site-specific

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。

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）。

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。

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。

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, activates the proprotein form of caspase-1 independent of the inflammasome adaptor ASC[2]. Talabostat competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26 DPP-IV, and there is a high-affinity interaction with the catalytic site due to the formation of a complex between Ser630 624 and the boron of talabostat[3]. Talabostat can stimulate immune responses against tumors involving both the innate and adaptive branches of the immune system. In WEHI 164 fibrosarcoma and EL4 and A20 2J lymphoma models, PT-100 causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory. Talabostat treatment of WEHI 164-inoculated mice increases mRNA expression of cytokines and chemokines known to promote T-cell priming and chemoattraction of T cells and innate effector cells[3]. Talabostat treated mice show significant less fibrosis and FAP expression is reduced. Upon PT100 treatment, significant differences in the MMP-12, MIP-1α, and MCP-3 mRNA expression levels in the lungs are also observed. Treatment with PT100 in this murine model of pulmonary fibrosis has an anti-fibro-proliferative effect and increases macrophage activation[4]. [1]. Connolly BA, et al. Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potencyand in vivo efficacy and safety. J Med Chem. 2008 Oct 9;51(19):6005-13. [2]. Okondo MC, et al. DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis. Nat Chem Biol. 2017 Jan;13(1):46-53. [3]. Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80. [4]. Egger C, et al. Effects of the fibroblast activation protein inhibitor, PT100, in a murine model of pulmonary fibrosis. Eur J Pharmacol. 2017 Aug 15;809:64-72.

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。

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。

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。

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

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。

(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 flexibility and biocompatibility for optimal drug release while maintaining stability throughout the circulation in the body. Ultimately, (2-Pyridyldithio)-PEG4 acid is instrumental in the development and advancement of ADCs, a promising approach in cancer therapy.

Boc-D-2,3-diaminopropionic acid (N-t-Boc-amino-D-alanine) 作为一种含有Boc保护基团的氨基酸衍生物，主要应用于合成具有GluN2亚单位特异性活性的高效NMDA受体甘氨酸位点激动剂。

PV1162是一种高选择性的Chk2抑制剂，具有0.29 nM的IC50值。该化合物能够通过特异性靶向Chk2 ATP结合位点后方的门控依赖性疏水口袋，阻断ATP与Chk2的结合，从而有效抑制Chk2的磷酸化活性。由于这种机制，PV1162在抗癌治疗中展示了明显的应用前景。

NeoSTX（Neosaxitoxin）是一种特异性钠通道阻滞剂，其作用部位为第1位点。它与局部麻醉药共同作用，通过周围神经阻滞或局部浸润来提供手术麻醉，并显著延长术后镇痛时间。

Diglycyl-histidine is a tripeptide complexed with cupric ion designed to mimic specific Cu(II) transport site of ascorbate on albumin molecule.

MS8511 (hydrochloride) 是一种针对G9a GLP的共价不可逆抑制剂，靶向底物结合位点的半胱氨酸残基，具有IC50值为100 nM (G9a) 和140 nM (GLP)，以及Kd值44 nM (G9a) 和46 nM (GLP)的特点。该化合物可以降低细胞内H3K9me2水平，并增强抗增殖活性。MS8511 (hydrochloride) 适用于研究多种癌症，包括脑癌、乳腺癌、卵巢癌、肺癌、膀胱癌、黑色素瘤和结直肠癌，以及其他疾病，如阿尔茨海默病 (AD)、镰状细胞病和Prader-Willi综合征 (PWS)。

Metaphit methylsulfate 是一种特异性的PCP拮抗剂，作为大鼠脑匀浆中 [3H] 苯环利定结合位点的定位酰化剂。通过突触前机制，Metaphit methylsulfate 抑制了PCP诱导的运动行为。

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

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

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。

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.

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.

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.

IRES-C11是针对c-MYC基因内部核糖体进入位点(IRES)的特异性翻译抑制剂。IRES-C11通过阻断异源核糖核蛋白A1（一种对c-MYC IRES活性必需的跨作用因子）与其相应IRES之间的相互作用，从而发挥作用。值得注意的是，IRES-C11不抑制BAG-1、XIAP和p53的IRES活性。