK-IN-14是一种激酶（JNK1/2/3）抑制剂，IC50值为1.81、12.7和10.5 nM。它能诱导早期apoptosis，并在G2/M阶段引起细胞周期阻滞。与SP600125相比，在K562白血病细胞中，JNK-IN-14更强有效地抑制了Beclin-1的表达。
T78608	Anticancer agent 164	Apoptosis	Apoptosis
	CML-IN-1（compound 7）是一种高效抗癌药物，针对人类慢性粒细胞白血病（CML）细胞系K562，能有效诱导凋亡（apoptosis）。该化合物主要通过显著抑制PI3K/Akt信号通路的蛋白磷酸化来发挥作用，同时CML-IN-1（compound 4）也能通过抑制结直肠癌的MEK/ERK信号通路来阻止细胞增殖。
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...
T35423	7-oxo Staurosporine
	7-oxo Staurosporine is an antibiotic originally isolated from S. platensis with diverse biological activites. It inhibits PKC, PKA, phosphorylase kinase, EGFR, and c-Src in vitro (IC50s = 9, 26, 5, 200, and 800 nM, respectively). 7-oxo Staurosporine induces cell cycle arrest in the G2/M phase in human leukemia K562 cells with a minimal effective dose (MED) of 30 ng/ml. It is cytotoxic to P388 mouse leukemia cells that are resistant and susceptible to doxorubicin . 7-oxo Staurosporine inhibits gr...
T83786	8-Chloroadenosine-5'-triphosphate sodium 8-chloro ATP
	8-Chloroadenosine-5’-triphosphate（8-chloro ATP）是抗癌剂8-chloro cAMP的活性代谢物，也是核苷酸腺苷5’-三磷酸（ATP）的衍生物。它通过8-chloro cAMP、8-chloroadenosine以及一磷酸和二磷酸中间体形成。应用8-chloro cAMP或8-chloroadenosine后，8-chloro ATP可累积长达12小时，与细胞生长抑制、内源性ATP水平下降以及患者源多发性骨髓瘤细胞中RNA合成减少（但DNA合成不受影响）相关。在1.5至8 mM浓度范围内，它抑制topoisomerase II-α依赖的超螺旋pUC19 DNA放松，同时在1 mM时减少了K562人髓性白血病细胞中topoisomerase II-α催化的ATP水解50%。
T36978	AS-99 TFA
	AS-99 TFA is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 μM, Kd= 0.89 μM) with anti-leukemic activity. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo[1]. AS-99 TFA is tested against a panel of 20 histone methyltransferases, including NSD1, NSD2, NSD3, and SETD2. NO significant inhibition is observed at 50 μM of AS-99 TFA on any of the tested...

化合物

Tubulin inhibitor 6

Cat.No: T13224

Synonym: iHAP1

Target: Microtubule Associated

Pixantrone dimaleate

Cat.No: T2394

Synonym: 匹克生琼来酸盐,BBR-2778,Pixantrone Maleate,BBR 2778 dimaleate,马来酸匹衫琼

Target: Topoisomerase

Tubulin inhibitor 8

Cat.No: T13226

Target: Microtubule Associated

Cat.No: T12926

Target: Others, DUB

Cat.No: T1937

Synonym: Spautin 1

Target: Apoptosis, DUB, Autophagy

Cat.No: T1817

Synonym: GNF2

Target: SARS-CoV, Bcr-Abl

Cat.No: T63932

Tubulin inhibitor 7

Cat.No: T13225

Target: Microtubule Associated

Cat.No: T78815

Target: Histone Acetyltransferase

Cisplatin-resistant cells-IN-1

Cat.No: T82715

Tubulin polymerization-IN-9

Cat.No: T62217

Cat.No: T28092

MET/PDGFRA-IN-1

Cat.No: T78843

Target: c-Met/HGFR

Antiproliferative agent-30

Cat.No: T79322

Cat.No: T79754

Target: JNK

Anticancer agent 164

Cat.No: T78608

Target: Apoptosis

Cat.No: T36963

7-oxo Staurosporine

Cat.No: T35423

8-Chloroadenosine-5'-triphosphate sodium

Cat.No: T83786

Synonym: 8-chloro ATP

Cat.No: T36978

Cat. No.	Product Name	Target	Signaling Pathways
T1511	Daunorubicin hydrochloride Daunomycin HCl,盐酸佐柔比星,盐酸柔红霉素,RP-13057 Hydrochloride,Rubidomycin hydrochloride,Daunorubicin HCl,Daunomycin	Apoptosis; DNA/RNA Synthesis; Topoisomerase; Antibacterial; Antibiotic; Autophagy	Apoptosis; Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology
	Daunorubicin hydrochloride (Rubidomycin hydrochloride) 是一种蒽环类氨基糖苷类抗肿瘤药物，可抑制 DNA 复制和修复以及 RNA 和蛋白质合成。
TN2755	2-Desoxy-4-epi-pulchellin	Anti-infection	Microbiology/Virology
	2-Desoxy-4-epi-pulchellin 是分离自 Polygonum hydropiper 的二氯甲烷可溶部分的一种化合物。
T4S1943	Kirenol 奇壬醇,奇任醇,Kirel	Wnt/beta-catenin	Cytoskeletal Signaling; Stem Cells
	Kirenol (Kirel) 是分离自 Siegesbeckia orientalis 中的，具有抗氧化、抗炎、抗过敏、抗关节炎活性，可用于缓解疼痛的研究。
T4085	Paris saponin VII 重楼皂苷 VII,Chonglou Saponin VII,Polyphyllin-VII,Dioscinin,Paris saponin-VII	Apoptosis; BCL; Others; PARP; p38 MAPK; Akt; Caspase; P-gp; Autophagy	Apoptosis; Autophagy; Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; MAPK; Membrane transporter/Ion channel; Neuroscience; Others; PI3K/Akt/mTOR signaling; Proteases/Proteasome
	Paris saponin VII (Dioscini) 是从延龄草的根和根茎中分离的一种甾体皂苷。它减弱线粒体膜电位，增加凋亡相关蛋白的表达，并降低Bcl-2、caspase-9、caspase-3、PARP-1和p-Akt 的蛋白表达水平。它在 K562/ADR 细胞中诱导强烈的自噬，可研究白血病。
T6S1315	Oroxylin A 千层纸素A,6-Methoxybaicalein,Baicalein 6-methyl ether	Virus Protease; HIF/HIF Prolyl-Hydroxylase; Autophagy	Autophagy; Chromatin/Epigenetic; Metabolism; Microbiology/Virology
	Oroxylin A (Baicalein 6-methyl ether) 是一种有活性的黄酮，具有较强的抗癌作用。
T3398	Icaritin Anhydroicaritin,去水淫羊藿黄素,Cycloicaritin	Apoptosis; JAK; STAT; Autophagy	Angiogenesis; Apoptosis; Autophagy; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells
	Icaritin (Anhydroicaritin) 是Epimedium Genusis 的异戊二烯类黄酮衍生物，有效抑制 K562 细胞和原代 CML 细胞的增殖。它可以调节MAPK/ERK/JNK 和JAK2/STAT3/AKT 信号传导，并具有增强成骨的作用。
T2S2215	Crebanine	Apoptosis; Others; Akt	Apoptosis; Cytoskeletal Signaling; Others; PI3K/Akt/mTOR signaling
	Crebanine 是来自于韦诺萨千金藤的一种生物碱，通过抑制 MAPKs 和 Akt 信号通路表现出抗炎活性，还具有抗心律失常的作用。它可诱导人类癌细胞的 G1阻滞和凋亡。
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
TN5358	Eupahualin C
	Eupahualin C shows significant activities against cell lines of human chronic myelogenous leukemia (K562) and human bone cancer (U2OS).
TN3528	Bonducellpin D	Antifection	Microbiology/Virology
	Bonducellpin D may show inhibitory activities on the Para3 virus. It also exhibits moderate activity against four tested human cancer cell lines, HepG-2, K562, HeLa, and Du145.
T81318	R-30-Hydroxygambogic acid
	R-30-Hydroxygambogic acid是从藤黄提取的一种聚戊烯酰黄酮外聚体，对K562/R和K562/S两种人白血病细胞系的IC50分别为2.89 μM和1.27 μM。该化合物适用于癌症研究领域。
TN2192	Scutebarbatine B	Others	Others
	Scutebarbatine B shows weak cytotoxicity with IC50 values ranging from 35.11 to 42.73 μM against K562 cell lines and HL60 cell lines.
TN3760	Danshenol A	Reductase	Endocrinology/Hormones; Metabolism
	Danshenol A has strong aldose reductase (AR) inhibitory activity, has IC50 of 0.10 microM which is comparable to that of epalrestat in clinical use. Danshenol A also has antitumor activity in T-24, QGY, K562, Me180 and BIU87 cell lines, shows inhibited growth of K562 (IC50 = 0.53 μg/mL), T-24 (IC50 = 7.94 μg/mL), QGY (IC50 = 4.65 μg/mL) and Me180 (IC50 = 6.89 μg/mL) cell lines.
TN4215	Hispidanin B	Others	Others
	Hispidanin B shows significant cytotoxicities against tumor cell lines SGC7901, SMMC7721, and K562, with IC50 values of 10.7, 9.8, and 13.7 uM, respectively.
TN4976	Scutebata E	Others	Others
	Scutebata E shows weak cytotoxicity with IC50 values ranging from 35.11 to 42.73 μM against K562 cell lines.
T81232	S-30-Hydroxygambogic acid
	S-30-Hydroxygambogic acid，一聚戊烯酰黄酮外聚体，源自藤黄。针对人白血病细胞系K562/R及K562/S，其IC50值别为4.49 μM与3.61 μM。S-30-Hydroxygambogic acid主用于癌症研究领域。
T80996	Theasaponin E1
	Theasaponin E1，一种可从茶籽分离的茶皂苷，对人肿瘤细胞系K562和HL60展示了抗肿瘤潜能。此外，Theasaponin E1具备醌还原酶(QR)诱导活性，有助于作为抗癌预防药物的研究。
TN1144	Enmein	Antifection; Immunology/Inflammation related	Immunology/Inflammation; Microbiology/Virology
	Enmein 是分离自 I. serra 中，拥有免疫抑制活性。
TN4404	Ladanein	HCV Protease	Microbiology/Virology; Proteases/Proteasome
	Ladanein is a phytochemicals inhibitor that is known to disrupt the interactions of core and other hepatitis C virus (HCV) proteins.Ladanein possesses free radicals DPPH and ABTS +.scavenging activity, it also displays moderate (20-40 microM) activities against K562, K562R (imatinib-resistant), and 697 human leukemia cell lines.
T38243	Hygrolidin
	Hygrolidin is a macrocyclic lactone originally isolated from S. hygroscopicus. It inhibits proliferation of a variety of cancer cell lines, including DLD-1 colon cancer, LNCaP prostate cancer, and K562 leukemia cells (IC50s = 2.9, 5.2, and 33 ng/ml, respectively). Hygrolidin induces the expression and levels of p21 in DLD-1 cells, but not WI-38 fibroblasts, and leads to cell accumulation in the G1 and S phases without inducing apoptosis. It has antiparasitic activity against T. cruzi, L. donovan...
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...
TN2646	16-Hydroxycleroda-3,13-dien-15,16-olide	Autophagy	Autophagy
	16-Hydroxycleroda-3,13-dien-15,16-olide, and prodigiosin are presented as candidates for autophagy inducers that can trigger cell death in a supplement or alternative medicine for cancer therapy. 16-Hydroxycleroda-3,13-dien-15,16-olide regulates the expre

天然产物

Daunorubicin hydrochloride

Cat.No: T1511

Synonym: Daunomycin HCl,盐酸佐柔比星,盐酸柔红霉素,RP-13057 Hydrochloride,Rubidomycin hydrochloride,Daunorubicin HCl,Daunomycin

Target: Apoptosis, DNA/RNA Synthesis, Topoisomerase, Antibacterial, Antibiotic, Autophagy

2-Desoxy-4-epi-pulchellin

Cat.No: TN2755

Target: Anti-infection

Cat.No: T4S1943

Synonym: 奇壬醇,奇任醇,Kirel

Target: Wnt/beta-catenin

Paris saponin VII

Cat.No: T4085

Synonym: 重楼皂苷 VII,Chonglou Saponin VII,Polyphyllin-VII,Dioscinin,Paris saponin-VII

Target: Apoptosis, BCL, Others, PARP, p38 MAPK, Akt, Caspase, P-gp, Autophagy

Cat.No: T6S1315

Synonym: 千层纸素A,6-Methoxybaicalein,Baicalein 6-methyl ether

Target: Virus Protease, HIF/HIF Prolyl-Hydroxylase, Autophagy

Cat.No: T3398

Synonym: Anhydroicaritin,去水淫羊藿黄素,Cycloicaritin

Target: Apoptosis, JAK, STAT, Autophagy

Cat.No: T2S2215

Target: Apoptosis, Others, Akt

Norglaucine hydrochloride

Cat.No: TN6054

Cat.No: TN5358

Cat.No: TN3528

Target: Antifection

R-30-Hydroxygambogic acid

Cat.No: T81318

Scutebarbatine B

Cat.No: TN2192

Target: Others

Cat.No: TN3760

Target: Reductase

Cat.No: TN4215

Target: Others

Cat.No: TN4976

Target: Others

S-30-Hydroxygambogic acid

Cat.No: T81232

Cat.No: T80996

Cat.No: TN1144

Target: Antifection, Immunology/Inflammation related

Cat.No: TN4404

Target: HCV Protease

Cat.No: T38243

Cat.No: T37008

16-Hydroxycleroda-3,13-dien-15,16-olide

Cat.No: TN2646

Target: Autophagy

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