membrane protein inhibitor

HNMPA 是膜不可渗透的胰岛素受体酪氨酸激酶 (insulin receptor tyrosine kinase) 抑制剂。HNMPA 可以抑制人胰岛素受体的酪氨酸和丝氨酸自磷酸化。HNMPA 对环 AMP 依赖性蛋白激酶或蛋白激酶 C 活性没有影响。

Glutathione arsenoxide hydrochloride (Glutathione arsenoxide hydrochloride(1271726-51-2 Free base)) 是一种潜在的抗癌活性分子和肿瘤代谢抑制剂。Glutathione arsenoxide hydrochloride 靶向线粒体内膜腺嘌呤核苷酸转移酶 (ANT)，对细胞增殖有抑制作用，促进细胞凋亡。Glutathione arsenoxide hydrochloride 可用于识别如蛋白质二硫异构酶一样的细胞表面蛋白质。

Dodecylphosphocholine (DPC) 是一种去污剂，普遍用于膜蛋白核磁共振的研究。

C-215 是MmpL3抑制剂。它在 HTS 中被鉴定为对结核分枝杆菌具有独立的甘油活性，对哺乳动物细胞的非特异性毒性较低，对结核分枝杆菌的IC90=16 μM，并且能够有效抑制在巨噬细胞中生长的结核分枝杆菌。

NCGC00262650 是 AMA1-RON2 相互作用和 c-Src 酪氨酸激酶活性的抑制剂。

BRCA1-IN-2 是一种可穿过细胞膜的 BRCA1 蛋白-蛋白相互作用（PPI）抑制剂，具有抗肿瘤活性，通过破坏 BRCA1 (BRCT)2 与蛋白质的相互作用来发挥作用。

BHPI is a potent inhibitor of nuclear estrogen–ERα-regulated gene expression. Elicits sustained ERα-dependent activation of the endoplasmic reticulum (EnR) stress sensor, the unfolded protein response (UPR), and persistent inhibition of protein synthesis.

K-252b is an indolocarbazole isolated from the actinomycete Nocardiopsis and is a PKC inhibitor. K-252b can be used to inhibit extracellular kinases of cells in culture because it can’t pass through the cell membrane freely.

TC13172是一种靶向混合谱系激酶结构域样蛋白（MLKL）的强效共价抑制剂，在10 µM浓度下对MLKL表现出显著选择性，优于密切相关的受体相互作用丝氨酸/苏氨酸激酶1（RIPK1）和RIPK3。TC13172能以2 nM的EC50有效抑制TSZ组合（TNF-α、Smac模拟物和Z-VAD-FMK）诱导的HT-29细胞坏死性凋亡，并在100 nM浓度下阻断TSZ诱导的MLKL寡聚化和质膜转位。

JNJ-9676是一种具有口服活性的冠状病毒膜蛋白抑制剂，通过膜蛋白二聚体跨膜结构域形成的结合口袋，从而阻断病毒组装与释放，对新冠病毒和SARS-CoV具有纳米摩尔水平的抗病毒活性。

Paeoniflorin-6′-O-benzene sulfonate (CP-25) 是一种 G 蛋白偶联受体激酶 2 (GRK2) 的抑制剂，能够阻止 GRK2 移动至细胞膜，并抑制 JAK1/STAT3 信号通路。它还可以抑制 IL-17A/CXCL2 所诱导的 HaCaT 细胞增殖。在小鼠模型中，Paeoniflorin-6′-O-benzene sulfonate 降低了多种炎症因子和趋化因子，例如 IL-17A、IL-17F、IFN-γ、TNF-α、IL-22、IL-23、CXCL2、CXCL3 和 CXCL9，从而减轻 Imiquimod 诱导的银屑病症状。

CIM-834 是一种口服活性选择性抑制剂，专门针对冠状病毒膜蛋白 (M protein)，对SARS-CoV-2和SARS-CoV具备显著的病毒组装抑制作用。CIM-834 通过非共价结合膜蛋白的短形式 (Mshort)，稳定这种形式，并阻止其转变为病毒粒子组装所需的长形式 (Mlong)，从而抑制病毒颗粒的形成。CIM-834 有潜力被用于研究 COVID-19 和其他冠状病毒感染。

Spirovirimat (Compound 7) 是一种高效的猴痘病毒 (MPXV) p37 protein 抑制剂，IC50 为 35 nM。通过抑制病毒膜包裹过程，Spirovirimat 阻止细胞外病毒颗粒的形成，适用于猴痘病毒感染研究。

Glutathione arsenoxide (GSAO) TFA 是一种有潜力的抗癌活性分子和肿瘤代谢抑制剂。它靶向线粒体内膜上的腺嘌呤核苷酸转移酶 (ANT)，并导致细胞增殖停滞和细胞死亡。此外，该化合物可用于识别细胞表面蛋白质，如蛋白质二硫异构酶。

PRMT5-MTA-IN-1 (Compound A9a) 是一种抑制蛋白精氨酸甲基转移酶PRMT5-MTA的化合物。它对结肠直肠癌细胞HCT116野生型和MTAP del突变体的增殖具有抑制作用，IC50分别为16 nM和2.47 μM。PRMT5-MTA-IN-1 展现出优良的肝微粒体稳定性和膜通透性，并在CD-1小鼠中具有良好的药代动力学特征。

SLUPP-225 is an efflux pump inhibitor (EPI) by interacting with the membrane fusion protein AcrA, a critical component of the AcrAB-TolC efflux pump in Escherichia coli.

SLUPP-417 is an efflux pump inhibitor (EPI) by interacting with the membrane fusion protein AcrA, a critical component of the AcrAB-TolC efflux pump in Escherichia coli.

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.

Phosphatidylserine is a naturally occurring phospholipid that comprises 2-10% of total phospholipids in mammals and is enriched in the central nervous system, particularly the retina. It is anionic and found mainly on the inner leaflet of the cell membrane. It is biosynthesized from phosphatidylcholine or phosphatidylethanolamine by phosphatidyl synthase 1 (PSS1) or PSS2, respectively, in the endoplasmic reticulum and can be reversibly converted back by the same enzymes. It can also be irreversibly converted to phosphatidylethanolamine by phosphatidylserine decarboxylase in the mitochondria. Phosphatidylserine binds to T cell immunoglobulin mucin type 1 (TIM-1) and TIM-4 receptors as well as brain-specific angiogenesis inhibitor 1 (BAI1), leading to anti-inflammatory and anti-atherosclerotic effects. It is also a cofactor involved in the activation of various signaling pathways through activation of protein kinase C, neutral sphingomyelinase, and c-Raf-1 protein kinase among others. Phosphatidylserine is externalized during apoptosis by scramblases in the plasma membrane as a signal for phagocytes to engulf the cell. Phosphatidylserines (bovine) is a mixture of bovine phosphatidylserines containing fatty acids with variable chain lengths at the sn-1 and sn-2 positions.

16F16 is a protein disulfide isomerase (PDI) inhibitor.1It inhibits PDI reductase activity in an enzyme assay when used at concentrations ranging from 1 to 100 μg/ml.116F16 reduces PC12 cell apoptosis induced by the misfolded huntingtin protein HTTQ103. It suppresses PDI-dependent mitochondrial outer membrane permeabilization (MOMP) in isolated PC12 cell mitochondria. 16F16 (2, 3, 4, and 10 μM) reduces HTTN90Q73mutant huntingtin-induced medium spinal neuron death and MOMP in rat corticostriatal slices. It also reduces pyramidal neuron death induced by amyloid-β precursor protein (APP) in rat corticostriatal slices. 1.Hoffstrom, B.G., Kaplan, A., Letso, R., et al.Inhibitors of protein disulfide isomerase suppress apoptosis induced by misfolded proteinsNat. Chem. Biol.6(12)900-906(2010)

A2ti-2 是一种亲和力较低且具有选择性的膜联蛋白 A2/S100A10 异四聚体 (A2t) 抑制剂（IC50 : 230 μM)。A2ti-2 具有抗病毒活性，可选择性破坏 A2 和 S100A10 之间的蛋白质相互作用，可防止人乳头瘤病毒 16 型 (HPV16) 感染。

Rp-cAMPS sodium 是一种cAMP的硫代磷酸酯类似物，是一种蛋白激酶 A 抑制剂，也是具有膜渗透性的 cAMP 拮抗剂，通过阻断 cAMP 诱导的构象转变来抑制 cAMP 依赖性蛋白激酶，可用于研究心血管疾病。

Endosidin-2是一种囊外囊抑制剂,具有细胞渗透性的亚苄基苯甲酰肼，可与外囊复合体70 kDa（EXO70）亚基的外囊成分结合（Kd = 253 μM，EXO70A1）。Endosidin-2会破坏蛋白质在内质体和质膜之间的转运，从而促进蛋白质转运至液泡降解。它还能抑制 HeLa 细胞中内吞转铁蛋白向质膜的再循环，并能靶向哺乳动物 EXO70的多种异构体，导致外泌失调。Endosidin2 可作为工具分子研究胞吐。

Sec61-IN-2 (A347) is a protein secretion inhibitor.