|
T5399
|
GeA-69
|
PARP |
Chromatin/Epigenetic;
DNA Damage/DNA Repair |
|
GeA-69 是一种选择性变构 PARP14 大结构域 2 (MD2) 抑制剂，Kd 值为 2.1 µM。 |
|
T0373
|
Erlotinib
OSI-744,NSC 718781,CP358774,埃罗替尼,R1415
|
EGFR;
Autophagy |
Angiogenesis;
Autophagy;
JAK/STAT signaling;
Tyrosine Kinase/Adaptors |
|
Erlotinib (CP358774) 是一种 EGFR 一代抑制剂，抑制 EGFR 19 Del 和 L858R 突变。Erlotinib 具有抗肿瘤活性，用于治疗 EGFR 突变的非小细胞肺癌。Erlotinib 用药会产生 EGFR C797S 耐药突变。 |
|
T7724
|
Tepoxalin
RWJ-20485,RWJ20485,ORF20485,替泊沙林,ORF-20485,RWJ 20485,ORF 20485
|
Lipoxygenase;
COX |
Immunology/Inflammation;
Metabolism;
Neuroscience |
|
Tepoxalin (RWJ 20485) 是有效的5-脂氧合酶和环氧合酶抑制剂，表现出强大的抗炎活性和较小的胃肠道刺激性。 |
|
T9810
|
TNIK-IN-5
|
Wnt/beta-catenin |
Cytoskeletal Signaling;
Stem Cells |
|
TNIK-IN-5 是高效的 TNIK 抑制剂 (IC50= 0.05 μM)。TNIK-IN-5 可以有效抑制细胞中的 Wnt 信号通路。TNIK-IN-5 在体外显示出良好的抗结直肠癌活性。 |
|
T38651
|
Lauryl maltose neopentyl glycol
LMNG
|
Others |
Others |
|
Lauryl maltose neopentyl glycol是一种能溶解和稳定膜蛋白的洗涤剂。Lauryl maltose neopentyl glycol能从膜上提取完整的膜蛋白，从而改善G蛋白偶联受体和呼吸系统复合物等膜蛋白的稳定性。Lauryl maltose neopentyl glycol具有增溶作用。 |
|
T6040
|
Aloxistatin
E64d,Loxistatin,阿洛司他丁,E64c ethyl ester
|
SARS-CoV;
Cysteine Protease |
Microbiology/Virology;
Proteases/Proteasome |
|
Aloxistatin (E64d) 是一种不可逆的、可透过膜的溶酶体和细胞溶质半胱氨酸蛋白酶抑制剂，能够抑制完整血小板中的钙蛋白酶活性。它是一种半胱氨酸蛋白酶抑制剂，具有血小板聚集抑制活性。 |
|
T16087
|
Quiflapon
喹夫拉朋,MK-591
|
Apoptosis;
FLAP |
Apoptosis;
Immunology/Inflammation |
|
Quiflapon (MK-591) 是一种选择性和特异性的FLAP 抑制剂，可诱导细胞凋亡。它也是口服白三烯生物合成抑制剂，在完整的人和诱导的大鼠多形核白细胞 PMNLs 中，其IC50值分别为 3.1 nM 和 6.1 nM。 |
|
T12913
|
Siguazodan
SKF 94836
|
PDE |
Metabolism |
|
Siguazodan (SKF 94836) 是选择性的，口服有效的磷酸二酯酶 III 抑制剂，IC50为 117 nM。它可增加完整血小板中 cAMP 的积累，EC50为 18.88 μM。它也抑制苯肾上腺素诱导的 5-HT 释放，IC50为 4.2 μM。 |
|
TP2008L
|
Lyn peptide inhibitor acetate
Lyn peptide inhibitor acetate(222018-18-0 free base)
|
IL Receptor |
Immunology/Inflammation |
|
Lyn peptide inhibitor acetate(222018-18-0 free base) 是一种有效的细胞渗透性 Lyn 偶联 IL-5 受体信号通路抑制剂，同时保持其他信号完整。它阻断 Lyn 活化并抑制 Lyn 酪氨酸激酶与 IL-3/GM-CSF/IL-5 受体的 βc 亚基的结合。它可用于哮喘、过敏和其他嗜酸性粒细胞疾病的研究。 |
|
TP1956L
|
PKC ζ pseudosubstrate acetate
PKC ζ pseudosubstrate acetate (799764-07-1 free base)
|
PKC |
Chromatin/Epigenetic;
Cytoskeletal Signaling |
|
PKC ζ pseudosubstrate acetate 是蛋白激酶 C (PKC) ζ 的抑制剂；附着于细胞通透性触角足结构域载体肽。由 PKC ζ 假底物结构域的氨基酸 113-129 组成，通过二硫键连接到触角足结构域载体肽。 Antennapedia 肽在 4 或 37°C 时被完整细胞积极吸收，确保快速有效地吸收抑制肽。一旦进入细胞，二硫键在细胞质中被还原，导致抑制肽的释放。通过 PKC ζ 非依赖性途径诱导肥大细胞脱粒。 |
|
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。 |
|
T29600
|
Acetylethylcholine mustard
Aech-M
|
Others |
Others |
|
Acetylethylcholine mustard can effect muscarinic receptor-coupled attenuation of cAMP formation for intact GH3 cells. |
|
T1467
|
Acemetacin
阿西美辛,K-708,TVX 1322
|
COX |
Immunology/Inflammation;
Neuroscience |
|
Acemetacin (TVX 1322) 是一种非甾体抗炎类的化合物。 |
|
T24527
|
Netzahualcoyone
|
Others |
Others |
|
Netzahualcoyone inhibited the respiration of intact cells of B. subtilis but had no effect on the respiration of E. coli. |
|
T29465
|
5-Oxodecanoic acid
5-Ketocapric acid,5-Oxocapric acid
|
Others |
Others |
|
5-Oxodecanoic acid is a biochemical. 5-Oxodecanoic acid can be reducced to 5-hydroxydecanoic acid by intact cells of baker's yeast. |
|
TP2395
|
Nph-peptide
|
|
|
|
Nph-peptide can be used for photoaffinity labeling of the N-formyl peptide receptor site of intact human polymorphonuclear leukocytes. |
|
T68859
|
Rudolfomycin
|
Others |
Others |
|
Rudolfomycin is a class II anthracycline antitumor antibiotic that inhibit the synthesis of nucleolar RNA in intact tumor cells. |
|
T33955
|
PF-6808472
OX-44,OX44,PF 6808472,OX 44,PF6808472
|
Others |
Others |
|
PF-6808472 is a cell permeable covalent probe suitable for click chemistry designated to measure kinase selectivity in intact cells. PF-6808472 contains sulfonyl fluoride group, which react with conserved lysine residue within kinase ATP binding site. |
|
TP1903
|
PKG inhibitor peptide
cGMP Dependent Kinase Inhibitor Peptide
|
|
|
|
Competitive inhibitor of cGMP-dependent protein kinase (PKG); analog of a substrate peptide corresponding to a phosphorylation site of histone H2B. Competes with synthetic substrates (Ki = 86 mM) but does not inhibit phosphorylation of intact histones by |
|
T26172
|
S3QEL-2
S3QEL2,S3QEL 2
|
Others |
Others |
|
S3QEL-2 is a retrograde signaling modulator. It acts by strongly mitigating the oxidative stress-induced apoptosis that limits the yield of functional ß-cells from intact islets. |
|
TP1451
|
TAT peptide
|
|
|
|
TAT peptide corresponds to the polycationic aa49-57 region of TAT protein. TAT peptide is a cell-penetrating peptide (CPP) used to cargo larger molecules through the lipophilic barrier of the cellular membranes to deliver them inside the cells with intact |
|
T60333
|
Cyclopentenyl uracil
|
Others |
Others |
|
Cyclopentenyl uracil 是一种无细胞毒性的尿苷激酶 (uridine kinase) 抑制剂，可有效阻断完整小鼠体内宿主和肿瘤组织对循环尿苷的回收。 |
|
T84457
|
DC4 Crosslinker
|
Others |
Others |
|
DC4 crosslinker, an 18Å mass spectrometry-cleavable crosslinking reagent, features two intrinsic positive charges facilitating the fragmentation of cross-linked peptides into their constituent peptides through collision-induced dissociation or in-source decay. Initial fragmentation leads to cleavage adjacent to the positive charges, enabling the identification of cross-linked peptides as pairs of ions with precise mass separation. Furthermore, the resultant intact peptide fragments can undergo f... |
|
T73180
|
NSC 295642
|
Others |
Others |
|
NSC 295642 是一种磷酸酶抑制剂。NSC 295642 可以显着增加完整细胞中的磷酸Erk 细胞核差异。NSC 295642 可用于癌症研究。 |
|
T79819
|
AMB639752
|
Others |
Others |
|
AMB639752为一种高效DGKα抑制剂，能通过抑止整合体内DGKα活性，复原因重复刺激导致的SAP缺失型淋巴细胞的细胞死亡(RICD)。此化合物适合于X连锁淋巴增生性疾病1(XLP-1)的相关研究。 |
|
T37670
|
CAY10568
|
Others |
Others |
|
Most local anesthetics act by abolishing voltage gated sodium channel currents indiscriminately in all populations of neurons. Selective analgesia through TRPV1-mediated entry of a cationic lidocaine derivative, QX314, was recently reported. CAY10568 is a physically smaller, less hydrophobic version of QX314 designed to be even more permeable to TRPV1 ion channel when activated by agonists such as capsaicin and N-oleoyl dopamine. CAY10568 when given in combination with suitable TRPV1 agonists sh... |
|
T37569
|
4-Methylumbelliferyl-β-D-Galactoside
|
|
|
|
4-Methylumbelliferyl-β-D-galactoside (MUG) is a fluorogenic substrate for β-galactosidase (β-gal).1Hydrolysis of MUG by β-gal releases the fluorescent moiety 4-MU, which displays a pH-dependent excitation maximum of 330, 370, and 385 nm at pH 4.6, 7.4, and 10.4, respectively, and an emission maximum between 445-454 nm.2MUG has been used to detect β-gal activity in intact bacteria, yeast, and mammalian cells.1
1.Vidal-Aroca, F., Giannattasio, M., Brunelli, E., et al.One-step high-throughput assay... |
|
T21962
|
HZ52
|
Others |
Others |
|
HZ52 是一种有效可逆的5-脂氧合酶(5-LO)抑制剂，在完整的人类多形核白细胞中可阻断白三烯的合成，IC50为 0.7 μM。 |
|
T84493
|
CAY10649
|
Others |
Others |
|
1CAY10649, a thiazolinone compound, directly inhibits 5-lipoxygenase (5-LO) product formation in intact polymorphonuclear leukocytes (PMNL) with an IC50 value of 0.28 μM and in a soluble fraction of an S100 PMNL cell lysate with an IC50 value of 0.09 μM, following stimulation by calcium and arachidonic acid. This activity highlights its potential in mitigating inflammatory responses by targeting the biosynthesis of leukotrienes, substances implicated in various inflammatory processes such as neu... |
|
T82543
|
diSulfo-Cy3 alkyne
|
|
|
|
diSulfo-Cy3 alkyne 是一款炔基的点击化学试剂，且为水溶性染料，其吸光度和发射特性与Cy3荧光团一致。该染料适用于蛋白质标记，以及水相环境中完整生物体的标记。 |
|
TP1956
|
PKC ζ pseudosubstrate
|
|
|
|
Inhibitor of protein kinase C (PKC) ζ; attached to cell permeabilisation Antennapedia domain vector peptide. Consists of amino acids 113 - 129 of PKC ζ pseudosubstrate domain linked by a disulphide bridge to the Antennapedia domain vector peptide. The Antennapedia peptide is actively taken up by intact cells, at 4 or 37°C, ensuring rapid and effective uptake of the inhibitor peptide. Once inside the cell, the disulphide bonds are subjected to reduction in the cytoplasm leading to release of the ... |
|
T77014
|
Frovocimab
|
|
|
|
Frovocimab (LY 3015014)为一种人源化IgG4单克隆抗体(mAb)，其功能为中和PCSK9，通过抑制PCSK9与LDL受体(LDLR)的结合，促使已结合的PCSK9正常进行蛋白水解切割。 |
|
T68701
|
Abarelix acetate
|
Others |
Others |
|
Abarelix acetate is a synthetic third generation gonadotropin-releasing hormone receptor (GnRHR) antagonist. It increases histamine release from rat peritoneal mast cells in vitro and from a human skin model ex vivo. In vivo, abarelix decreases plasma luteinizing hormone (LH) levels six hours post-treatment in castrated rats, with levels returning to baseline within 24 hours.3 Abarelix (2 mg/kg) also transiently decreases plasma testosterone levels in intact rats, with levels returning to baseli... |
|
T38107
|
JJH260
JJH260
|
Others |
Others |
|
JJH260 is an N-hydroxy hydantoin carbamate that inhibits androgen-induced gene 1 (AIG1), an enzyme that hydrolyzes fatty acid esters of hydroxy fatty acids (FAHFAs). It blocks the hydrolysis of 9-PAHSA with an IC50 value of 0.57 μM. JJH260 also inhibits the novel FAHFA hydrolase androgen-dependent TFPI-regulating protein (ADTRP; IC50 = 8.5 μM), as well as the serine hydrolase ABHD6 and the lysophospholipases LYPLA1 and LYPLA2. JJH260 inhibits the FAHFA hydrolase activity of LNCaP and T cell lysa... |
|
T30783
|
CDy9
CDy 9,CDy-9
|
Others |
Others |
|
CDy9 is a highly selective fluorescent probe for the detection and isolation of mESC using fluorescence microscopy and flow cytometry. CDy9 allows the detection and isolation of intact stem cells with marginal impact on their function and capabilities. CD |
|
T79756
|
Beclin1-ATG14L interaction inhibitor 1
|
Autophagy |
Autophagy |
|
Beclin1-ATG14L interaction inhibitor 1 (com 19) 作为一种选择性抑制剂，特定抑制脂质激酶VPS34的复合物 I 中Beclin1与ATG14L的相互作用，而对Beclin 1-UVRAG作用重要的VPS34复合物 II 无影响。由此，其阻断VPS34复合物 I 形成，抑制自噬过程，但不干扰复合物 II 介导的囊泡运输。 |
|
T38351
|
DYn-2
|
Others |
Others |
|
Mild oxidation can convert the sulfhydryl group of cysteine residues on proteins to cysteine-sulfenic acid derivatives (Cys-SOH). Protein sulfenylation, then, is a post-translational modification that is relevant to redox signaling. DYn-2 is a chemoselective probe for detecting sulfenylated proteins in intact cells. DYn-2 consists of 1,3-cyclohexanedione coupled to an alkyne moiety by a 3-carbon spacer. The cyclohexanedione group selectively reacts with protein sulfenic acid modifications. The a... |
|
T69603
|
BR103354
|
Others |
Others |
|
BR103354 is a novel fibroblast activation protein (FAP) inhibitor with anti-diabetic and anti-steatotic effects. BR103354 inhibited FAP with an IC50 value of 14 nM, showing high selectivity against dipeptidyl peptidase (DPP)-related enzymes and prolyl oligopeptidase (PREP). BR103354 exhibited good pharmacokinetic properties as evidenced by oral bioavailability of 48.4% and minimal hERG inhibition. Single co-administration of BR103354 with hFGF21 reduced nonfasting blood glucose concentrations, i... |
|
T37473
|
SBFI AM
Sodium-binding Benzofuran Isophthalate Acetoxymethyl ester
|
|
|
|
SBFI AM is a membrane-permeant, fluorescent Na+ indicator dye. It is selective for Na+ over K+ with Kd values of 20 and 120 mM for these ions, respectively. [1]Increasing concentration of Na+ increases the ratio of excitation efficiency at 330-345 nm to that at 370-390 nm with emission collected at 450-550 nm. [1] Therefore, ratio fluorometry and imaging can be performed with the same wavelengths. SBF AM is suitable for single intracellular dye injection and is typically used for high-resolutio... |
|
T35944
|
15-keto-17-phenyl trinor Prostaglandin F2α ethyl amide
15-keto-17-phenyl trinor Prostaglandin F2α ethyl amide
|
Others |
Others |
|
Bimatoprost is the Allergan trade name for 17-phenyl trinor prostaglandin F2α ethyl amide (17-phenyl trinor PGF2α ethyl amide), an F-series PG analog which has been approved for use as an ocular hypotensive drug. Oxidation of the C-15 hydroxyl group produces 15-keto-17-phenyl trinor PGF2α ethyl amide. 15-keto-17-phenyl trinor PGF2α ethyl amide is a potential metabolite of 17-phenyl trinor PGF2α ethyl amide when 17-phenyl trinor PGF2α ethyl amide is administered to intact animals. No pharmacologi... |
|
TP1955
|
PKC β pseudosubstrate
|
|
|
|
Selective cell-permeable peptide inhibitor of protein kinase C (IC50 ~ 0.5 μM). Consists of amino acids 19 - 31 of PKC pseudosubstrate domain linked by a disulphide bridge to a cell permeabilisation Antennapedia domain vector peptide. The Antennapedia pep |
|
T36806
|
TPC2-A1-P
TPC2-A1-P
|
Others |
Others |
|
TPC2-A1-P is a powerful and membrane permeable agonist of two pore channel 2 (TPC2) with an EC50 of 10.5 μM. TPC2-A1-P plays its role by mimicking the physiological actions of PI(3,5)P2. TPC2-A1-P also shows higher potency to induce Na2+ mobilisation from TPC2 than TPC-A1-N . TPC2-A1-P can be used to probe different functions of TPC2 channels in intact cells[1][2][3].
Two-pore channels (TPC1-3) are ancient members of the voltage-gated ion channel superfamily. TPCs are expressed throughout the en... |
|
TP1971
|
Pseudo RACK1
|
|
|
|
Activator of protein kinase C; attached to cell permeabilization Antennapedia domain vector peptide. Consists of peptide derived from the C2 domain of PKC β linked by a disulfide bridge to the Antennapedia domain vector peptide. The Antennapedia peptide i |
|
T36947
|
Pyrithiamine (hydrobromide)
|
Others |
Others |
|
Pyrithiamine is the pyridine analog of thiamine that prevents growth of organisms that require intact thiamine. [1] It inhibits the growth of bacterial and fungal species at a pyrithiamine:thiamine ratio of 10:1 in growth media and induces symptoms of thiamine deficiency in mice at a dietary ratio of 3:1. These effects are reversible with addition of sufficient thiamine in all species. Pyrithiamine inhibits the formation of cocarboxylase from thiamine in chicken blood in a dose-dependent manner.... |
|
T83665
|
α-Helical CRF (9-41) TFA
α-Helical Corticotropin-Releasing Factor (9-41)
|
|
|
|
α-Helical CRF (9-41) 是一种合成的皮质酮释放因子（CRF）拮抗剂。它在0.5至5 µM浓度范围内，能抑制CRF诱导的大鼠前叶垂体细胞释放促肾上腺皮质激素（ACTH）。在体内研究中，α-Helical CRF (9-41) (0.02-0.6 µmol/kg) 能够抑制未经麻醉的完整大鼠体内CRF诱导的ACTH释放，并在0.6 µmol/kg剂量下抑制大鼠应激诱导的ACTH释放。此外，α-Helical CRF (9-41) 在尼古丁诱导的条件性焦虑大鼠模型中增加社交互动时间，并减少小鼠的类似暴饮暴食的乙醇消费。 |
|
T38220
|
11-cis Retinol
|
Others |
Others |
|
11-cisRetinol is an isomer of vitamin A . It is formed from vitamin A,viaatrans-retinyl ester intermediate, by the enzyme RPE65 in the retinal pigment epithelium and then converted to 11-cis retinal as part of the visual cycle.1,211-cisRetinol is an agonist of salamander and human red rod opsins expressed in COS cells and an inverse agonist of salamander red cone opsin, as well as human red and green cone opsins expressed in COS cells.3It promotes pigment formation in cone, but not rod, photorec... |
|
T37297
|
Ru360
|
Others |
Others |
|
Ru360, an oxygen-bridged dinuclear ruthenium amine complex, is a selective mitochondrial calcium uptake inhibitor. Ru360 potently inhibits Ca2+ uptake into mitochondria with an IC50 of 0.184 nM. Ru360 binds to mitochondria with high affinity (Kd of 0.34 nM). Ru360 has antiarrhythmic and cardioprotective effects[1][2].
Ru360 permeates slowly into the cell, and specifically inhibits mitochondrial calcium uptake in intact cardiomyocytes and in isolated heart. 1 μm Ru360 is taken up by myocardial ce... |
|
T40869
|
Moxonidine hydrochloride
BDF5895hydrochloride,盐酸莫索尼定
|
Others |
Others |
|
Moxonidine Hydrochloride is a selective agonist at the imidazoline receptor subtype 1, used as antihypertensive agent.
Target: I1-R
Moxonidine Hydrochloride is a centrally acting antihypertensive agent. Mixed Nischarin (I1 imidazoline receptor) and α2-AR (adrenergic) agonist; displays 40-fold higher affinity for I1 receptors versus α2-adrenoceptors. Moxonidine reduced stimulated NE overflow (log EC50: -6.15 +/- 0.14). AGN192403, a selective ligand at I1-R, had no influence on the dose-response... |
|
T35597
|
Neuromedin U-23 (rat) (trifluoroacetate salt)
|
Others |
Others |
|
Neuromedin U-23 (NMU-23) is a neuropeptide involved in diverse biological processes, including smooth muscle contraction, energy homeostasis, and nociception.1It is an agonist of neuromedin-U receptor 1 (NMUR1; EC50= 0.17 nM for the human receptor in a calcium mobilization assay using HEK293 cells) and NMUR2 (EC50= ~1.4-2 nM for arachidonic acid release in CHO cells expressing the human receptor).2,3NMU-23 (1 μM) induces contractions in isolated rat colon smooth muscle strips.4It decreases body ... |
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