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Cat. No. | Product Name | Target | Signaling Pathways |
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T41302 |
Itaconate-alkyne
ITalk |
Others | Others |
Itaconate-alkyne (ITalk) 是一种生物正交探针,用于对炎症性巨噬细胞中的衣康酸进行定量和位点特异性化学蛋白质组学分析,并能够对其直接靶标进行生化评估和蛋白质组学分析。 | |||
T26408 |
A 21960
Ethyl 2-chloroacetoacetate,A21960,A-21960 |
||
A 21960 (Ethyl 2-chloroacetoacetate) 能抑制 resolvase 与两个直接重复的 res 位点之间的突触形成,阻断位点特异性重组反应,可用于研究细菌感染。 | |||
T23509 |
VU 0285683
|
GluR | Neuroscience |
VU 0285683 是 mGluR5 的特异性负变构调节剂,对 MPEP 结合位点具有高亲和力。 VU 0285683 表现出抗焦虑样活性。 | |||
T7011 |
Verubecestat
MK-8931,维罗司他 |
Beta-Secretase; BACE | Neuroscience |
Verubecestat (MK-8931) 是一种高亲和力的、具有口服活性的BACE1和BACE2抑制剂,Ki 分别为 2.2 nM 和 0.38 nM。它可以有效降低 Aβ40,并具有潜力用于阿尔茨海默氏病。 | |||
T12575 |
Unesbulin
PTC596 |
Apoptosis; BMI-1 | Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
Unesbulin (PTC596) 是一种口服有效和选择性的 B 细胞特异性莫洛尼氏鼠白血病病毒整合位点 1 抑制剂。它在急性髓细胞白血病细胞中可下调 MCL-1 并诱导不依赖 p53 的线粒体凋亡,具有抗白血病作用。 | |||
T76907 |
Palivizumab
Synagis,MEDI 493 |
RSV | Microbiology/Virology |
Palivizumab (MEDI 493) 是一种人源化 RSV 特异性单克隆抗体,选择性抑制RSV A和B亚型F蛋白A抗原位点的表位,可用于预防呼吸道合胞病毒感染 (RSV)。 | |||
T10781 |
CGP 78608 hydrochloride
PAMQX |
NMDAR; iGluR | Membrane transporter/Ion channel; Neuroscience |
CGP 78608 hydrochloride 是 NMDA 受体甘氨酸结合位点的特异性拮抗剂 (IC50 = 6 nM)。 CGP 78608 hydrochloride 具有抗惊厥活性。 CGP 78608 hydrochloride 增强 GluN1/GluN3A 介导的甘氨酸电流(估计 EC50 = 26.3 nM)。 | |||
T35827L |
PKCε Inhibitor Peptide acetate
PKCε Inhibitor Peptide acetate(182683-50-7 Free base) |
PKC | Chromatin/Epigenetic; Cytoskeletal Signaling |
PKCε Inhibitor Peptide acetate 是一种特异性 PKCε 抑制剂,含有其特定受体活化 C 激酶 (RACK) 的位点。 PKCε Inhibitor Peptide acetate 抑制 PKCε 的转运,但不抑制 αPKC,βPKC 和 δPKC 的转运。 | |||
TP2131L |
Rac1 Inhibitor W56 acetate(1095179-01-3 free base)
|
Rho | Cell Cycle/Checkpoint |
Rac1 Inhibitor W56 acetate(1095179-01-3 free base) 包含 Rac1 的鸟嘌呤核苷酸交换因子 (GEF) 识别/激活位点的残基 45-60 的肽;选择性抑制 Rac1 与 Rac1 特异性 GEF TrioN、GEF-H1 和 Tiam1 的相互作用。 | |||
T31011 |
Coralyne chloride
|
Topoisomerase | DNA Damage/DNA Repair |
Coralyne chloride 是一种具有强抗癌活性的原小檗碱。它可用于制备 Coralyne 衍生物,是一种基于荧光 DNA 的分子整流剂,通过位点特异性插入构建成 DNA 双链体。它可作为一种拓扑异构酶 I 毒性分子,诱导拓扑异构酶 I 介导 DNA 裂解。 | |||
T16550 |
PKR-IN-C16
|
Others | Others |
PKR-IN-C16 是一种特异性蛋白激酶抑制剂。它能够抑制 PKR 的自磷酸化,解除 PKR 在原代神经元细胞培养中诱导的翻译阻断。 | |||
T69933 |
VA4 TG2 inhibitor
|
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VA4 is a novel irreversible TG2 transamidase site-specific inhibitor. | |||
T71477 |
CP4d inhibitor
|
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CP4d is a novel reversible tg2 transamidase site-specific inhibitor | |||
T68508 | Ametoctradin | ||
Ametoctradin is a new Oomycete-specific fungicide and a potent Qo site inhibitor of the mitochondrial respiration complex III. | |||
T38694 |
Sp-8-CPT-cAMPS
|
||
Sp-8-CPT-cAMPS is a powerful and specific cAMP analog that activates cAMP-dependent protein kinase A (PKA I and PKA II) selectively and effectively. It exhibits a 153-fold preference for site A of RI over site A of RII, and a 59-fold preference for site B of RII over site B of RI. | |||
T20382 |
Diglycyl-histidine
NSC334195,NSC-334195,Gly-gly-his,Glycylglycyl-L-histidine,NSC 334195 |
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Diglycyl-histidine is a tripeptide complexed with cupric ion designed to mimic specific Cu(II) transport site of ascorbate on albumin molecule. | |||
T69949 | CGP-78608 | ||
CGP-78608 is a glycine site-specific N-methyl-D-aspartate receptor antagonist prevents activation of the NMDA/NO/CGMP pathway by ammonia. | |||
T68349 |
Lck inhibitor II
|
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Lck inhibitor II is a cell-permeable, ATP binding site-targeting, tri-substituted pyrimidine that acts as a highly potent Lck (lymphocyte specific kinase) inhibitor | |||
TP1778 |
Fibrinogen Binding Inhibitor Peptide
|
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Fibrinogen Binding Inhibitor Peptide, a synthetic dodecapeptide, represents the specific platelet receptor recognition site of the human fibrinogen g-chain (residues 400-411). | |||
T38696 | Rp-8-CPT-cAMPS | ||
Rp-8-CPT-cAMPS is a powerful and competitive antagonist of cAMP-induced activation of cAMP-dependent protein kinase (PKA) I and II. Acting as a potent cAMP analog, Rp-8-CPT-cAMPS exhibits a preference for site A of RI over site A of RII. Additionally, it favors site B of RII over site B of RI. This compound effectively inhibits cAMP-dependent PKA activation and demonstrates selectivity in binding to specific sites within the protein kinase. | |||
T38900 |
Renin FRET Substrate I
|
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Renin FRET Substrate I is a specific compound that functions as a substrate for human renin. It is specifically designed to contain the exact cleavage site found in the N-terminal peptide of human angiotensinogen. | |||
T26407 |
A 20832
A-20832,A20832 |
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A-20832 inhibits resolvase-promoted site-specific recombination postsynaptically at strand cleavage. It does not inhibit resolvase binding to res, as measured by filter binding, or synapse formation. DNase I analysis in the presence of A-20832 indicates t | |||
T61774 |
SARS 3CLpro-IN-1
|
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SARS 3CLpro-IN-1 (Compound 3b) is a stereo-specific SARS 3CL protease inhibitor that belongs to the octahydroisochromene scaffold. It demonstrates inhibition against the P1 site imidazole, with an IC50 value of 95 μM [1]. | |||
TP2131 |
Rac1 Inhibitor W56
|
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Rac1 Inhibitor W56 is a peptide comprising residues 45-60 of the guanine nucleotide exchange factor (GEF) recognition/activation site of Rac1. Rac1 Inhibitor W56 selectively inhibits Rac1 interaction with Rac1-specific GEFs TrioN, GEF-H1 and Tiam1. | |||
T70049 |
Ro 04-5595 free base
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Ro 04-5595 is a selective antagonist of NMDA receptors NR2B subunits. Ro 04-5595 had an EC 50 of 186 ± 32 nmol/L. Ro 04-5595 was predicted to bind the EVT-101 binding site, not the ifenprodil-binding site. Specific binding, defined with a new NR2B-specific antagonist Ro 04-5595 at 10 microM was fully inhibited by several compounds with the following rank order of affinities--Ro 25-6981 > CP-101,606 > Ro 04-5595 = ifenprodil >> eliprodil > haloperidol > spermine > spermidine > MgCl2 > CaCl2--and... | |||
TP1371 |
N-Acetyl-Ser-Asp-Lys-Pro TFA
|
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N-Acetyl-Ser-Asp-Lys-Pro (TFA) is an endogenous tetrapeptide that is naturally produced in the bone marrow. It serves as a specific substrate for the N-terminal site of ACE, the enzyme responsible for angiotensin converting activity. | |||
T72103 |
β-Aminopropionitrile hydrochloride
BAPN hydrochloride |
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β-Aminopropionitrile (BAPN) hydrochloride 是一特异性、不可逆性、口服活性的氨酰氧化酶 (LOX) 抑制剂,针对 LOX 或 LOXL 同工酶活性位点。 | |||
T35442 |
1-Amino-1-deoxy-D-fructose (hydrochloride)
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1-Amino-1-deoxy-D-fructose is an amino monosaccharide.1It induces site-specific DNA damage at pyrimidine residues in cell-free assays. 1-Amino-1-deoxy-D-fructose moieties have been found as a component of fructosamines, glycated serum proteins that are elevated in patients with conditions such as diabetes.2,3 | |||
T71565 | MOA-stilbene | ||
MOA-stilbene, also known as 3-Methoxy-2-(2-styrylphenyl)propenic acid methyl ester, is a fluorescence inhibitor. MOA-stilbene is a new tool for investigation of the reactions of the chloroplast cytochrome bf complex. MOA-stilbene is known to be a specific inhibitor of the Qo site of mammalian cytochrome bc 1 complex. | |||
T16008 |
Maleimido-tri(ethylene glycol)-propionic acid
Mal-PEG3-acid |
Others | Others |
Maleimido-tri(ethylene glycol)-propionic acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Maleimido-tri(ethylene glycol)-propionic acid is used for the preparation of neolymphostin-based ADC precursors for site-spec | |||
T61664 |
Benzoquinoquinoxaline
|
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Benzoquinoquinoxaline (BQQ) is a heterocyclic compound featuring an aminoalkyl side chain. BQQ exhibits preferential binding to DNA triplex structures, intercalating between the bases to stabilize the triplex conformation. Additionally, conjugation of BQQ to 1,10-phenanthroline enables specific binding and cleavage of double-strand DNA at the site where a triplex structure forms [1]. | |||
T40419 |
IRES-C11
IRES-C11 |
c-Myc | Cell Cycle/Checkpoint |
IRES-C11 is a specific inhibitor of translation that targets the internal ribosome entry site (IRES) of the c-MYC gene. It functions by blocking the interaction between heterogeneous nuclear ribonucleoprotein A1, a trans-acting factor required for c-MYC IRES activity, and its corresponding IRES. Notably, IRES-C11 does not inhibit the IRES activity of BAG-1, XIAP, and p53. | |||
T35976 | 6-Formylpterin | ||
Xanthine oxidase (XO) generates reactive oxygen species, including hydrogen peroxide (H2O2), as it oxidizes specific substrates in the presence of water and oxygen. 6-Formylpterin is an oxidized pterin produced by photolytic breakdown of folic acid. It binds to one of two active sites on XO nearly quantitatively and irreversibly and prevents the metabolism of other substrates at the second site, resulting in hetero-substrate" inhibition at nanomolar concentrations. However | |||
T83718 |
5-FAM-LPETGG TFA
5-Carboxyfluorescein-LPETGG |
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5-FAM-LPETGG是一种荧光肽,由排序酶识别序列LPETGG与荧光标记5-carboxyfluorescein (5-FAM) 结合而成,其激发/发射最大值分别为492/518 nm。通过排序酶催化的转肽连接,它已被用于靶蛋白的特异性标记。 | |||
T75752 |
N-Acetyl-Ser-Asp-Lys-Pro acetate
|
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N-Acetyl-Ser-Asp-Lys-Pro (Ac-SDKP) acetate 是血管紧张素转换酶 (ACE) N 端活性位点的特异性底物。N-Acetyl-Ser-Asp-Lys-Pro acetate 是多能干细胞增殖的天然抑制剂。N-Acetyl-Ser-Asp-Lys-Pro acetate 具有抗炎和抗纤维化特性。 | |||
T83529 |
(Rac)-Luciferin 6′-methyl ether sodium
(Rac)-6′-Methoxyluciferin sodium |
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D-Luciferin 6'-methyl ether (6'-Methoxyluciferin; compound 19a) sodium 是北美萤火虫Photinus pyralis荧光素酶 (PpyLuc) 的有效抑制剂,具有0.1 μM的IC50值。作为D-荧光素的类似物,本化合物在PpyLuc的ATP及荧光素结合位点展示了非特异性的相互作用。 | |||
T80269 |
AC3-I, myristoylated
Autocamtide-3 Derived Inhibitory Peptide |
CaMK | Neuroscience |
AC3-I, myristoylated 为一种具有高度特异性的 CaMKII 抑制剂,为 Autocamtide-3 衍生的生物活性肽。通过将 Autocamtide-3 中的 Thr-9 磷酸化位点替换为 Ala,赋予该肽抗蛋白水解能力,从而制备出该肉豆蔻酰化形式。 | |||
TP2254 |
GTP-Binding Protein Fragment, G alpha
|
Others | Others |
Using specific antisera raised against synthetic peptides, we find that three distinct GTP-binding protein alpha subunits remain bound to the plasma membrane even after activation with nonhydrolyzable GTP analog. Trypsin cleaves each alpha subunit at a si | |||
T79414 |
SARS-CoV-2-IN-60
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SARS-CoV | Microbiology/Virology |
SARS-CoV-2-IN-60(compound 5a)是SARS-CoV-2 nsp16-nsp10甲基转移酶的竞争性及不可逆抑制剂,与SAM结构相竞争,具有特异性地结合于nsp16的SAM结合位点旁的新发现口袋。其IC50值为9 μM,Ki值为26 μM,显示出针对泛冠状病毒的治疗潜力。 | |||
T78055 |
MYC-RIBOTAC
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c-Myc | Cell Cycle/Checkpoint |
MYC-RIBOTAC 是一种针对MYC内部核糖体进入位点(IRES)的核糖核酸酶靶向降解剂(RIBOTAC)。该化合物结合了MYC mRNA的靶向组分以及一种可招募并激活RNA酶L1的小分子。通过降低MYC的mRNA和蛋白质表达水平,MYC-RIBOTAC诱导细胞发生凋亡,应用于抗肿瘤治疗的研究。 | |||
T17331 |
(2-pyridyldithio)-PEG4 acid
|
Others | Others |
(2-Pyridyldithio)-PEG4 acid is a four-unit cleavable polyethylene glycol (PEG) linker specifically designed for the synthesis of antibody-drug conjugates (ADCs)[1]. It serves as a crucial component in the conjugation of antibodies and drugs, enabling targeted drug delivery and enhanced therapeutic efficacy. This linker possesses a (2-pyridyldithio) group at one end, facilitating the attachment of the linker to the specific site on the antibody molecule. The PEG4 chain provides the necessary flex... | |||
T73973 | Imatinib Impurity E | ||
Imatinib Impurity E 是 Imatinib 的杂质。Imatinib 是一种口服生物可用的酪氨酸激酶抑制剂,可选择性抑制 BCR/ABL,v-Abl,PDGFR,c-kit 激酶活性。Imatinib (STI571) 靠近 ATP 结合位点结合,将其锁定在封闭或自我抑制的构象中,因此半竞争性抑制蛋白质的酶活性。Imatinib 还抑制 SARS-CoV 和MERS-CoV。 | |||
T37861 |
Talabostat
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Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8/9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9,... |
Cat. No. | Product Name | Target | Signaling Pathways |
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TN4505 | Masticadienolic acid | Others | Others |
Masticadienolic acid is a specific competitive inhibitor of secreted phospholipase A2, it not only protects the active site histidine from alkylation but also inhibits the action of secreted from pancreas, synovial fluid, and bee venom. Masticadienolic ac |