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抑制剂 & 化合物

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Cat. No. Product Name Target Signaling Pathways
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

VA4 is a novel irreversible TG2 transamidase site-specific inhibitor.
T71477 CP4d inhibitor

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

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

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

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

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

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

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

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

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

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

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)

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

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

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

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

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

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

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

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,...

化合物

Itaconate-alkyne
Cat.No: T41302
Synonym: ITalk
Target: Others
A 21960
Cat.No: T26408
Synonym: Ethyl 2-chloroacetoacetate,A21960,A-21960
Target:
VU 0285683
Cat.No: T23509
Synonym:
Target: GluR
Verubecestat
Cat.No: T7011
Synonym: MK-8931,维罗司他
Target: Beta-Secretase, BACE
Unesbulin
Cat.No: T12575
Synonym: PTC596
Target: Apoptosis, BMI-1
Palivizumab
Cat.No: T76907
Synonym: Synagis,MEDI 493
Target: RSV
CGP 78608 hydrochloride
Cat.No: T10781
Synonym: PAMQX
Target: NMDAR, iGluR
PKCε Inhibitor Peptide acetate
Cat.No: T35827L
Synonym: PKCε Inhibitor Peptide acetate(182683-50-7 Free base)
Target: PKC
Rac1 Inhibitor W56 acetate(1095179-01-3 free base)
Cat.No: TP2131L
Synonym:
Target: Rho
Coralyne chloride
Cat.No: T31011
Synonym:
Target: Topoisomerase
PKR-IN-C16
Cat.No: T16550
Synonym:
Target: Others
VA4 TG2 inhibitor
Cat.No: T69933
Synonym:
Target:
CP4d inhibitor
Cat.No: T71477
Synonym:
Target:
Ametoctradin
Cat.No: T68508
Synonym:
Target:
Sp-8-CPT-cAMPS
Cat.No: T38694
Synonym:
Target:
Diglycyl-histidine
Cat.No: T20382
Synonym: NSC334195,NSC-334195,Gly-gly-his,Glycylglycyl-L-histidine,NSC 334195
Target:
CGP-78608
Cat.No: T69949
Synonym:
Target:
Lck inhibitor II
Cat.No: T68349
Synonym:
Target:
Fibrinogen Binding Inhibitor Peptide
Cat.No: TP1778
Synonym:
Target:
Rp-8-CPT-cAMPS
Cat.No: T38696
Synonym:
Target:
Renin FRET Substrate I
Cat.No: T38900
Synonym:
Target:
A 20832
Cat.No: T26407
Synonym: A-20832,A20832
Target:
SARS 3CLpro-IN-1
Cat.No: T61774
Synonym:
Target:
Rac1 Inhibitor W56
Cat.No: TP2131
Synonym:
Target:
Ro 04-5595 free base
Cat.No: T70049
Synonym:
Target:
N-Acetyl-Ser-Asp-Lys-Pro TFA
Cat.No: TP1371
Synonym:
Target:
β-Aminopropionitrile hydrochloride
Cat.No: T72103
Synonym: BAPN hydrochloride
Target:
1-Amino-1-deoxy-D-fructose (hydrochloride)
Cat.No: T35442
Synonym:
Target:
MOA-stilbene
Cat.No: T71565
Synonym:
Target:
Maleimido-tri(ethylene glycol)-propionic acid
Cat.No: T16008
Synonym: Mal-PEG3-acid
Target: Others
Benzoquinoquinoxaline
Cat.No: T61664
Synonym:
Target:
IRES-C11
Cat.No: T40419
Synonym: IRES-C11
Target: c-Myc
6-Formylpterin
Cat.No: T35976
Synonym:
Target:
5-FAM-LPETGG TFA
Cat.No: T83718
Synonym: 5-Carboxyfluorescein-LPETGG
Target:
N-Acetyl-Ser-Asp-Lys-Pro acetate
Cat.No: T75752
Synonym:
Target:
(Rac)-Luciferin 6′-methyl ether sodium
Cat.No: T83529
Synonym: (Rac)-6′-Methoxyluciferin sodium
Target:
AC3-I, myristoylated
Cat.No: T80269
Synonym: Autocamtide-3 Derived Inhibitory Peptide
Target: CaMK
GTP-Binding Protein Fragment, G alpha
Cat.No: TP2254
Synonym:
Target: Others
SARS-CoV-2-IN-60
Cat.No: T79414
Synonym:
Target: SARS-CoV
MYC-RIBOTAC
Cat.No: T78055
Synonym:
Target: c-Myc
(2-pyridyldithio)-PEG4 acid
Cat.No: T17331
Synonym:
Target: Others
Imatinib Impurity E
Cat.No: T73973
Synonym:
Target:
Talabostat
Cat.No: T37861
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
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

天然产物

Masticadienolic acid
Cat.No: TN4505
Synonym:
Target: Others
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