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Targets Recommended: P-gp

24

抑制剂 & 化合物

17

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

Others Others
(+)-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).
T62002 Topoisomerase I inhibitor 7

Others Others
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%)。
T26180 Sdz 280 446

Sdz 280,446,Sdz 280-446

Others Others
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.
T34645 Simetride

Others Others
Simetride is used in the Reversal of resistance to vincristine in P388 leukemia.
T26413 A 30312

A-30312,A30312

Others Others
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.
T68184 Saquayamycin B

Others Others
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

Others Others
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
T37542 Anguinomycin A

Others Others
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.
T33510 MS-073

CP162398,CP-162398,CP 162398,MS 073

Others Others
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
T35439 (E)-5-(2-Bromovinyl)uracil

Others Others
(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.
T36693 FD-211

Others Others
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...
T38152 Gilvocarcin M

Others Others
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.
T36181 Quinaldopeptin

Others Others
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).
T36397 TAN 420E

Others Others
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

Others Others
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...
T35423 7-oxo Staurosporine

Others Others
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

Others Others
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...
T36745 cDPCP

Others Others
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...
T70856 3-Oxobetulin Acetate

Others Others
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...
T36096 Thiocoraline

Others Others
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

Others Others
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
Indotecan
Cat.No: T15578
Synonym: NSC-724998,LMP-400
Target: Topoisomerase
Topovale
Cat.No: T9088
Synonym: ARC111,ARC 111,ARC-111,Topoval
Target: Topoisomerase
(+)-Goniothalesdiol
Cat.No: T35410
Synonym:
Target: Others
Topoisomerase I inhibitor 7
Cat.No: T62002
Synonym:
Target: Others
Sdz 280 446
Cat.No: T26180
Synonym: Sdz 280,446,Sdz 280-446
Target: Others
Simetride
Cat.No: T34645
Synonym:
Target: Others
A 30312
Cat.No: T26413
Synonym: A-30312,A30312
Target: Others
Saquayamycin B
Cat.No: T68184
Synonym:
Target: Others
PD 116152
Cat.No: T28311
Synonym: PD116,152,PD 116,152,PD116152,PD-116,152,PD-116152
Target: Others
Anguinomycin A
Cat.No: T37542
Synonym:
Target: Others
MS-073
Cat.No: T33510
Synonym: CP162398,CP-162398,CP 162398,MS 073
Target: Others
(E)-5-(2-Bromovinyl)uracil
Cat.No: T35439
Synonym:
Target: Others
FD-211
Cat.No: T36693
Synonym:
Target: Others
Gilvocarcin M
Cat.No: T38152
Synonym:
Target: Others
Quinaldopeptin
Cat.No: T36181
Synonym:
Target: Others
TAN 420E
Cat.No: T36397
Synonym:
Target: Others
Migrastatin
Cat.No: T35616
Synonym:
Target: Others
7-oxo Staurosporine
Cat.No: T35423
Synonym:
Target: Others
Pericosine A
Cat.No: T37594
Synonym:
Target: Others
cDPCP
Cat.No: T36745
Synonym:
Target: Others
3-Oxobetulin Acetate
Cat.No: T70856
Synonym:
Target: Others
Thiocoraline
Cat.No: T36096
Synonym:
Target: Others
Terrecyclic Acid
Cat.No: T36330
Synonym:
Target: Others
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.
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.
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.
T81052 T988C

(+)-T988C

Others Others
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。
T68865 Amoorastatin

Others Others
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.
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.
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.
T75453 11-epi-Chaetomugilin I

Others Others
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。
T36931 Penicillide

Others Others
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
T35483 19,20-Epoxycytochalasin D

Others Others
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
Synonym:
Target: Antibacterial
Erythromycin
Cat.No: T1032
Synonym: 红霉素,E-Mycin
Target: ribosome, Antibacterial, Antibiotic
Etoposide
Cat.No: T0132
Synonym: VP-16,依托泊苷,依托泊甙,VP-16-213
Target: Apoptosis, Mitophagy, Topoisomerase, Antibacterial, Antibiotic, Autophagy
Bruceantin
Cat.No: TQ0213
Synonym: 鸦胆亭,(-)-Bruceantin,NCI165563,鸦胆停,NSC165563
Target: Others
Medicarpin
Cat.No: TN1918
Synonym: 美迪紫檀素
Target: Apoptosis, BCL, ROS, JNK
Deoxylapachol
Cat.No: TN1569
Synonym:
Target: Antifection, Antifungal
Quasipanaxatriol
Cat.No: TN6450
Synonym:
Target:
Kulinone
Cat.No: TMA0896
Synonym:
Target: Others
Piptocarphin A
Cat.No: TN4798
Synonym:
Target: Others
T988C
Cat.No: T81052
Synonym: (+)-T988C
Target: Others
Amoorastatin
Cat.No: T68865
Synonym:
Target: Others
Kulactone
Cat.No: TN1838
Synonym: 苦楝萜酮内酯
Target: Antifection
Piptocarphin F
Cat.No: TN4799
Synonym:
Target: Others
11-epi-Chaetomugilin I
Cat.No: T75453
Synonym:
Target: Others
Penicillide
Cat.No: T36931
Synonym:
Target: Others
FD-838
Cat.No: TN4053
Synonym:
Target: Antifection
19,20-Epoxycytochalasin D
Cat.No: T35483
Synonym:
Target: Others
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