61
6
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T15795 |
Luzindole
N-乙酰-2-苄基色胺,N-0774 |
Melatonin Receptor; MT Receptor | GPCR/G Protein; Neuroscience |
Luzindole (N-0774) 是一种选择性褪黑素受体拮抗剂,可抑制实验性自身免疫性脑脊髓炎,有抗抑郁样活性。它优先靶向 MT2 (Mel1b),对于人 MT2 和 MT1 的 Ki 值分别为 10.2 和 158 nM。 | |||
T24444 |
Medifoxamine
LG 152,Medifoxamina,LG-152,LG152 |
Dopamine Receptor; Monoamine Oxidase | GPCR/G Protein; Neuroscience |
Medifoxamine (LG 152) 是一种选择性非单胺氧化酶抑制剂,通过对5 HT 再摄取的抑制展现其抗抑郁活性。Medifoxamine 优先抑制多巴胺再摄取 (dopamine reuptake)。 | |||
T4627 |
SPI--112Me
|
Others | Others |
SPI--112Me 是 SPI-112 的前药,在无细胞试验中,它优先抑制 Shp2 的 PTPase 活性超过 Shp1 和 PTP1B 20 倍。 | |||
T16699 |
PYZD-4409
|
Others; E1/E2/E3 Enzyme | Others; Ubiquitination |
PYZD-4409 是一种特异性 UBA1 抑制剂,IC50 为 20 μM。 PYZD-4409 在恶性细胞中诱导细胞死亡,并且对恶性细胞的细胞毒性优于对正常造血细胞的细胞毒性。 | |||
T28628 |
RVX-297
RVX297 |
Epigenetic Reader Domain | Chromatin/Epigenetic |
RVX-297 是口服具有活性的,对BD2有选择性的BET 高效抑制剂,作用于BRD2(BD2)、BRD3(BD2)、BRD4(BD2) 的IC50分别为 0.08、0.05、0.02 μM。它能够阻碍多种免疫细胞炎症基因的表达,对临床前模型急性炎症及自身免疫均有效。 | |||
T22921 |
LE 300
|
Dopamine Receptor; 5-HT Receptor | GPCR/G Protein; Neuroscience |
LE 300 是选择性多巴胺 D1 样受体拮抗剂,作用于人多巴胺 D1 和 D5 受体的Kis 分别为 1.9 nM 和 7.5 nM。在大鼠尾动脉实验中,它作用于5-HT2A 受体的pA2 为 8.32。 | |||
T14080 |
AA147
ATF6-activator-147 |
Others | Others |
AA147 (ATF6-activator-147) 是小分子内质网蛋白稳态调节剂,能够选择性激活未折叠蛋白反应的 ATF6臂。 | |||
T11553 |
Heptamidine dimethanesulfonate
SBi4211 dimethanesulfonate |
Others | Others |
Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) 是一种与喷他脒有关的、强效的钙结合蛋白 S100B 的抑制剂 (Kd=6.9 μM),选择性地杀死表达 S100B 的黑素瘤细胞。它是有效的强直性肌营养不良 (DM) 研究工具。 | |||
T9172 |
Simufilam dihydrochloride
PTI-125 dihydrochloride |
Others | Others |
Simufilam dihydrochloride (PTI-125 dihydrochloride) 是口服具有活力的、毒性低的 filamin A 激活剂。它可优先结合改变的 FLNA,并恢复其天然构象,恢复受体和突触活性,并减少其与 a7nAChR/TLR4 的关联和下游病理作用。它可用于研究阿尔茨海默症。 | |||
T6729 |
Lomibuvir
VX-222,VCH-222 |
HCV Protease | Microbiology/Virology; Proteases/Proteasome |
Lomibuvir (VCH-222) (VX-222) 是丙型肝炎病毒 NS5B 聚合酶的一种非核苷变构抑制剂,Kd 值为 17 nM,已证明具有临床疗效。Lomibuvir 抑制 1b/Con1 型 HCV 亚基因组复制子,EC50为 5.2 nM。Lomibuvir 优先抑制延长的 RNA 合成,而非从头合成的 RNA。 | |||
T4687 |
Ro5-3335
CBFβ-Runx1 inhibitor II,Ro 5-3335 |
DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
Ro5-3335 (CBFβ-Runx1 inhibitor II) 是苯二氮化合物,是RUNX1-CBFβ 相互作用抑制剂,可抑制 RUNX1/CBFB 依赖性反式激活,能作为核心结合因子 (CBF) 白血病抑制剂。 | |||
T24260 |
Kelletinin I
|
||
Kelletinin I inhibit preferentially DNA polymerase alpha. | |||
T24798 |
SK-7041
SK 7041 |
||
SK-7041 is an effective HDAC inhibitor that acts by preferentially inhibiting class I HDAC1 and HDAC2. | |||
T70862 |
AMPK Activator SC4
|
||
SC4 is a potent, direct AMPK activator. SC4 preferentially activates α2 complexes and stimulates skeletal muscle glucose uptake. | |||
T69869 |
Cyanabactin
|
||
Cyanabactin is a novel ABA receptor agonist. It preferentially activates Pyrabactin Resistance 1 (PYR1) with low nanomolar potency. | |||
T34492 |
Salinazid
Nilazid,Salicylaldehyde isonicotinoyl hydrazone,Salizid,Salizide,Nupasal,SIH1 |
Others | Others |
Salinazid (Salicylaldehyde isonicotinoyl hydrazone) 是一种有效的抗结核药。 | |||
T41152 |
R-BC154
R-BC154 |
||
R-BC154 is a high affinity fluorescent α4β1/α9β1 inhibitor (Kdvalues are 12.7 and 38 nM, respectively); fluorescent version of BOP. Rapidly and preferentially mobilizes HSCs and progenitorsin vivo. Excitation maximum, 561 nm; emissiosn maximum, 585 nm. | |||
T11038 |
Dibutyryl-cGMP sodium
Bt2cGMP sodium |
Others | Others |
Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analog. Dibutyryl-cGMP sodium preferentially activates cGMP-dependent protein kinase (PKG). Dibutyryl-cGMP sodium inhibits [3H]-arachidonic acid release in human platelets stimulated by gamma | |||
T33487 |
Motexafin gadolinium
PCI0120,Gd texaphyrin,PCI-0120,PCI 0120,Gd-Texgadolinium,API-GP 3 |
||
Motexafin gadolinium, also known as PCI 0120, is a synthetic metallotexaphyrin with radiosensitizing and chemosensitizing properties. Motexafin gadolinium accumulates in tumor cells preferentially due to their increased rates of metabolism, generating rea | |||
T38414 |
NSC 80467
|
||
NSC 80467, a selective DNA damaging agent, functions by inhibiting survivin. Specifically, it preferentially targets DNA synthesis, leading to the induction of two distinct markers of DNA damage, namely γH2AX and pKAP1. | |||
T34393 |
Rostaporfin
SnET2,tin etiopurpurin dichloride,tin ethyl etiopurpurin dichloride,Purlytin,Sn(IV) etiopurpurin |
||
Rostaporfin (also known as REM-001, tin ethyl etiopurpurin, Sn(IV) etiopurpurin, Purlytin, SnET2), is a synthetic purpurin with photosensitizing activity. Rostaporfin preferentially accumulates in tumor cells due to an increased rate of metabolism. Upon e | |||
T68675 |
Porfiromycin
|
||
Porfiromycin is a n N-methyl derivative of the antineoplastic antibiotic mitomycin C isolated from the bacterium Streptomyces ardus and other Streptomyces bacterial species. Bioreduced porfiromycin generates oxygen radicals and alkylates DNA, producing interstrand cross-links and single-strand breaks, thereby inhibiting DNA synthesis. Porfiromycin is preferentially toxic to hypoxic cells. | |||
T13691 |
Etifoxine
HOE 36-801 |
Others | Others |
Etifoxine preferentially acts on β2 or β3 subunit-containing GABAA receptors. GABAA receptor Etifoxine exhibits anxiolytic activity in rodents and humans with no sedative, myorelaxant or mnesic side effects. Etifoxine acts as a ligand of the translocator protein (TSPO); promotes axonal regeneration. Etifoxine(HOE 36-801) is potentiator of GABAA receptor function in cultured neurons. | |||
T35785 |
N-Oleoyl Leucine
|
||
N-Oleoyl leucine is an N-acyl amide generated by PM20D1 that uncouples mitochondrial respiration independent of uncoupling protein 1 (UCP1) in vitro. N-Oleoyl leucine (25 mg/kg, i.p.) decreases body weight and food intake, preferentially decreasing fat mass in a diet-induced obesity mouse model. It improves glucose homeostasis in a fasting glucose tolerance test and increases VO2 while slightly decreasing overall locomotor activity. | |||
T68919 |
Nabumetone Alcohol
|
||
Nabumetone alcohol is the alcohol form of nabumetone, a non-steroidal anti-inflammatory drug (NSAID) that is rapidly metabolized in the liver to a major active metabolite, 6-methoxy-2-naphthyl acetic acid, which inhibits the cyclooxygenase enzyme and preferentially blocks COX-2 activity (which is indirectly responsible for the production of inflammation and pain during arthritis). | |||
TP2016 |
Huwentoxin-IV
Huwentoxin IV |
||
Selective NaV1.7 channel blocker. Preferentially inhibits neuronal NaV1.7, 1.2 and 1.3 (IC50 values are 26, 150 and 338 nM respectively), compared to muscle subtypes NaV1.4 and 1.5 (IC50 = >10 μM). Inhibits the channel by binding at the neurotoxin recepto | |||
T81283 |
RGD-targeted Proapoptotic Peptide
|
||
RGD-targeted Proapoptotic Peptide为一肽类化合物,其C端RGD-4C肽段(ACDCRGDCFC)能够特异性地与肿瘤新生血管的整合素结合位点优先结合。 | |||
TP1504 |
Urocortin III, mouse TFA (357952-10-4 free base)
Urocortin III, mouse TFA |
||
Urocortin III, mouse TFA is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III preferentially binds and activates CRF-R2. Urocortin III (Ucn3) is a known component of the behavioral stress response system. Urocortin III and CRF-R2 in th | |||
T35926 |
Bz-IEGR-pNA (acetate)
|
||
Bz-IEGR-pNA is a colorimetric substrate for Factor Xa.1 Factor Xa preferentially binds to and cleaves the Ile-Glu-Gly-Arg (IEGR) peptide sequence to release p-nitroanilide (pNA), which can be quantified by colorimetric detection at 405 nm as a measure of Factor Xa activity.References1. Aruell, L., Friberger, P., Karlsson, G., et al. A new sensitive and highly specific chromogenic peptide substrate for factor Xa. Thromb. Res. 11(5), 595-609 (1977). Bz-IEGR-pNA is a colorimetric substrate for Fact... | |||
T76183 |
Corazonin
|
||
Corazonin是一种在昆虫体内普遍存在的高度保守神经肽激素,主要调节社会性昆虫的等级身份和行为。它在工蜂和/或其他社会性昆虫的觅食个体中优先表达。 | |||
T63243 | GRP78-IN-2 | ||
GRP78-IN-2 是葡萄糖调节蛋白 78 (GRP78) 抑制剂,能够优先靶向细胞表面 GRP78,具有显著的的抗血管生成和抗癌作用,且不影响其他正常细胞。 | |||
T79579 |
ddUTP
2′,3′-Dideoxyuridine-5′-triphosphate |
Reverse Transcriptase | Microbiology/Virology |
ddUTP (2′,3′-Dideoxyuridine-5′-triphosphate) 作为HIV与AMV逆转录酶的选择性抑制剂,其Ki为0.05 µM及1 µM。ddUTP在dTTP位点掺入生长中的DNA链,从而抑制其进一步的链延伸。 | |||
T37236 |
(±)17(18)-DiHETE
|
||
Eicosapentaenoic acid is an ω-3 fatty acid abundantly available in marine organisms. (±)17(18)-DiHETE is one of the major metabolites produced when eicosapentaenoic acid (EPA) is incubated with various rat tissue homogenates or cynomolgus monkey seminal vesicles. The route of production of (±)17(18)-DiHETE likely proceeds through cytochrome P450-catalyzed epoxidation at the ω-3 double bond followed by conversion to the vicinal diols by epoxide hydrolase. EPA is also metabolized preferentially by... | |||
T75954 |
Mambalgin 1 TFA
|
||
Mambalgin 1 TFA, a selective inhibitor of ASIC1a (with IC50 values of 192 nM for human ASIC1a and 72 nM for the ASIC1a/1b dimer), preferentially binds to the channel in its closed/inactive state. It demonstrates selectivity for ASIC1a over a range of other channels, including ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2, and Kv1.2. In vivo, Mambalgin 1 TFA effectively prolongs the latency of the withdrawal response in mouse tail-flick and paw-flick tests. | |||
T9569 | simufilamum | ||
Simufilam 是一种低毒,口服的 filamin A (FLNA) 激活剂。Simufilam 优先结合大脑中改变的FLNA,恢复其天然构象,恢复受体和突触活性,并减少其与 a7nAChR/TLR4 的关联和下游病理作用。Simufilam 可用于阿尔茨海默症的研究。 | |||
T60767 |
NAAA-IN-1
|
||
NAAA-IN-1 (Compound 1) 可用于炎症和疼痛的研究。NAAA-IN-1 是NAAA 的选择性抑制剂 (IC50 = 7 nM)。NAAA 优先水解内源性生物脂棕榈酰乙醇酰胺 (PEA) 和油酰乙醇酰胺 (OEA),是一种半胱氨酸酰胺酶。 | |||
T61754 | TMX-4116 | ||
TMX-4116为酪蛋白激酶1α (CK1α) 降解剂,具有显著的选择性,尤其是在MOLT4、Jurkat 和 MM.1S 细胞系中,其对CK1α的降解活性强,DC50值低于200 nM。因此,TMX-4116被用于多发性骨髓瘤相关研究。 | |||
T76343 |
α-Conotoxin S IA
|
||
α-Conotoxin SIA 是一种选择性的烟碱型乙酰胆碱受体 (nAChR) 拮抗剂,与肌肉 nAChR 具有高亲和力。α-Conotoxin SIA 在小鼠肌肉中,优先靶向肌肉 nAChR 的 α/δ 界面。而对于TorpedonAChR,α-Conotoxin SIA 对 α/γ 的亲和力比 α/δ 界面高得多。 | |||
T70660 |
Azalanstat HCl
|
||
Azalanstat HCl is an anti-obesity drug acting as a lanosterol 14α-demethylase inhibitor. Azalanstat HCl has been shown to inhibit cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes and hamster liver, by inhibiting the cytochrome P450 enzyme lanosterol 14 alpha-demethylase. When administered orally to hamsters fed regular chow, RS-21607 (50 mg/kg/day) lowered serum cholesterol in a dose-dependent manner (ED50 = 62 mg/kg) in a period of 1 week. It preferentially lowered l... | |||
T83833 |
Rp-2'-Deoxyuridine-5'-O-(1-thiotriphosphate) sodium
Rp-dUTP-α-S |
||
Rp-2'-Deoxyuridine-5'-O-(1-thiotriphosphate) (Rp-dUTP-α-S) 是含硫核苷酸 dUTP-α-S 的同分异构体,也是嘌呤P2Y2受体的激动剂。在表达P2Y2受体的1321N1星形胶质瘤细胞中,该化合物特异性诱导肌醇磷酸积累(EC50 = 12.5 µM),相较于表达P2Y4的1321N1细胞,在10 µM浓度下效果更显著。 | |||
T60635 |
Simufilam hydrochloride
|
||
Simufilam (PTI-125) (hydrochloride) 是一种具有口服活性的细丝蛋白 A (FLNA) 激活剂,具有低毒性,可用于阿尔茨海默病研究。Simufilam (hydrochloride) 优先结合改变的细丝蛋白 A 并恢复其天然构象,恢复受体和突触活性,并减少其与 a7nAChR/TLR4 的关联和下游病理作用。 | |||
T68875 |
Xylocydine
|
||
Xylocydine is a novel Cdk inhibitor, which is an effective inducer of apoptosis in hepatocellular carcinoma cells in vitro and in vivo. Xylocydine also strongly inhibits the activity of Cdk7 and Cdk9, in vitro as well as in cell cultures, that is temporally associated with apoptotic cell death in xylocydine-induced HCC cells. Xylocydine can effectively suppress the growth of HCC xenografts in Balb/C-nude mice by preferentially inducing apoptosis in the xenografts, whereas the drug did not cause... | |||
T76285 |
β-Endorphin (6-31), human
β-EP (6-31), human |
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
β-Endorphin是一种内源性阿片类神经肽,作为opioid receptor激动剂,主要与μ-阿片受体发生作用。该肽在中枢和周围神经系统特定神经元中表达,是人类体内三种内啡肽之一。β-Endorphin在减轻压力、维护生理平衡及调控神经系统的疼痛感知中发挥作用。 | |||
T70661 |
Azalanstat mesylate
|
||
Azalanstat mesylate is an anti-obesity drug acting as a lanosterol 14α-demethylase inhibitor. Azalanstat mesylate has been shown to inhibit cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes and hamster liver, by inhibiting the cytochrome P450 enzyme lanosterol 14 alpha-demethylase. When administered orally to hamsters fed regular chow, RS-21607 (50 mg/kg/day) lowered serum cholesterol in a dose-dependent manner (ED50 = 62 mg/kg) in a period of 1 week. It preferentially... | |||
T75856 |
Huwentoxin-IV TFA
|
||
Huwentoxin-IV TFA是一种具有高效性和选择性的钠通道阻滞剂,能够抑制Nav1.7、Nav1.2、Nav1.3和Nav1.4神经元,其IC50分别为26、150、338和400nM。通过优先结合于神经毒素受体位点4,Huwentoxin-IV TFA特异性地阻断周围神经的Nav1.7亚型。该化合物适用于炎症性及神经性疼痛动物模型的研究。 | |||
T74681 | NecroIr2 | ||
NecroIr2 是一种铱 (III) 复合物,是顺铂 (Cisplatin) 耐药肺癌细胞 (A549R) 的坏死诱导剂。NecroIr2 选择性积累在线粒体中,导致氧化应激和线粒体膜电位 (MMP) 的损失。NecroIr2 能够激活受体相互作用的丝氨酸苏氨酸激酶 3 (RIPK3) 和混合谱系激酶结构域样假激酶 (MLKL),调节CDK4表达。 | |||
T76025 |
Urocortin III, mouse TFA
|
||
Urocortin III, mouse TFA是CRF(促肾上腺皮质激素释放因子)相关的肽。该化合物主要通过结合并激活CRF-R2发挥作用。Urocortin III(Ucn3)是已知参与调节行为压力反应体系的组分之一。它和CRF-R2在大脑杏仁核中共同作用,从而参与调控复杂的社会动力学行为。 | |||
T82508 |
Eciskafusp alfa
|
PD-1/PD-L1 | Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation |
Eciskafusp alfa是一种针对程序性细胞死亡1(PDCD1,亦称PD-1)的顺式靶向IL2v免疫细胞因子。它优先选择抗原特异性干细胞样PD-1+ TCF-1+ CD8+ T细胞,并促使这些细胞分化成更高效的效应器细胞。Eciskafusp alfa主要用于癌症与慢性感染的研究领域。 | |||
T78126 |
Dothiepin
Dosulepin,Dothep |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Dothiepin(Dosulepin; Dothep)是一种具备镇静/抗焦虑作用的抗抑郁药物。该化合物主要通过抑制去甲肾上腺素的再摄取,而非血清素,以增强去肾上腺素能神经传递。同时,Dothiepin作为组胺H1受体的拮抗剂,具备显著的镇痛活性,适用于治疗心因性面部疼痛、特发性纤维肌痛综合征或类风湿关节炎,并且不具有心脏毒性。 | |||
T74634 | MS9427 TFA | ||
MS9427 TFA 是一种有效的 PROTACEGFR 降解剂,对野生型 EGFR 和突变型 EGFRL858R 的 Kd 分别为 7.1 nM 和 4.3 nM。MS9427 TFA 通过泛素/蛋白酶体系统 (UPS) 和自噬/溶酶体途径选择性地降解突变体,但不降解 WTEGFR。MS9427 TFA 对 NSCLC 细胞增殖有较强的抑制作用。MS9427 TFA 可用于抗癌研究。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T8044 |
Ajmalicine
阿吗里新,Lamuran,Delta-Yohimbine,Raubasine,Ajmalicin |
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Ajmalicine (Raubasine) 是一种有效的抗肾上腺素 (adrenolytic) 剂,优先阻断 α1-肾上腺素受体 (α1-adrenoceptor)。Ajmalicine 是一种可逆性但非竞争性尼古丁受体 (nicotine receptor) 完全抑制剂,IC50 为 72.3 μM。Ajmalicine 还可用于降压、蛇毒,具有镇静活性。 | |||
T4000 |
(±)-Equol
Equol,(±)-雌马酚,(R,S)-Equol |
Estrogen Receptor/ERR; Estrogen/progestogen Receptor; Drug Metabolite | Endocrinology/Hormones; Metabolism |
(±)-Equol ((R,S)-Equol) 是 equol 的外消旋体。它对 ERα 和 ERβ 的 EC50s of 分别为 200 和 74 nM。Equol 是大豆异黄酮黄豆苷和大豆黄素的代谢产物。 | |||
T6491 |
(-)-(S)-Equol
(−)-Equol,Equol,4',7-Dihydroxyisoflavan,4',7-Isoflavandiol,雌马酚 |
Estrogen Receptor/ERR; Estrogen/progestogen Receptor; Endogenous Metabolite | Endocrinology/Hormones; Metabolism |
(-)-(S)-Equol (4',7-Dihydroxyisoflavan) 是雌激素受体β的高亲和力配体。 | |||
T13608 |
Chaetoglobosin A
|
Others | Others |
Chaetoglobosin A, the active compound extracted of Penicillium aquamarinium, is a member of the cytochalasan family. It preferentially induces apoptosis. | |||
TN5057 |
Stachybotramide
|
LDL | Metabolism |
Stachybotramide preferentially stimulate the plasma cholesteryl ester transfer protein (CETP)-mediated transfer of cholesteryl esters (CE) from high density lipoprotein (HDL) to both very low density lipoprotein (VLDL) and low density lipoprotein (LDL). | |||
TC0022 |
Desoxypeganine
Deoxypeganine |
AChE | Neuroscience |
Desoxypeganine (Deoxypeganine) 是胆碱酯酶的抑制剂。它优先作用于丁酰胆碱酯酶,作为单胺氧化酶 A 而不是单胺氧化酶 B 的选择性抑制剂。它在酒精滥用的药理学治疗中的潜在用途,以减少酒精滥用者的渴望和抑郁,并且也可能有用作为戒烟辅助。 |