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25

抑制剂 & 化合物

16

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T6018	Zosuquidar trihydrochloride 唑喹达三盐酸盐,Zosuquidar (LY335979) 3HCl,RS 33295-198 trihydrochloride,RS 33295-198 (D06387) 3HCl,Zosuquidar 3HCl,LY-335979 trihydrochloride	P-gp	Membrane transporter/Ion channel; Neuroscience
	Zosuquidar trihydrochloride (LY-335979 trihydrochloride) 是一种P-糖蛋白抑制剂，Ki 值为 59 nM。
T15578	Indotecan NSC-724998,LMP-400	Topoisomerase	DNA Damage/DNA Repair
	Indotecan (LMP-400) 是一种有效的拓扑异构酶 1 抑制剂，对 P388、HCT116和MCF-7 细胞系的IC50值分别为 300、1200和560 nM。
T9088	Topovale ARC111,ARC 111,ARC-111,Topoval	Topoisomerase	DNA Damage/DNA Repair
	Topovale (ARC111) 是一种有效的拓扑异构酶 I 抑制剂。Topovale 抑制缺氧介导的缺氧诱导因子 1alpha 的积累。 Topovale 对一组癌细胞表现出低 nM 细胞毒性。与 P388 细胞相比，在 CPT 抗性拓扑异构酶 I (TOP1) 缺陷的 P388/CPT45 细胞中，Topovale 细胞毒性和 Topovale 诱导的细胞凋亡减少了 > 100 倍。
T35410	(+)-Goniothalesdiol
	(+)-Goniothalesdiol, isolated from the bark of the Malaysian tree G. borneensis, is a tetrahydrofuran compound known to have significant cytotoxic effects against P388 mouse leukemia cells and pesticidal activities. It has been shown to have promising cytotoxic activity against p388 mouse leukemia cells (ED50 ≥30 μg/ml).
T26180	Sdz 280 446 Sdz 280,446,Sdz 280-446
	Sdz 280 446 is one of the most active cyclopeptolide of many resistance-modifying agents in restoring rhodamine-123 retention within multidrug-resistant P388 cells.
T62002	Topoisomerase I inhibitor 7
	Topoisomerase I inhibitor 7 (Compound 8) 是有效的Topoisomerase I 抑制剂。Topoisomerase I inhibitor 7 显著抑制肿瘤生长（高达 79%）。在接受 P388 淋巴瘤移植的小鼠模型中，Topoisomerase I inhibitor 7延长了小鼠寿命（153%）。
T26413	A 30312 A-30312,A30312
	A 30312 is a fused indole, which overcomes multidrug resistance in P388/Adr cells in vitro. It potentiates the cytotoxicity of the antitumor drugs Adriamycin, vincristine and vinblastine in multidrug-resistant cells with no effect on drug-sensitive parent P388 cells.
T34645	Simetride
	Simetride is used in the Reversal of resistance to vincristine in P388 leukemia.
T68865	Amoorastatin
	Amoorastatin is a natural product that has been studied in cancer research. Its derivative was found to significantly inhibit growth of the murine P388 lymphocytic leukemia cell lines.
T68184	Saquayamycin B
	Saquayamycin B is a glycoside of aquayamycin that acts on Gram-positive bacteria and inhibits the growth of adriamycin-sensitive and adriamycin-resistant P388 leukemia cells.
T28311	PD 116152 PD116,152,PD 116,152,PD116152,PD-116,152,PD-116152
	PD 116152 is a highly substituted phenazine with antitumor activity isolated from the culture broth of a Streptomyces sp. The antitumor activity versus murine P388 leukemia is T/C 149. PD 116152 is selectively active versus the bacterium Streptococcus pne
T33510	MS-073 CP162398,CP-162398,CP 162398,MS 073
	MS-073 (CP-162398) is a P-glycoprotein inhibitor (P-gp). The in vitro resistance to vincristine (VCR) was almost completely reversed in VCR-resistant P388 cells, and the resistance of VCR, adriamycin (ADM), etoposide, and actinomycin D in ADM-resistant hu
T37542	Anguinomycin A
	Anguinomycin A is an antibiotic first isolated from a Streptomyces sp. and analog of leptomycin B that is highly cytotoxic to mouse P388 leukemia cells in vitro (IC50 = 0.1-0.2 ng/ml). It also demonstrates antitumor activity at 62.5 μg/kg/day against Lewis lung carcinoma in mice.
T36693	FD-211
	FD-211 is a δ lactone originally isolated from M. lutea with anticancer activity.1 It is cytotoxic to adriamycin-susceptible P388, T-24, HeLa, A549, and HL-60 cancer cells (IC50s = 4, 0.5, 1, 1, and 0.2 μg/ml, respectively), as well as adriamycin-resistant HL-60/ADR cells (IC50 = 0.1 μg/ml). FD-211 also inhibits DNA, RNA, and protein synthesis in HeLa cells (IC50 = 1.25 μg/ml for all). \|1. Nozawa, O., Okazaki, T., Sakai, N., et al. A novel bioactive δ lactone FD-211. Taxonomy, isolation and char...
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).
T38152	Gilvocarcin M
	Gilvocarcin M is an antibiotic originally isolated from S. gilvotanareus. It is active against S. aureus when used at a concentration of 32 μg/ml. Gilvocarcin M inhibits growth of KB cells (IC50 = 0.52 μg/ml) but has no effect on survival in a P388 mouse model of leukemia when used at doses ranging from 25 to 400 mg/kg. Gilvocarcin M intercalates into bacteriophage PM2 DNA. It is toxic to rats with an intravenous LD50 value of 450 mg/kg.
T36397	TAN 420E
	TAN 420E is a bacterial metabolite originally isolated from Streptomyces. It scavenges 2,2-diphenyl-1-picrylhydrazyl radicals in a cell-free assay (IC50 = 1.3 μM) and reduces thiobarbituric acid reactive substances (TBARS) in rat liver microsomes by 72% when used at a concentration of 100 μg/ml. TAN 420E is active against B. brevis, B. cereus, M. flavus, and S. aureus (MICs = 50-100 μg/ml). It is cytotoxic to P388 and KB lymphocytic leukemia cells (EC50s = 0.022 and 0.3 μg/ml, respectively).
T35616	Migrastatin
	Migrastatin is a bacterial metabolite that has been found inStreptomyceswith antimuscarinic and anticancer activities.1,2It binds to M1-5muscarinic acetylcholine receptors (Kis = >200, 200, 31, 43, and >200 μM, respectively) and inhibits calcium mobilization induced by carbamoylcholine in SK-N-SH cells (IC50= 28 μM), as well as in primary rat bladder smooth muscle cells.1Migrastatin inhibits the migration of EC17 esophageal cancer cells in a wound healing assay (IC50= 10 μg/ml) and 4T1 mouse mam...
T35439	(E)-5-(2-Bromovinyl)uracil
	(E)-5-(2-Bromovinyl)uracil (BVU) is a pyrimidine base and an inactive metabolite of the antiviral agents sorivudine and (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU) that may be regenerated to BVDU in vivo. BVU irreversibly inactivates dihydropyrimidine dehydrogenase (DPD) in an NADPH-dependent manner. It enhances the efficacy of the chemotherapeutic agent and DPD substrate 5-fluorouracil in a P388 murine leukemia model when administered at a dose of 200 μmol/kg, increasing survival time.
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...
T37594	Pericosine A
	Pericosine A is a fungal metabolite that has been found inP. byssoidesand has anticancer activity.1It inhibits the growth of a variety of cancer cells, including breast, colon, lung, ovary, stomach, and prostate cell lines (GI50s = 0.05-24.55 μM) and increases survival in a P388 mouse xenograft model when administered at a dose of 25 mg/kg. Pericosine A inhibits EGFR by 40 to 70% when used at a concentration of 100 μg/ml. It also reacts with organosulfur compounds in skunk spray to form stable t...
T70856	3-Oxobetulin Acetate
	3-Oxobetulin acetate is a derivative of the cholesterol biosynthesis inhibitor betulin. It inhibits the growth of P388 murine lymphocytic leukemia cells (EC50 = 0.12 µg/ml), as well as human MCF-7 breast, SF-268 CNS, H460 lung, and KM20L2 colon cancer cells (GI50s = 8, 10.6, 5.2, and 12.7 µg/ml, respectively), but not BxPC-3 pancreas or DU145 prostate cancer cells (GI50s = >10 µg/ml for both). 3-Oxobetulin acetate inhibits replication of X4 tropic recombinant HIV (NL4.3-Ren) in MT-2 lymphoblasto...
T36745	cDPCP
	cDPCP is a platinum-containing DNA-crosslinking agent.1Unlike cisplatin or oxaliplatin , cDPCP forms monofunctional DNA adducts. It is transported into cells by organic cation transporter 1 (OCT1) and OCT2, inhibiting proliferation of MDCK cells expressing the human transporters with IC50values of 8.1 and 1.5 μM, respectively. cDPCP inhibits RNA polymerase II-mediated transcription in a reporter assay using HeLa cells. It increases survival in murine S180 sarcoma and P388 leukemia models when ad...
T36096	Thiocoraline
	Thiocoraline is a depsipeptide and DNAbis-intercalator originally isolated fromMicromonosporawith antibacterial and anticancer activities.1,2It is active against the Gram-positive bacteriaS. aureus,B. subtilis, andM. luteus(MICs = 0.05, 0.05, and 0.03 μg/ml, respectively) but not Gram-negativeE. coli,K. pneumoniae, orP. aeruginosa(MICs = >100 μg/ml for all).1Thiocoraline inhibits RNA and DNA polymerase and thymidylate synthase (IC50s = 6, 6, and 15 μg/ml, respectively), as well as RNA and DNA sy...
T36330	Terrecyclic Acid
	Terrecyclic acid is a sesquiterpene originally isolated from A. terreus with antibiotic and anticancer activity. It is active against S. aureus, B. subtilis, and M. roseus (MICs = 25, 50, and 25 μg/ml, respectively). Terrecyclic acid induces a heat shock response, increases levels of reactive oxygen species (ROS), and inhibits NF-κB activity and cell growth in 3T3-Y9-B12 cells. In vivo, terrecyclic acid (0.1, 1, and 10 mg/ml) reduces the number of ascitic fluid tumor cells in a mouse model of P3...

化合物

Zosuquidar trihydrochloride

Cat.No: T6018

Synonym: 唑喹达三盐酸盐,Zosuquidar (LY335979) 3HCl,RS 33295-198 trihydrochloride,RS 33295-198 (D06387) 3HCl,Zosuquidar 3HCl,LY-335979 trihydrochloride

Target: P-gp

Cat.No: T15578

Synonym: NSC-724998,LMP-400

Target: Topoisomerase

Cat.No: T9088

Synonym: ARC111,ARC 111,ARC-111,Topoval

Target: Topoisomerase

(+)-Goniothalesdiol

Cat.No: T35410

Cat.No: T26180

Synonym: Sdz 280,446,Sdz 280-446

Topoisomerase I inhibitor 7

Cat.No: T62002

Cat.No: T26413

Synonym: A-30312,A30312

Cat.No: T34645

Cat.No: T68865

Cat.No: T68184

Cat.No: T28311

Synonym: PD116,152,PD 116,152,PD116152,PD-116,152,PD-116152

Cat.No: T33510

Synonym: CP162398,CP-162398,CP 162398,MS 073

Cat.No: T37542

Cat.No: T36693

Cat.No: T36181

Cat.No: T38152

Cat.No: T36397

Cat.No: T35616

(E)-5-(2-Bromovinyl)uracil

Cat.No: T35439

7-oxo Staurosporine

Cat.No: T35423

Cat.No: T37594

3-Oxobetulin Acetate

Cat.No: T70856

Cat.No: T36745

Cat.No: T36096

Terrecyclic Acid

Cat.No: T36330

Cat. No.	Product Name	Target	Signaling Pathways
T37341	N-Acetyltyramine	Antibacterial	Microbiology/Virology
	N-Acetyltyramine 是一种群体感应抑制剂，由溶藻弧菌 M3-10 产生。N-Acetyltyramine 可以抑制C. violaceumATCC 12472 的群体感应。它可以逆转阿霉素耐药白血病 P388 细胞的耐药性。
T1032	Erythromycin 红霉素,E-Mycin	ribosome; Antibacterial; Antibiotic	Microbiology/Virology
	Erythromycin (E-Mycin) 是由放线菌产生的大环内酯类抗生素。它结合细菌的 50S 核糖体亚基，通过阻断转肽和易位反应来抑制 RNA 依赖性蛋白的合成。
T0132	Etoposide VP-16,依托泊苷,依托泊甙,VP-16-213	Apoptosis; Mitophagy; Topoisomerase; Antibacterial; Antibiotic; Autophagy	Apoptosis; Autophagy; DNA Damage/DNA Repair; Microbiology/Virology
	Etoposide (VP-16-213) 是一种拓扑异构酶 II 的抑制剂，通过与拓扑异构酶 II 和 DNA 形成复合物来抑制 DNA 合成 (IC50=60.3 μM)。Etoposide 具有抗肿瘤活性，可以诱导细胞凋亡、自噬。
TQ0213	Bruceantin 鸦胆亭,(-)-Bruceantin,NCI165563,鸦胆停,NSC165563	Others	Others
	Bruceantin (NSC-165563) 提取自痢鸦胆子中，显示出对 B16黑色素瘤，结肠癌38，L1210和白血病 P388的抑制活性。
TN1918	Medicarpin 美迪紫檀素	Apoptosis; BCL; ROS; JNK	Apoptosis; Immunology/Inflammation; MAPK
	Medicarpin 是从紫花苜蓿中分离出的一种类黄酮。它通过调节 P-gp 介导的药物外流，诱导白血病 P388 细胞凋亡并克服多药耐药性。
TN1569	Deoxylapachol	Antifection; Antifungal	Microbiology/Virology
	Deoxylapachol 是新西兰褐藻Landsburgia quercifolia 的主要细胞毒性成分，有抗真菌和抗癌活性。
TN6450	Quasipanaxatriol
	Quasipanaxatriol can greatly enhance the cytotoxicity of the anti-cancer drugs in P388/ADM cells.
TN4798	Piptocarphin A	Others	Others
	Piptocarphin A shows strong cytotoxic activity against mouse lymphoid tumor cell line P388 with the IC(50) value of 0.77 microM.
TMA0896	Kulinone	Others	Others
	Kulinone has cytotoxic effects, with IC50 values of 5.6-21.2 ug/mL, it inhibited (ED(50) 2.5-6.2 microg/mL) the P388 cancer cell line.
T81052	T988C (+)-T988C
	T988C为一种七环ETP（epidithiodioxopiperazine）天然产物，对P388白血病细胞系培养细胞显示出显著的细胞毒性。
TN4799	Piptocarphin F	Others	Others
	Piptocarphin F shows strong cytotoxic activities against mouse lymphoid tumor cell line P388. It also shows cytotoxic activity (IC50 3.87-12.5 umol/L) against the human leukemic cell line HL-60.
TN1838	Kulactone 苦楝萜酮内酯	Antifection	Microbiology/Virology
	Kulactone has cytotoxic effects, with IC50 values of 5.6-21.2ug/mL, it inhibited (ED(50) 2.5-6.2 microg/mL) the P388 cancer cell line.
T36931	Penicillide
	Penicillide is a fungal metabolite originally isolated from Penicillium that has diverse biological activities. It is an inhibitor of calpain 2/m-calpain (IC50 = 7.1 μM) and acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 22.9 μM). It is also an antagonist of oxytocin receptors (IC50 = 67 μM). Penicillide inhibits RNA synthesis in P388 murine leukemia cells.
TN4053	FD-838	Antifection	Microbiology/Virology
	FD-838 shows good antileishmanial and moderate anticancer activities, it can moderately inhibit the growth of cultured P388 and HL-60 cell lines. FD-838 has anti-fungal activity, it can significantly inhibit the growth of two plant fungal pathogens Botryt
T75453	11-epi-Chaetomugilin I
	11-epi-Chaetomugilin I 是一种在Chaetomium globosum 中发现的代谢物。11-epi-Chaetomugilin I 对小鼠 P388 白血病细胞系、人类 HL-60 白血病细胞系、小鼠 L1210 白血病细胞系和人类 KB 表皮样癌细胞系具有显著的细胞毒性活性。
T35483	19,20-Epoxycytochalasin D
	19,20-Epoxycytochalasin D is a fungal metabolite that has been found in the endophytic fungus Nemania sp. UM10M. It is active against the chloroquine-sensitive and -resistant strains of P. falciparum (MIC = 0.4 ng/ml for both) without inducing cytotoxicity in Vero cells. It is cytotoxic to BT-549, LLC-PK11, and P388 cells (IC50s = 7.84, 8.4, and 0.16 &#181M, respectively) but not SK-MEL, KB, or SKOV3 cells up to a concentration of 10 &#181M.

天然产物

N-Acetyltyramine

Cat.No: T37341

Target: Antibacterial

Cat.No: T1032

Synonym: 红霉素,E-Mycin

Target: ribosome, Antibacterial, Antibiotic

Cat.No: T0132

Synonym: VP-16,依托泊苷,依托泊甙,VP-16-213

Target: Apoptosis, Mitophagy, Topoisomerase, Antibacterial, Antibiotic, Autophagy

Cat.No: TQ0213

Synonym: 鸦胆亭,(-)-Bruceantin,NCI165563,鸦胆停,NSC165563

Target: Others

Cat.No: TN1918

Synonym: 美迪紫檀素

Target: Apoptosis, BCL, ROS, JNK

Cat.No: TN1569

Target: Antifection, Antifungal

Quasipanaxatriol

Cat.No: TN6450

Cat.No: TN4798

Target: Others

Cat.No: TMA0896

Target: Others

Cat.No: T81052

Synonym: (+)-T988C

Cat.No: TN4799

Target: Others

Cat.No: TN1838

Synonym: 苦楝萜酮内酯

Target: Antifection

Cat.No: T36931

Cat.No: TN4053

Target: Antifection

11-epi-Chaetomugilin I

Cat.No: T75453

19,20-Epoxycytochalasin D

Cat.No: T35483

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