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T3050
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ML-7 hydrochloride
ML-7 HCl,ML-7盐酸盐
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Serine/threonin kinase;
Myosin;
YAP;
PKA;
PKC |
Cell Cycle/Checkpoint;
Chromatin/Epigenetic;
Cytoskeletal Signaling;
Metabolism;
Stem Cells;
Tyrosine Kinase/Adaptors |
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ML-7 hydrochloride (ML-7 HCl) 是一种可渗透细胞的、可逆的、有效的、ATP 竞争性的肌球蛋白轻链激酶(MLCK) 特异性抑制剂，IC50为300 nM。它还抑制平滑肌肌球蛋白轻链激酶、PKA 和 PKC。 |
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T33451
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ML 7
ML7,ML-7
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ML 7 is an inhibitor of myosin light chain kinase that protects cardiac function from ischemia/reperfusion (I/R) injury. |
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T8954
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ML179
ML-179
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Others |
Others |
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ML179 是一种有效的选择性肝受体同源物 1 (LRH1, NR5A2) 反向激动剂，IC50 为 320 nM。 |
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T6010
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Idarubicin hydrochloride
盐酸伊达比星,Idamycin,4-demethoxydaunorubicin (NSC256439, 4-DMDR) HCl,4-Demethoxydaunorubicin hydrochloride,Idarubicin HCl,伊达比星盐酸盐,Zavedos
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Topoisomerase;
Antibacterial;
Autophagy;
Antifungal |
Autophagy;
DNA Damage/DNA Repair;
Microbiology/Virology |
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Idarubicin hydrochloride (Zavedos) 是一种蒽环类抗白血病药物，能抑制细菌和酵母菌生长，还抑制拓扑异构酶 II，干扰 DNA 复制和 RNA 转录。 |
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T36141
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Boscalid
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Mitochondrial Metabolism |
Metabolism |
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Boscalid 是一种广谱羧酰胺类杀菌剂，通过与线粒体复合物 II/琥珀酸脱氢酶的泛醌位点结合来抑制真菌呼吸。 |
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T38915
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Antibacterial agent 32
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Antibacterial agent 32 exhibits potent antimicrobial activity against E. coli strains NCTC 13351, M 50, and 7 MP, with minimum inhibitory concentration (MIC) values of 1 mcg/mL, 2 mcg/mL, and 8 mcg/mL, respectively (WO2013030733A1, example 43). |
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T62240
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Sirt1/2-IN-1
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Sirt1/2-IN-1 (Compound 7) 是一种 SIRT1 和 SIRT2 的抑制剂， 能够作用于 SIRT1 (IC50: 1.81 μg/mL)、SIRT2 (IC50: 2.10 μg/mL) 和 SIRT3 (IC50: 20.5 μg/mL)，并具有α-微管蛋白的超乙酰化活性 (IC50: 32.05 μg/mL)。Sirt1/2-IN-1 表现出显著的抗癌作用。 |
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T80412
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Bactenecin 7
Bac-7
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Bactenecin 7为一种抗菌肽，其对阴沟肠杆菌具有抑制作用（MIC, 25 - 200 μg/ml），同时对铜绿假单胞菌和表皮葡萄球菌的MICs值均小于或等于200 μg/ml。 |
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T67909
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TAK1 inhibitor
compound 13a
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Topoisomerase |
DNA Damage/DNA Repair |
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TAK1 inhibitor 是一种抑制剂，对MCF-7、A549 、DU-145 、MDA MB-231有抑制作用，IC50分别为 0.021、0.14、0.064 、0.19 。化合物13 具有较好的抑菌活性,麦克风范围为93.7 ~ 46.9μg / mL,麦克风范围为7.8 ~ 5.8μg / mL。 |
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T81382
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PROTAC BRD9 Degrader-7
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PROTACs |
PROTAC |
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PROTACBRD9Degrader-7 是具有口服活性的BRD9选择性降解剂，DC50 值为 1.02 nM，表现出较好的口服生物利用度，其Cmax 达到 3436.95 ng/mL。 |
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T78654
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MraY-IN-3 hydrochloride
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MraY-IN-1（compound 12a）是一种针对细菌转位酶MraY的有效抑制剂，具有140 μM的IC50值。其对Escherichia coli K12、Bacillus subtilis W23和Pseudomonas fluorescens Pf-5展现出抗菌活性，相应的MIC50为7 µg/mL、12 µg/mL和46 µg/mL。MraY-IN-1适用于抗菌药物的研究领域。 |
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T36905
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Nanangenine F
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Nanangenine F is a drimane sesquiterpene fungal metabolite that has been found inA. nanangensis.1It is active againstB. subtilis(IC50= 78 μg/ml) and cytotoxic to NS-1, DU145, and MCF-7 cancer and NFF non-cancerous cells (IC50s = 49, 95, 49, and 84 μg/ml, respectively).
1.Lacey, H.J., Gilchrist, C.L.M., Crombie, A., et al.Nanangenines: Drimane sesquiterpenoids as the dominant metabolite cohort of a novel Australian fungus, Aspergillus nanangensisBeilstein J. Org. Chem.152631-2643(2019) |
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T38916
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Antibacterial agent 51
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Antibacterial agent 51 (example 45) is a potent antibacterial compound effective against E. coli strains NCTC 13351, M 50, and 7 MP, with MIC values of 4, 8, and 8 mcg/mL, respectively (WO2013030733A1). |
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T37536
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Carbazomycin A
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Carbazomycin A is a bacterial metabolite that has been found in Streptomyces and has diverse biological activities.1,2It is active againstS. aureus,T. asteroides, andT. mentagrophytes(MIC = 12.5 μg/ml for all), as well as the plant pathogenic fungusP. oryzae(MIC = 25 μg/ml). Carbazomycin A is cytotoxic to MCF-7, KB, NCI H187, and Vero cells (IC50s = 26.2, 30.1, 18.4, and 32.6 μg/ml, respectively).2
1.Sakano, K.-I., Ishimaru, K., and Nakamura, S.New antibiotics, carbazomycins A and B. I. Fermenta... |
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T35912
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Pyrocoll
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Pyrocoll is a bacterial metabolite originally isolated from Streptomyces. It inhibits the growth of A. aurescens, A. globiformis, A. oxydans, A. pascens, and R. erythropolis bacteria (MICs = 10, 1, 10, 3, and 10 μg/ml, respectively) and HMO2, HepG2, and MCF-7 cancer cells (GI50s = 0.28, 0.42, and 2.2 μg/ml, respectively) in vitro. Pyrocoll is also active against P. falciparum and T. rhodesiense (IC50s = 1.19 and 1.97 μg/ml, respectively). |
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T64172
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MraY-IN-1
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MraY-IN-1 (compound 12a) 是细菌转位酶 MraY 的有效抑制剂 (IC50: 140 μM)。MraY-IN-1 对大肠杆菌 K12 (MIC50: 7 μg/ml)、枯草芽孢杆菌 W23 (MIC50: 12 μg/ml) 和荧光假单胞杆菌 Pf-5 (MIC50: 46 μg/ml) 具有抗菌作用。MraY-IN-1 能够用于抗菌的研究。 |
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T37537
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Carbazomycin D
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Carbazomycin D is a bacterial metabolite that has been found inStreptomycesand has diverse biological activities.1,2It is active against the fungiT. asteroidesandT. mentagrophytes(MIC = 100 μg/ml for both) and the bacteriumM. tuberculosis(IC50= 25 μg/ml). Carbazomycin D is cytotoxic to MCF-7, KB, NCI H187, and Vero cells (IC50s = 21.3, 33.2, 12.9, and 34.3 μg/ml, respectively).2
1.Naid, T., Kitahara, T., Kaneda, M., et al.Carbazomycins C, D, E and F, minor components of the carbazomycin complexJ... |
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T27970
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Mabuterol free base
Mabuterol,PB 868Cl
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Others |
Others |
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Mabuterol is a selective agonist of β2 adrenoreceptor with no beta 1-stimulation. Mabuterol inhibited the positive inotropic effect of isoprenaline at 10(-7) g/ml and decreased the maximum driving frequency at 3 X 10(-6) g/ml. Mabuterol was 3 times more p |
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T78673
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Antibacterial agent 135
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Antibacterialagent 135（示例7）是一种针对多种细菌具有抑制作用的有效抗菌剂，包括铜绿假单胞菌、鲍曼不动杆菌、大肠杆菌和肺炎克雷伯菌，其最小抑菌浓度（MIC）大于64 μg/mL。 |
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T61308
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Antifungal agent 27
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Antifungal agent 27 (compound 7) is a chemical compound possessing antifungal properties. It exhibits moderate antibacterial activity and weak antifungal activity against MRSA and C. albicans SS5314, with minimal inhibitory concentration (MIC) values of 8 and 32 μg/mL, respectively [1]. |
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T35423
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7-oxo Staurosporine
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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... |
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T38917
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Antibacterial agent 50
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Antibacterial agent 50 (example 47) is a compound that exhibits antibacterial activity. It shows minimum inhibitory concentration (MIC) values of 32, 64, and 128 mcg/mL against three strains of E. coli, namely NCTC 13351, M 50, and 7 MP, respectively (WO2013030733A1). |
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T64160
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MraY-IN-3
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MraY-IN-3 (12a) 是一种细菌转位酶 MraY 的有效抑制剂 (IC50: 140 μM)。MraY-IN-3 能够作用于 E. coli K12 (MIC: 7 μg/ml)、B. subtilis W23 (MIC: 32 μg/ml)、P. fluorescens Pf-5 (MIC: 46 μg/ml)。 |
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T74953
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Antimicrobial agent-7
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Antimicrobial agent-7 (Compound 12) 为一化合物，对革兰氏阴性及革兰氏阳性菌展现出显著的抗菌能力，MIC值介于 2-8 μg/mL 之间。此外，该化合物还对脂多糖引发的炎症有着抗炎作用。 |
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T60414
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Antibacterial agent 73
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Antibacterial agent 73（化合物 7a）具有抗结核、抗菌和抗真菌活性。 Antibacterial agent 73 具有良好的抗结核活性，对 Mtb H37Rv 的 MIC 为 0.65 μg/mL。 Antibacterial agent 73在 MCF-7 乳腺癌细胞系中也表现出细胞毒性，IC 50 为 8.20 μM [1]。 |
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T68667
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Oxanosine
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Oxanosine is an analog of guanosine that has been found in S. capreolus and has diverse biological activities, including antibacterial, antiviral, and anticancer properties. It is active against a variety of bacteria, including S. flexneri, P. mirabilis, and E. coli (MICs = 6.25, 12.5, 25 µg/ml, respectively, on peptone, but not nutrient, agar). Oxanosine inhibits replication of the HIV-1 strain IIIb in infected CEM and U937, but not H9, cells (EC50s = 7, 27, and >500 µg/ml, respectively). It al... |
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T70856
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3-Oxobetulin Acetate
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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... |
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T36409
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Roccellic Acid
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Roccellic acid is a lichen secondary metabolite that has been found in R. montagnei and has antibacterial and anticancer activities.1,2 It is active against the bacteria S. gordonii and P. gingivalis (MIC = 46.9 μg/ml for both).1 Roccellic acid (100 μg/ml) inhibits proliferation of MDA-MB-231, MCF-7, and DLD-1 cancer cells by 65.3, 75.8, and 87.9%, respectively.2
|1. Sweidan, A., Chollet-Krugler, M., Sauvager, A., et al. Antibacterial activities of natural lichen compounds against Streptococcus ... |
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T35437
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(-)-Viriditoxin
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(-)-Viriditoxin is a mycotoxin originally isolated from A. viridinutans that has antibacterial and antiproliferative activity. It is active against methicillin-sensitive and -resistant S. aureus (MSSA and MRSA, respectively), tetracycline-sensitive and -resistant Staphylococcus, vancomycin-sensitive and -resistant Enterococcus, and penicillin-sensitive and -resistant S. pneumoniae (MICs = 2-32 μg/ml). (-)-Viriditoxin is also active against fish pathogens, including S. iniae and S. parauberis (MI... |
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T37330
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Pyridindolol
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Pyrindolol is a bacterial metabolite that has been found inS. alboverticillatus.1It inhibits neutral β-galactosidase by 50% under acidic, but not neutral, conditions when used at a concentration of 2 μg/ml. It is selective for β-galactosidase isolated from bovine liver over β-galactosidases isolated from human, bovine, pig, and rat tissues and sialidases isolated fromC. perfringens,Streptomyces, and the H3N2 strain of influenza virus (IC50s = >250 μg/ml for all).1,2
1.Aoyagi, T., Kumagai, M., Ha... |
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T37553
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(-)-Mycousnine
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(-)-Mycousnine is a microbial metabolite and derivative of usnic acid originally isolated fromM. nawaethat has antibacterial and antifungal activities.1,2It is active against the Gram-positive bacteriaB. subtilis,K. rhizophila, andS. aureus(MICs = 4, 8, and 4 g/ml, respectively) but not the Gram-negative bacteriaE. coli,S. typhimurium, andK. pneumoniae(MICs = >128 g/ml for all).2(-)-Mycousnine is also active against the fungiT. mentagrophytes,T. rubrum, andC. albicans(MICs = 25, 25, and 100 μg/m... |
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T35902
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Milbemycin A4 oxime
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Milbemycin A4 oxime is a derivative of milbemycin A4 and a component of milbemycin oxime , compounds that both have insecticidal and nematocidal activity. Milbemycin A4 oxime (0.05 mg/kg) reduces the number of microfilariae of the heartworm D. immitis in naturally infested dogs. It inhibits the growth of clinical isolates of C. glabrata with MIC80 values ranging from 16 to greater than 32 μg/ml. Milbemycin A4 oxime (2.5 μg/ml) blocks efflux of fluconazole from a clinical isolate of C. glabrata, ... |
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T37887
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1-Heptadecanoyl-rac-glycerol
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1-Heptadecanoyl-rac-glycerol is a monoacylglycerol that contains heptadecanoic acid at the sn-1 position. It is active against the bacteria E. aerogens, E. cloacae, P. mirabilis, and S. faecalis (MIC = 78 μg/ml for all).1 1-Heptadecanoyl-rac-glycerol has been found in T. africana, I. sonorae, and wheat bran.1,2,3
|1. Kuete, V., Metuno, R., Ngameni, B., et al. Antimicrobial activity of the methanolic extracts and compounds from Treculia africana and Treculia acuminata (Moraceae). S. Afr. J. Bot. ... |
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T36844
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Inostamycin A
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Inostamycin A is a bacterial metabolite that has been found inStreptomycesand has anticancer activity.1It is an inhibitor of CDP-diacylglycerol:inositol 3-phosphatidyltransferase (IC50= 0.02 μg/ml in A431 cell membranes) and is selective for CDP-diacylglycerol:inositol 3-phosphatidyltransferase over phospholipase C (PLC) and phosphatidylinositol kinase at 10 μg/ml.2Inostamycin A decreases viability of YCU-T892, KCC-TC873, KB, HSC-4, and YCU-T891 oral squamous cell carcinoma (OSCC) cells in a con... |
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T37413
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Calcitonin (salmon) (trifluoroacetate salt)
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Calcitonin is a peptide hormone that lowers blood calcium level and inhibits bone resorption. It belongs to the calcitonin family of peptides, which also includes amylin , calcitonin gene-related peptide , and adrenomedullin. The binding of salmon calcitonin to the human calcitonin receptor (CTR) is not modulated by receptor activity-modifying proteins (RAMPs), which influence affinity of human calcitonin to CTR. Salmon calcitonin binds to human CTR2 with IC50 values of 0.933, 0.224, 0.134, and ... |
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T37594
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Pericosine A
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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... |
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T35451
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β-Defensin-2 (human) (trifluoroacetate salt)
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β-Defensin-2 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts.1It inhibits the growth of periodontopathogenic and cariogenic bacteria, includingP. gingivalisandS. salivarius.2β-Defensin-2 (30 μg/ml) stimulates gene expression and production of IL-6, IL-10, CXCL10, CCL2, MIP-3α, and RANTES by keratinocytes.3It also stimulates calcium mobilization, migration, and proliferation of keratinocytes whe... |
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T36296
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BIO5192 hydrate
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BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels[1][2].
The combination of BIO5192 hydrate (1 mg/kg; i.v.) and Plerixafor (5 mg/kg; s.c.) exert an additive effect on progenitor mobilization[1].BIO5192 hydrate (30 mg/kg; s.c; bid; during days... |
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T36978
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AS-99 TFA
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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... |
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T35683
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2-deoxy-D-Glucose-13C6
2-deoxy-D-Glucose-13C6
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2-deoxy-D-Glucose-13C6is intended for use as an internal standard for the quantification of 2-deoxy-D-glucose by GC- or LC-MS. 2-deoxy-D-Glucose is a glucose antimetabolite and an inhibitor of glycolysis.1,2It inhibits hexokinase, the enzyme that converts glucose to glucose-6-phosphate, as well as phosphoglucose isomerase, the enzyme that converts glucose-6-phosphate to fructose-6-phosphate.32-deoxy-D-Glucose (16 mM) induces apoptosis in SK-BR-3 cells, as well as inhibits the growth of 143B oste... |
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T35426
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β-Defensin-1 (human) (trifluoroacetate salt)
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β-Defensin-1 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts.1It inhibits the growth ofB. adolescentis,L. acidophilus,B. breve,B. vulgatus,L. fermentum,B. longum, andS. thermophilusin an antimicrobial radial diffusion assay.2β-Defensin-1 also inhibits the growth of periodontopathogenic and cariogenic bacteria, includingP. gingivalisandS. salivarius, and of susceptibleM. tuberculosisH37Rv but no... |
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T35527
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PI3Kα-IN-4
PI3Kα-IN-4
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PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα, with an IC50 of 1.8 nM. PI3Kα-IN-4 has antitumor activity[1].
PI3Kα-IN-4 (compound 10) inhibits PI3Kα, β, δ, and γ, with IC50s of 1.8, 271.0, 13.9, and 13.8 nM, respectively in kinase assays[1].PI3Kα-IN-4 inhibits PI3Kα, β, δ, and γ, with IC50s of 12.1,1393, 183, and >10000 nM, respectively in cell based assays[1].
PI3Kα-IN-4 (compound 10) (30 mg/kg; p.o. once daily for 21 d) achieves the best efficacy, which could inhibit t... |
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