162
13
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T7537 |
Norgestimate
炔诺肟酯,诺孕酯 |
Progesterone Receptor | Others |
Norgestimate 是一种具有口服活性、高度选择性的孕激素活性和较小雄激素作用的孕激素,是一种合成的孕激素类似物。它可用作口服的避孕药。 | |||
T2324 |
Darunavir
地瑞那韦,达芦那韦,TMC114 |
HIV Protease | Microbiology/Virology; Proteases/Proteasome |
Darunavir (TMC114) 是一种 HIV 蛋白酶抑制剂,用于治疗艾滋病和 HIV 感染。 由于单独使用时会出现抗病毒药物耐药性,因此与其他抗 HIV 药物联合使用。 | |||
T5500 |
DORA-22
|
OX Receptor | GPCR/G Protein; Neuroscience |
DORA-22 是一种双食欲素受体拮抗剂,可改善轻度压力引起的失眠,对记忆的影响很小。 | |||
T13721 |
Homo-PROTAC cereblon degrader 1
|
Others; Ligand for E3 Ligase | Others; PROTAC |
Homo-PROTAC cereblon degrader 1 (compound 15a) 是一种高效 cereblon 降解剂,对 IKZF1 和 IKZF3 的影响很小。 | |||
T11211 |
EP4 receptor antagonist 1
|
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
EP4 receptor antagonist 1 是一种有效的特异性前列腺素 EP4受体拮抗剂,对人和小鼠 EP4受体的 IC50分别为6.1 nM 和16.2 nM。 EP4 receptor antagonist 1 可用于癌症免疫治疗的研究。 | |||
T6187 |
TDZD-8
GSK-3β Inhibitor I,NP 01139 |
GSK-3 | PI3K/Akt/mTOR signaling; Stem Cells |
TDZD-8 (NP 01139) 是抑制GSK-3β的抑制剂,其 IC50=2 μM。它对 Cdk-1/cyclin B,CK-II,PKA 和 PKC 的作用较弱,IC50值均 >100 μM。 | |||
T6029 |
ONX-0914
ONX0914,PR-957,ONX 0914 |
Proteasome; HIV Protease; Antibacterial | Microbiology/Virology; Proteases/Proteasome; Ubiquitination |
ONX-0914 (PR-957) 是选择性的低分子量多肽-7(LMP7)的抑制剂,LMP7 是免疫蛋白酶体的类糜蛋白酶亚单位。它是分枝杆菌蛋白酶体的非竞争性不可逆抑制剂,Ki 值为5.2 μM。它通过 HSF-1 介导的 p-TEFb 活化激活潜伏的 HIV-1。 | |||
TP1760L |
AMARA peptide acetate(163560-19-8 free base)
|
Others | Others |
AMARA peptide acetate(163560-19-8 free base) 是 SIK 和 AMPK 的底物。AMARA 肽是蛋白激酶家族几个成员的底物。它由 AMP 激活的蛋白激酶 (AMPK) 的磷酸化位点组成。 | |||
T61518 |
TAK-653
|
iGluR | Membrane transporter/Ion channel; Neuroscience |
TAK-653是一种选择性AMPA受体正向异构调节剂(PAM),表现出极低的激动剂活性,在大鼠模型中引发类抗抑郁反应,同时保持良好的安全性。 | |||
T73040 |
CYP1B1-IN-4
|
P450 | Metabolism |
CYP1B1-IN-4为选择性CYP1B1抑制剂(IC50=0.2 nM),属2,4-二芳基噻唑类化合物。其对细胞的毒性低,且在人类及大鼠肝微粒体中表现出稳定性。 | |||
T4664 |
ML 297
ML297 |
Potassium Channel | Membrane transporter/Ion channel |
ML 297 是选择性的 GIRK1/2激活剂,EC50为 0.16 μM。ML 297 在癫痫病的研究中具有价值。 | |||
T3465 |
Vesnarinone
维司力农,OPC-8212,Arkin,Piteranometozine |
HIV Protease; PDE | Metabolism; Microbiology/Virology; Proteases/Proteasome |
Vesnarinone (Arkin) 是一种喹啉酮衍生物,可抑制磷酸二酯酶III 活性,增加钙通量和减小钾通量。 | |||
T9698 |
UC2288
|
Mdm2; p53 | Apoptosis |
UC2288 是新型的、细胞通透性、口服有效的p21衰减试剂,基于索拉非尼的结构合成。在不依赖 于p53的情况下,它可以下调 p21 mRNA 的表达,降低 p21 蛋白水平,对 p21 蛋白的稳定性影响很小。它对VEGFR2 和 Raf 激酶没有抑制作用,即使在 10 μM。 | |||
T2534 |
Pitavastatin calcium
P-872441,nisvastatin,itavastatin,Pitavastatin hemicalcium,匹伐他汀钙,NK-104 |
Apoptosis; Mitophagy; Endogenous Metabolite; HMG-CoA Reductase; Autophagy | Apoptosis; Autophagy; Metabolism |
Pitavastatin calcium (NK-104) 是一种羟甲基戊二酰-CoA 还原酶抑制剂。它在 HepG2 细胞中抑制乙酸合成胆固醇的IC50为 5.8 nM。它是高效的肝细胞低密度脂蛋白胆固醇受体诱导剂。具有抗癌活性。 | |||
T17197 |
UCL 2077
|
||
UCL 2077 是癫痫相关 KCNQ 通道的亚型选择性阻滞剂,也是一种选择性慢后超极化通道阻滞剂,在培养的海马神经元中 IC50 为 500 nM,对 Ca2+ 通道、动作电位、输入电阻的影响小 ,以及超极化后的介质。 | |||
T15576 |
Indibulin
2-(1-(4-氯苄基)-1H-吲哚-3-基)-2-氧代-N-(吡啶-4-基)乙酰胺,ZIO 301,D 24851 |
Apoptosis; Microtubule Associated | Apoptosis; Cytoskeletal Signaling |
Indibulin (D 24851) 是一种口服有效的微管蛋白合成抑制剂,具有抗有丝分裂和抗肿瘤活性,且神经毒性小。它降低了肌间神经张力,产生异常的纺锤体,激活有丝分裂检查点蛋白 Mad2 和 BubR1,并诱导有丝分裂停滞和细胞凋亡。 | |||
T32039 |
HADA Hydrochloride
HCC-Amino-D-alanine hydrochloride,HADA HCl |
Autophagy | Autophagy |
HADA Hydrochloride (HCC-Amino-D-alanine hydrochloride) 是一种具有蓝色荧光的D 氨基酸 (λem~450 nm)。FDAAs 在肽聚糖 (PG) 合成位点有效地与多种细菌的 PGs 结合。HADA Hydrochloride 而用于在最小干扰下特异性和共价探测细菌的生长。 | |||
T13102 |
TCMDC-135051
|
Others | Others |
TCMDC-135051 是一种高选择性和有效性的蛋白激酶 PfCLK3 抑制剂,具有低的靶外毒性。TCMDC-135051 可以防止滋养体到裂殖体的转变,破坏转录并减少向蚊子载体的传播。TCMDC-135051 具有抗寄生虫活性 (EC50=320 nM)。 | |||
T15410 |
GNF351
|
Aryl Hydrocarbon Receptor | Immunology/Inflammation |
GNF351 是芳烃受体 (AhR) 的完全拮抗剂,具有抑制 DRE 依赖性和非依赖性活性的能力。它与结合到 AhR 的光亲和性 AhR 配体竞争,IC50为 62 nM。它在小鼠或人角质形成细胞中的毒性极小。 | |||
T21537L |
TMC647055 Choline Hydroxide Salt
TMC647055 Choline Hydroxide Salt (1204416-97-6 free base) |
HCV Protease | Microbiology/Virology; Proteases/Proteasome |
TMC647055 Choline Hydroxide Salt 是一种新型有效的 HCV NS5B 聚合酶非核苷抑制剂,可用于治疗 HCV 感染。它具有纳摩尔级细胞效力(EC(50) 为 82 nM),相关细胞毒性较小(CC(50)>20 μM),在大鼠和狗中具有良好的药代动力学特征。 TMC647055 显示出有体外生化、动力学和病毒学特征的前景。 | |||
T1483 |
Citalopram hydrobromide
Lu 10-171,Nitalapram HBr,Bonitrile HBr,XU-62-320,Lu 10-171 HBr,氢溴酸西酞普兰,Citalopram HBr |
5-HT Receptor; Serotonin Transporter; Autophagy | Autophagy; GPCR/G Protein; Neuroscience |
Citalopram hydrobromide (XU-62-320) 是一种选择性 5-羟色胺再摄取抑制剂,可选择性地抑制 CNS 神经元对 5-羟色胺的再摄取,从而增强中枢神经系统中的 5-羟色胺能活性,也具有抗抑郁活性。它抑制兔血小板中 5-HT 的摄取,IC50为 14 nM。 | |||
T28377 |
PF-06827443
PF6827443,PF 6827443,PF-6827443 |
||
PF-06827443 is a orally bioavailable, CNS-penetrant M1-selective PAM with minimal agonist activity. | |||
T29175 |
YKAs3003
YKAs-3003 |
||
YKAs3003, a potent inhibitor of pathogenic KAS III, displays minimal inhibitory concentration (MIC) values in the range 128-256 microg/mL against various bacteria. | |||
T26395 |
6-Benzylthioinosine
6-BT,6Benzylthioinosine,6-Bn-thioinosine |
||
6-Benzylthioinosine, a broad-spectrum metabolic inhibitor, inhibits glucose uptake, decreases glycolysis and ATP concentration with minimal changes in ROS and mitochondrial respiration. | |||
T39502 |
Lipid 5
|
||
Lipid 5 is an amino lipid compound that demonstrates proficient mRNA delivery in rodent and primate models, displaying favorable pharmacokinetics and minimal toxicity. | |||
T24206 |
JNJ-28330835
JNJ 28330835,JNJ28330835 |
||
JNJ-28330835 is a selective androgen receptor modulator with minimal prostate hypertrophic activity. | |||
T11912 | LY3154207 | Others | Others |
LY3154207 is a subtype selective, potent, and orally available human dopamine D1 receptor positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC50=3 nM). | |||
T38226 |
TSHR antagonist S37b
|
||
TSHR antagonist S37b, the less potent enantiomer of TSHR antagonist S37a, exhibits minimal efficacy in inhibiting the thyrotropin receptor (TSHR). It is utilized in thyroid function research[1]. | |||
T29209 |
ZD4190 HCl
ZD-4190,ZD-4190 HCl,ZD 4190,ZD4190,ZD-4190 hydrochloride |
||
ZD-4190, a potent VEGFR inhibitor, prevents tumour outgrowth in a model of minimal residual carcinoma in deep tissues. | |||
T40658 |
[D-Asn5]-Oxytocin
[D-Asn5]-Oxytocin |
||
[D-Asn5]-Oxytocin exhibits minimal specific oxytocic and vasodepressor effects. Comparative cumulative dose-response investigations reveal that [D-Asn5]-Oxytocin demonstrates a similar intrinsic activity to oxytocin in terms of oxytocic activity. | |||
T11716 |
JH-LPH-33
|
Others | Others |
JH-LPH-33, a sulfonyl piperazine analog, is a potent UDP-2,3-diacylglucosamine pyrophosphate hydrolase LpxH inhibitor. It exhibits remarkable antibiotic activity, reflected by a minimal inhibitory concentration (MIC) value of 0.66 μg/mL. | |||
T61425 |
Tyrosinase-IN-5
|
||
Tyrosinase-IN-5 (compound 16c) is a highly effective inhibitor of tyrosinase, exhibiting an IC50 value of 0.02 μM. This compound efficiently suppresses melanogenesis while posing minimal toxicity to cells [1]. | |||
T62588 | TCMDC-136230 | ||
TCMDC-136230 是一种疟原虫钙动力学的新型抑制剂,但对血红素结晶的抑制作用较小。 | |||
T28852 |
SRI-31040
SRI 31040 |
||
SRI-31040 is a potent DAT allosteric modulator. It partially inhibits DAT uptake without altering DAT-mediated reverse transport and with minimal inhibition of DAT binding. | |||
T38870 |
Antibacterial agent 45
|
||
Antibacterial Agent 45 (AA45) exemplifies a potent antibacterial compound that effectively reduces the minimal inhibitory concentration (MIC) value of Ceftazidime, another antibacterial agent. | |||
T61773 | Keap1-Nrf2-IN-4 | ||
Keap1-Nrf2-IN-4, a powerful neddylation inhibitor, demonstrates significant anti-proliferation activity against MGC-803 cells (IC50 = 2.55 μM), effectively impeding their migration and inducing apoptosis. Additionally, it effectively inhibits tumor growth while exhibiting minimal toxicity [1]. | |||
T73127 | C16-K-cBB1 | ||
C16-K-cBB1 是一种对 MRSA(甲氧西林耐药金黄色葡萄球菌)有效且选择性的抗菌剂,其 MIC 为 1 μg/mL。C16-K-cBB1 具有很好的选择性,由于其溶血活性较弱。在 12.5 μg/mL 浓度下,C16-K-cBB1 能够在 120 分钟内杀死 MRSA 细胞。 | |||
T62440 | TCMDC-125431 | ||
TCMDC-125431 是一种新型的疟原虫钙动力学抑制剂,而对血红素结晶的抑制作用较低。 | |||
T83006 |
Antitumor agent-29
|
||
Antitumor agent-29为新型肝细胞靶向抗肿瘤前体,表现出优异抗肿瘤活性及低毒性副作用。 | |||
T36178 |
Aspalatone
|
||
Aspalatone is an anti-platelet aggregator (IC50 = 180 μM, in vitro) that prolongs bleeding time significantly in a rodent model of thromboembolism. Additionally at a minimal effective dose of 24 mg/kg, aspalatone generates antioxidant and neuroprotective effects against kainic acid-induced epilepsy in rat hippocampus. | |||
TP1760 |
AMARA peptide
|
||
AMARA peptide is a substrate for SIK and AMPK.AMARA peptide is a minimal substrate of several members of the protein kinases family. It consists of the phosphorylation site for AMP-activated Protein Kinase (AMPK). | |||
T68356 | AM-3189 | ||
AM-3189 is a potent and selective GPR40 Agonist with minimal CNS penetration, superior pharmacokinetic properties and in vivo efficacy comparable to AMG 837. AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. Similar to AMG 837, while highly potent on GPR40, AM-3189 was highly selective over the closely related GPCRs, GPR41 and GPR43. 13kdemonstrated low clearance, moderate volume of distribution, and good oral bioavai... | |||
T27614 | INU-152 | ||
INU-152 is a pan-RAF inhibitor. INU-152 has potent anti-tumor activity in preclinical models of BRAFV600E mutant cancer. INU-152 inhibits all RAF isoforms and inhibits MAPK pathways in mutant BRAF cells. INU-152 exhibits minimal paradoxical pathway activa | |||
T39259 |
Arzoxifene
LY353381,Arzoxifene,SERMIII |
||
Arzoxifene (LY353381) is an orally active selective estrogen receptor modulator (SERM) exhibiting a fixed ring structure analogous to raloxifene. This compound demonstrates potent antiestrogenic effects on breast cancer and endometrium while displaying minimal side effects. Additionally, Arzoxifene elicits favorable estrogenic effects on bone health and lipid profile. | |||
T83025 | Antiparasitic agent-19 | ||
Antiparasitic agent-19 (compound 40) 是一种化合物,具备广泛的抗寄生虫活性,且对布氏锥虫、婴儿利什曼原虫和克氏锥虫具有较低的毒性。 | |||
T80444 |
Phlo1b
μ-TrTx-Phlo1b |
Sodium Channel | Membrane transporter/Ion channel |
Phlo1b(μ-TrTx-Phlo1b)为含35个氨基酸残基的肽毒素,特异性抑制Nav1.7通道。相较之下,其对Nav1.2与Nav1.5的抑制作用较弱。 | |||
T39944 |
HSD1590
|
||
HSD1590 is a highly effective and potent inhibitor of ROCK1 and ROCK2, with IC50 values of 1.22 nM and 0.51 nM, respectively. It demonstrates exceptional binding affinity to ROCK, with Kd values below 2 nM. Moreover, HSD1590 showcases minimal cytotoxicity, making it an ideal compound for various applications. | |||
T81744 | mTOR inhibitor-14 | mTOR | PI3K/Akt/mTOR signaling |
mTORinhibitor-14(compound 14c)是一种mTOR高效抑制剂,对CYP2C8的抑制作用较弱,并能有效抑制肿瘤生长。 | |||
T70760 |
NVP018
|
||
NVP018, also known as BC 556, is a potent inhibitor of hepatitis B virus, hepatitis C virus (HCV), and HIV-1 replication, shows minimal inhibition of major drug transporters, and has a high barrier to generation of both HCV and HIV-1 resistance.. | |||
T61169 | PqsR-IN-1 | ||
PqsR-IN-1 (Compound 18) is a potent inhibitor of PqsR, which is a transcriptional regulator involved in the quorum sensing mechanism of Pseudomonas aeruginosa. This compound effectively reduces the production of pyocyanin and exhibits minimal cytotoxicity [1]. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2S0265 |
Robinin
NSC 9222,刺槐素 |
TLR | Immunology/Inflammation |
Flavone glycoside from Robinia with antibacterial and diuretic properties; derived from kaempferol.The ability of robinin to reverse the multidrug resistance of the human colon cancer cell line Colo 320 expreβing MDR1/LRP was explored by monitoring their uptake of Rhodamine 123, but was shown to have minimal effect. Robinin (NSC-9222) was detected in lysates of the human breast cancer cell line MCF-7 using liquid chromatography-tandem maβ spectrometry. | |||
T6194 |
Fidaxomicin
非达米星,Tiacumicin B,OPT-80,Clostomicin B1,PAR-101 |
Apoptosis; DNA/RNA Synthesis; Antibacterial; Antibiotic | Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology |
Fidaxomicin (Tiacumicin B) 是一种大环RNA 聚合酶抑制剂,具有窄谱活性。它选择性地根除致病性艰难梭菌,对构成正常健康肠道菌群的多种细菌影响很小。 | |||
TN4634 |
Neocyclomorusin
|
Antifection | Microbiology/Virology |
Neocyclomorusin displays minimal inhibitory concentration (MIC) value of 4 ug/mL against Klebsiella pneumoniae ATCC11296, Enterobacter cloacae BM47. | |||
TN4788 |
Pierreione B
|
mTOR | PI3K/Akt/mTOR signaling |
Pierreione B is an inhibitor of mTOR signaling with strong anticancer activity. Pierreione A and Pierreione B demonstrate solid tumor selectivity with minimal cytotoxicity. | |||
TN2360 |
Falcarinol
Falcarinol,Panaxynol,人参炔醇 |
HSP | Cytoskeletal Signaling; Metabolism |
Falcarinol, also known as Panaxynol, is a naturally occurring compound that acts as an orally active inhibitor of Hsp90. It effectively targets both the N-terminal and C-terminal regions of Hsp90, displaying high selectivity with minimal toxicities. Furthermore, Falcarinol (Panaxynol) demonstrates the ability to induce apoptosis. | |||
T36990 |
Moenomycin Complex
|
||
Moenomycin complex is a mixture of moenomycins A, A12, C1, C3 and C4, which are antibiotics isolated from several strains of Streptomyces that directly inhibit bacterial peptidoglycan glycosyltransferases. [1] The minimal inhibitory concentration of moenomycin A against various Gram-positive bacteria ranges from 1-100 nM.[1] | |||
TN1852 |
Lancifodilactone F
披针叶五味子二内酯 F |
HIV Protease | Microbiology/Virology; Proteases/Proteasome |
Lancifodilactone F exerts minimal cytotoxicity against C8166 cells (CC50 > 200 microg/mL) and shows anti-HIV activity with EC50 = 20.69 +/- 3.31 microg/mL and a selectivity index > 6.62. | |||
T75570 | Justicidin C | ||
Justicidin C 是一种抗病毒木脂素,对水泡性口炎病毒展现了较强的抗病毒活性,同时在兔肺细胞(RL-33)中显示较低的细胞毒性。 | |||
TN3450 |
Artanin
|
Antifection | Microbiology/Virology |
Artanin displays promising inhibition against both MSSA and MRSA with minimal inhibitory concentrations (MICs) of 8-64 ug/ml, but very weak against Gram-negative pathogen and yeast with MICs of 256 to ≥1024 ug/ml. | |||
T81769 |
Mollicellin I
|
||
Mollicellin I(compound 1)为一种Depsidone类化合物。其对Bre04人乳腺癌细胞系、Lu04人肺癌细胞系以及N04人神经瘤细胞系的生长抑制活性低,GI50s均超过10 μg/mL。 | |||
T78465 |
H-γ-Glu-Gln-OH
γ-Glutamylglutamine,γ-Glu-Gln |
||
H-γ-Glu-Gln-OH 是一种水溶性肽类化合物,用于药物结合。该载体特征为高溶解度、药物负载效能、优良生物相容性、低毒性,并能增强抗癌药物对肿瘤的靶向作用及疗效。 | |||
TN3080 | 5,6,7-Trimethoxycoumarin | P450; Antifection | Metabolism; Microbiology/Virology |
5,6,7-Trimethoxycoumarin shows moderate inhibitory activity against Micrococcus luteus, it also displays an intermediate cytotoxic effects against brine shrimp larvae. 5,6,7-Trimethoxycoumarin can improve gastroprotective effects, and it has low toxicity | |||
TN6674 |
Cyclo-(Pro-Gly)
Cyclo(Pro-Gly) |
||
Cyclo(Pro-Gly) is an active metabolite of piracetam-N-phenylacetyl-L-prolylglycine (GWS-111), it shows a greater resistance to an enzymatic effect than natural neuropeptides. Cyclo-(Gly-Pro) shows cytotoxicity at the concentration of 10 umol/L, it inhibit |