rearrangement

Taletrectinib (AB-106) 是具有口服活力的、选择性的 ROS1 NTRK 抑制剂。它对重组 ROS1、NTRK1、NTRK2 和 NTRK3 有较强的抑制作用，IC50值分别为 0.207、0.622、2.28 和 0.98 nM。它还抑制 ROS1 G2032R 和其他抗 Crizotinib 的 ROS1 突变体。

Bohemine 是一种合成的选择性CDK 抑制剂，是嘌呤类似物，具有抗癌活性。它对Cdk2 cyclin E、Cdk2 cyclin A 和Cdk9 cyclin T1的IC50分别为 4.6 μM、83 μM 和 2.7 μM。

IC 86621 是一种选择性和可逆的 ATP 竞争性 DNA-PK 抑制剂，IC50 为 120 nM。 IC 86621 增加 DNA 双链断裂 (DSB) 诱导的抗肿瘤活性，其 EC50 为 68 µM，用于 DNA-PK 介导的细胞 DSB 修复。

L-Glutathione reduced (Glutathione) 属于天然三肽，存在与细胞中，是一种内源性抗氧化剂，可以清除氧自由基。L-Glutathione reduced 是某些酶的辅助因子，参与蛋白质二硫键重排并减少过氧化物。

Revumenib（SNDX-5613） 是一种有效的选择性口服 menin-KMT2A 相互作用抑制剂，Ki 为 0.149 nM，IC50 为 10 在 20 nM 之间，可用于 MLL 基因重排的急性白血病研究。

Ionizable Lipid 4, 一种阳离子脂质，是在过氧化氢诱导下CA-lipid 5重排的产物。

AS-254s 是 absent, small, or homeotic-like 1 protein (ASH1L) 的抑制剂，IC50 为 94 nM (FP 测定)。对于 MLL1 重排的白血病细胞，AS-254s 显示出抗增殖活性，GI50 < 1 μM，并能诱导 MLL1-r 白血病细胞的分化。

PtdIns-(3,4,5)-P3 (PIP3) serves as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains such as phosphatidylinositol 3-kinase (PI3K) or PTEN. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking and initiates an intricate signaling cascade that has been implicated in cancer. 3,5-dimethyl PIT-1 is a dimethyl analog of PIT-1, the selective inhibitor of PIP3 Akt PH domain binding, that is designed for more favorable solubility in vivo. 3,5-dimethyl PIT-1 inhibits PI3K Akt signaling (IC50 = 27 μM), suppressing PI3K-PDK1-Akt-dependent phosphorylation, which has been shown to reduce cell viability and induce apoptosis in PTEN-deficient U87MG glioblastoma cells (IC50 = 36 μM). 4T1 breast cancer growth is significantly attenuated in BALB c mice with a dose of 1 mg kg of 3,5-dimethyl PIT-1 per day.

The phosphatidylinositol (PtdIns) phosphates represent a small percentage of total membrane phospholipids. However, they play a critical role in the generation and transmission of cellular signals. PtdIns-(3,4,5)-P3, also known as PIP3, is resistant to cleavage by PI-specific phospholipase C (PLC). Thus, it is likely to function in signal transduction as a modulator in its own right, rather than as a source of inositol tetraphosphates. PIP3 can serve as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking. PtdIns-(3,4,5)-P3 (1,2-dihexanoyl) is a synthetic analog of natural PIP3 with C6:0 fatty acids at the sn-1 and sn-2 positions. The compound features the same inositol and diacylglycerol (DAG) stereochemistry as that of the natural compound. The short fatty acid chains of this analog give it different physical properties from naturally-occurring PIP3, including higher solubility in aqueous media.

7-Biopterin is a 7-substituted pterin.1It is formed by non-enzymatic rearrangement of 4a-hydroxy-tetrahydropterin in the absence of pterin-4a-carbinolamine dehydratase (PCD)in vitroand levels are elevated in the urine of hyperphenylalaninemia patients carrying heterozygous mutations in the PCBD gene encoding PCD.1,2

MI-3454 是一种具有口服活性，选择性和高效性的 Menin-MLL1 相互作用抑制剂，可抑制具有 MLL1 易位或 NPM1 突变的急性白血病细胞增殖并诱导分化。MI-3454 通过下调参与白血病发生的关键基因，诱导MLL1重排或NPM1突变白血病小鼠模型中白血病的完全缓解或消退。

RET-IN-8 是转染期间重排激酶 (RET) 的抑制剂，能够用于癌症的研究。

RET-IN-15 是转染期间重排激酶 (RET) 的抑制剂，能够用于癌症的研究。

CBS1194 is a novel antiviral agent against influenza A virus (IAV), and is more specifically, a group 2 IAV fusion inhibitor. CBS1194 prevents membrane fusion of the virus through the inhibition of the conformational change of hemagglutinin (HA). CBS1194 causes steric hinderance that prevents the rearrangement of the HA that would normally be induced by low-pH, by fitting into the pocket by the fusion peptide.

Zenocutuzumab (MCLA-128) 是一种靶向 HER2 和 HER3 的细胞外结构域的人源化抗体，可用于研究由 NRG1 基因重排驱动的肿瘤。

XLR11, a synthetic cannabinoid (CB) featuring a tetramethylcyclopropyl group, exhibits enhanced affinity for the CB2 receptor, common among synthetic CBs for its receptor affinity. XLR11 degradant, a frequent impurity identified in GC-MS analysis of XLR11-containing samples, originates from the thermal decomposition of XLR11, leading to an opened ring structure. This change results in a distinct fragment ion in mass spectrometry, being 15 amu heavier than XLR11's base peak. Such a signature is indicative of a McLafferty rearrangement in the degradant, a reaction not observed in the parent compound.

Phosphatidylinositols, comprising about 10% of total cellular phospholipids, are glycerophospholipids featuring a glycerol backbone, two non-polar fatty acid tails (primarily C16:0 and C18:0), and a polar inositol head group. Synthesized from cytidine diphosphate diacylglycerol (CPD-DAG) and myoinositol via phosphoinositol synthase, these compounds play pivotal roles in cellular processes, including calcium regulation, vesicle trafficking, mitogenesis, cell survival, and actin rearrangement. Phosphorylation of their inositol rings produces phosphoinositides, crucial for these cellular functions. [Matreya, LLC. Catalog No. 1048]

Volazocine 是一种具有麻醉-拮抗特性的高效口服活性激动剂。其制备可以通过两种独立的合成方法完成：一种是对volazocine进行硝化和后续还原，另一种是通过cyclazocine甲醚的溶解金属还原，随后进行肟化和Semmler-Wolff重新排列。还研究并测试了几种类似物。

Biotin-TEG-ATFBA 作为点击化学试剂,具备全氟苯基叠氮基团.该化合物在光解后生成高度稳定的氮烯中间体,可通过中等至良好的产率进行插入和加成反应(非分子间重排).

Tetrabutylammonium trifluoromethanesulfonate，简称 TBAOTf。TBAOTf 广泛用于有机合成，作为强酸催化剂和相转移剂，特别是在亲核取代、消除和重排反应中表现出色。此外，它也是可充电电池的电解质添加剂和超临界流体的稳定剂。由于其卓越的稳定性、溶解度和选择性，TBAOTf 被认为是一种高效多功能的试剂，适用于多种应用。