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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T11696 |
Ivachtin
Caspase-3 Inhibitor VII |
Caspase | Apoptosis; Proteases/Proteasome |
Ivachtin (Caspase-3 Inhibitor VII) 是一种非肽,非竞争性和可逆的caspase-3抑制剂,IC50为 23 nM。它是其余胱天蛋白酶的适度抑制剂。 | |||
T6139 |
A-674563
A674563 |
ERK; GSK-3; Akt; PKA; CDK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors |
A-674563 是一种口服有效,选择性的Akt1抑制剂,Ki=11 nM。 | |||
T11381 |
Pictilisib dimethanesulfonate
GDC-0941 dimethanesulfonate,GDC-0941 2 MeSO3H salt |
Apoptosis; DNA-PK; PI3K; mTOR; Autophagy | Apoptosis; Autophagy; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
Pictilisib dimethanesulfonate (GDC-0941 2 MeSO3H salt) 是一种 PI3Kα/δ抑制剂,IC50值为 3 nM。对 p110β 和 p110γ的选择性分别为11倍和25倍。 | |||
T12338 |
OXFBD04
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
OXFBD04 是有效的、选择性的 BRD4 抑制剂(IC50= 166 nM)。OXFBD04 是有效的 BET 溴结构域配体,具有对 CREBBP 溴结构域额外的适度亲和力。OXFBD04 显示出抗癌活性。 | |||
TQ0101 |
MKC3946
|
IRE1 | Cell Cycle/Checkpoint |
MKC3946 是一种有效的可溶性 IRE1α 抑制剂,可在多发性骨髓瘤细胞系中引发适度的生长抑制,可用于癌症研究。 | |||
T6139L |
A-674563 2HCl(552325-73-2(fb-2hcl))
|
ERK; Akt; PKA; CDK; PKC | Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
A-674563 2HCl(552325-73-2(fb-2hcl)) 是一种 Akt1 抑制剂,Ki 为 11 nM,对 PKA 有效,对 Akt1 的选择性比 PKC 高 30 倍以上。 | |||
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。 | |||
T6419 |
BMS-536924
HY-10262,胰岛素样生长因子-1 受体拮抗剂,BMS 536924,CS-0117 |
Apoptosis; FAK; MEK; IGF-1R; Src | Angiogenesis; Apoptosis; Cytoskeletal Signaling; MAPK; Tyrosine Kinase/Adaptors |
BMS-536924 (BMS 536924) 是一种具有口服活性,竞争性和选择性的胰岛素样生长因子受体激酶和胰岛素受体抑制剂,IC50分别为 100 nM 和 73 nM。它具有抗癌活性。 | |||
T6865 |
Quisinostat dihydrochloride
Quisinostat 2HCl,Quisinostat (JNJ-26481585) 2HCl,JNJ26854165(Quisinostat) 2HCl,JNJ-26481585 2HCl |
Apoptosis; HDAC; Autophagy | Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair |
Quisinostat dihydrochloride (JNJ26854165(Quisinostat) 2HCl) 是一种有口服活性,高效的 pan-HDAC 抑制剂,具有广泛的抗肿瘤活性。它对 HDAC1、HDAC2、HDAC4、HDAC10和HDAC11 的IC50值分别为 0.11 nM、0.33 nM、0.64 nM、0.46 nM 和 0.37 nM。 | |||
T11143 |
EB-47
|
PARP | Chromatin/Epigenetic; DNA Damage/DNA Repair |
EB-47 是一种有效的 PARP-1/ARTD-1 选择性抑制剂,IC50 值为 45 nM,对 ARTD5 的IC50 值为 410 nM,表现出温和的药效。EB-47 模拟底物 NAD+,从烟酰胺延伸至腺苷亚区结合。 | |||
T2329 |
Dolutegravir sodium
度鲁特韦钠,GSK1349572,度鲁特韦钠盐,GSK-1349572A |
HIV Protease | Microbiology/Virology; Proteases/Proteasome |
Dolutegravir sodium (GSK-1349572A) 是一种高效、口服的 HIV 整合酶链转移抑制剂,在 HIV-1 整合酶催化的链转移中的 IC50值为 2.7 nM, 抑制 HIV-1 病毒在外周血单个核细胞中的复制,IC50为 0.51 nM。它对 Y143R,N155H 和 G140S/Q148H 突变体也保持高效。 | |||
T15781 |
LP-935509
|
Serine/threonin kinase; AAK1 (AP2 associated kinase 1) | Cell Cycle/Checkpoint; Metabolism; Neuroscience |
LP-935509 是一种选择性的、具有脑渗透的、小分子的衔接蛋白-2 相关激酶1 (AAK1) ATP 竞争性抑制剂,其 IC50=3.3 nM,Ki=0.9 nM。它是一种 BIKE 的有效抑制剂 (IC50=14 nM) 和中度的 GAK 抑制剂 (IC50=320 nM)。它能够逆转 SNL 手术后的疼痛。 | |||
TQ0291 |
Firategrast
SB 683699 |
Integrin | Cytoskeletal Signaling |
Firategrast (SB 683699) 是一种具有口服活性和特异性的α4β1/α4β7整合素拮抗剂。Firategrast 减少淋巴细胞进入中枢神经系统 (CNS) 的运输,降低多发性硬化症 (MS) 的活性。Firategrast 用于复发缓解性多发性硬化症。Firategrast 治疗与中位脑脊液与 CD4,CD8和CD19淋巴细胞计数的适度降低有关。 | |||
T68095 |
Losulazine
|
Dopamine Receptor; Norepinephrine | GPCR/G Protein; Neuroscience |
Losulazine 是一种新型的降压化合物。其确切的作用机制尚未确定,但其降压作用取决于完整的、功能性交感神经系统的存在。 | |||
T6055 |
Quisinostat
奎诺司他,JNJ-26481585 |
Apoptosis; HDAC; Autophagy | Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair |
Quisinostat (JNJ-26481585) 是一种高效的,具有口服活性的 pan-HDAC 抑制剂,对 HDAC1、HDAC2、HDAC4、HDAC10、HDAC11 作用的 IC50值范围为 0.11-0.64 nM。它在成神经细胞瘤中能诱导自噬,具有广泛的抗肿瘤活性。 | |||
T28163 |
NEU-730
|
Others | Others |
NEU-730, a novel inhibitor of TbrPDEB1, shows modest inhibition of T. brucei proliferation. | |||
T26710 |
Azapropazone
DuP-141,NSC-102824,AHR-3018,AHR 3018,MI-85 |
Others | Others |
Azapropazone is anti-inflammatory agent. Azapropazone has uricosuric properties used to treat rheumatoid arthritis and ankylosing spondylitis. Azapropazone lowered plasma uric acid but exerted only a modest and variable uricosuric effect without altering | |||
T32458 |
L 653328
L 653,328,L653328,L653,328,L-653,328,L-653328 |
Others | Others |
L 653328 is an ocular hypotensive agent that has modest beta-receptor blocking activity. | |||
T41065 |
Atrial natriuretic factor (1-28) (human, porcine)
Atrial natriuretic factor (1-28) (human, porcine),Atrial natriuretic peptide (1-28) |
||
Atrial natriuretic factor (1-28) from both human and porcine sources is a powerful suppressor of pro-opiomelanocortin (POMC) mRNA, while it only has a modest inhibition effect on βEP-LI release. | |||
T68409 |
SHP244
|
Others | Others |
SHP244 is an allosteric inhibitor of SHP2 with modest thermal stabilization of the enzyme. | |||
T26580 |
AI-4-57 Hydrochloride
AI457 HCl,AI-4-57 HCl,AI 4 57 HCl |
Others | Others |
AI-4-57 Hydrochloride is a ligand to the CBFß. AI-4-57 Hydrochloride is a modest potency inhibitor of the binding of wildtype CBFß to the RUNX1 Runt domain. | |||
T71231 |
VMY-1-101
|
Others | Others |
VMY-1-101 is a synthesized fluorescent CDK inhibitor. VMY-1-101 demonstrates potent CDK inhibitory activity, enhanced induction of G2/M arrest and modest apoptosis as compared to purvalanol B. | |||
T84739 |
Topoisomerase IIα-IN-8
|
Others | Others |
TopoisomeraseIIα-IN-8 (compound 15),作为人DNA拓扑异构酶IIa (htIIa) 的抑制剂,其IC50值为462 ± 38.0 μM,显示出较弱的抑制效果。 | |||
T32341 |
JWH-251
|
Others | Others |
JWH 251, a cannabimimetic indole, has a high affinity tothe central cannabinoid (CB1) receptor (Ki = 29 nM) and a comparatively modest affinity for the peripheral cannabinoid (CB2) receptor (Ki = 146 nM). JWH 251 can stimulates GTPγS and bind to CB1 and | |||
T61335 |
Rucaparib hydrochloride
|
Others | Others |
Rucaparib hydrochloride, also known as AG014699, is a powerful and orally active compound that inhibits PARP proteins including PARP-1, PARP-2, and PARP-3 with a Ki value of 1.4 nM for PARP1. Additionally, Rucaparib hydrochloride acts as a modest inhibitor of hexose-6-phosphate dehydrogenase (H6PD). This compound shows potential in research for castration-resistant prostate cancer (CRPC) [1] [2] [3] [4]. | |||
T79606 |
CAF-382
|
CDK | Cell Cycle/Checkpoint |
CAF-382(compound B1)为SNS-032类似物,同时兼具CDKL5和泛CDK抑制功能,对GSK3α/β展现出较弱亲和性(>1.8 μM)及抑制效力。该化合物通过抑制CDKL5作用,进而阻止CDKL5 E2结构域发生磷酸化。 | |||
T73842 |
Leriglitazone hydrochloride
|
Others | Others |
Leriglitazone (Hydroxypioglitazone) hydrochloride,吡格列酮的代谢产物。Leriglitazone (Hydroxypioglitazone) hydrochloride 是PPARγ激动剂,通过稳定PPARγ(AF-2) 共激活剂结合表面和增强共激活剂结合能力,提供高转录效力。 Leriglitazone (Hydroxypioglitazone) hydrochloride 与 PPARγC (LBD) 结合,其Ki 值为 1.2 μM,诱导PPARγ(LBD) 转录效率,EC50为 680 nM。 | |||
T81772 |
MOG (92–106), mouse, rat
|
||
MOG (92–106), mouse, rat 是一种来自小鼠/大鼠髓磷脂少突胶质细胞糖蛋白的生物活性肽,包含氨基酸片段92至106。在MOG (92–106) 诱导的实验性自身免疫性脑脊髓炎模型中,小鼠会对次级髓磷脂抗原呈现出广泛的B细胞反应性,尽管T细胞反应较弱。该肽段在SJL小鼠、DA大鼠以及恒河猴中均可诱导严重的脑炎。 | |||
T78135 |
Nicotelline
Nicotellin |
Others | Others |
Nicotelline(Nicotellin)是一种与尼古丁相关的生物碱,作为人类cDNA表达的细胞色素P-450 2A6(CYP2A6)的弱抑制剂,不显著抑制该酶介导的香豆素7-羟基化反应,在300 μM浓度下效果更是如此。此外,Nicotelline还被用作烟草烟雾中颗粒物(PM)的示踪剂和生物标记物。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T68351 |
Homodestcardin
|
Others | Others |
Homodestcardin is a cyclic depsipeptide fungal metabolite that has been found in T. roseum and has immunosuppressant activity. It inhibits concanavalin A-induced proliferation of isolated mouse T cells. | |||
TMA1890 |
Icariside F2
淫羊藿次苷F2 |
NF-κB | NF-κB |
Icariside F2 shows modest α-glucosidase inhibitory (4.60±1.74% to 11.97±3.30%) and antioxidant activities. It also displays potent NF-κB inhibitory effects, with the IC50 value of 16.25 ± 2.19 uM. | |||
TN3707 |
Coronarin B
|
Antifection | Microbiology/Virology |
Coronarin B has cytotoxic activity, it also has modest antiplasmodial activity. | |||
TN5134 |
Tetrahydroxysqualene
|
Antifection | Microbiology/Virology |
Tetrahdroxysqualene shows antimycobacterial activity with an MIC of 10.0 microg/mL, while showing only modest cytotoxicity. | |||
TN4835 |
Przewalskin
|
HIV Protease | Microbiology/Virology; Proteases/Proteasome |
Przewalskin A and Przewalskin B showed modest anti-HIV-1 activity with EC50 = 41 and 30 microg/mL, respectively. | |||
T38777 |
Ilexoside O
|
Others | Others |
Ilexoside O, a triterpene saponin derived from Ilex pubescens roots, demonstrates modest inhibition of xanthine oxidase (XOD) activity with an IC50 value of 53.05 μM. | |||
T83481 |
1,1′-Disinomenine
|
||
1,1'-Disinomenine,一种从Sinomenium acutum茎部分离得到的生物碱,对A549和Hela细胞表现出较弱的抑制效果。 | |||
T79960 |
Aloveroside A
|
Others | Others |
Aloveroside A为芦荟乙醇提取物分离得到的三葡萄糖基萘衍生物,其在100 μg/mL的剂量下展现出约18.68%的bACE抑制活性。 | |||
T80778 |
weak Hepatoprotective agent-1
|
||
Weak Hepatoprotective agent-1 (Compound 11),一种从Arctium lappa L. 分离得到的天然产物,在10 μM浓度下具有弱肝保护活性。 | |||
T75461 |
Harzianum A
|
Others | Others |
Harzianum A 是一种单端孢霉烯化合物,可从 Trichoderma harzianum 中分离得到。Harzianum A 对小仓鼠肾细胞没有细胞毒性,对革兰氏阴性和革兰氏阳性细菌没有活性,但在 100 μg/mL 时具有适度的抗真菌活性。 | |||
T75566 |
11-Oxomogroside II A1
|
Others | Others |
11-Oxomogroside II A1(化合物 7)是一种从罗汉果乙醇提取物中分离的氧化葫芦苷,对12-O-十四烷酰基激素-13-乙酸酯(TPA)诱导的Epstein-Barr病毒(EBV)早期抗原(EBV-EA)活化具有抑制效果,并对一氧化氮(NO)供体(+/-)-(E)-甲基-2-[(E)羟基亚氨基]-5-硝基-6-甲氧基-3-己酰胺(NOR 1)的活化也展示出轻微的抑制作用。 |