caspase-6-in-1

Caspase-6-IN-1 is a novel Allosteric Inhibitor of Caspase-6 Activation, blocking the interaction between C6 and mHTT1-586.

Bfl-1-IN-6 (Compound 20) 是一种口服有效的Bcl-2相关蛋白 A1 (BFL1) 抑制剂，IC50为19 nM。Bfl-1-IN-6 能稳定BFL1蛋白、激活裂解的caspase 3，并在小鼠模型中展现抗肿瘤活性。

Ac-VEID-AMC is a fluorogenic substrate based on the caspase-6 cleavage site in lamin A at amino acids VEID during apoptosis.1It has also been reported to be cleaved by related proteases, including caspase-8.2Caspase activity can be quantified by fluorescent detection of free AMC (also known as 7-amino-4-methylcoumarin), which is excited at 340-360 nm and emits at 440-460 nm. 1.Talanian, R.V., Quinlan, C., Trautz, S., et al.Substrate specificities of caspase family proteasesJ. Biol. Chem.272(15)9677-9682(1997) 2.Chae, H.J., Park, K.M., Lee, G.Y., et al.Je-Chun-Jun induced apoptosis of human cervical carcinoma HeLa cellsActa Pharmacologica Sinica25(10)1372-1379(2004)

LL-37 is a cationic and α-helical antimicrobial peptide expressed in human bone marrow, testis, granulocytes, and gingival epithelium and is upregulated in psoriatic lesions. It inhibits growth of Gram-positive E. coli D21 and Gram-negative B. megatarium in a concentration-dependent manner and LL-37 expression is induced in A549 epithelial cells, alveolar macrophages, neutrophils, and monocyte-derived macrophages following M. tuberculosis infection. LL-37 binds sheep erythrocytes coated with S. minnesota Re-LPS and induces agglutination with a minimal agglutinating concentration (MAC) of 12.1 μg/ml. It is a chemoattractant for, and can induce calcium mobilization in, human monocytes, neutrophils, and T cells that naturally express formyl peptide receptor-like 1 (FPRL1) and FPRL1-transfected HEK293 cells. LL-37 (10-15 μM) pretreatment of dengue virus type 2 (DENV-2) reduces its infectivity as well as levels of viral genomic RNA and NS1 antigen. In vivo, LL-37 inhibits cecal ligation and puncture-induced caspase-1 activation and pyroptosis of peritoneal macrophages, reduces levels of the inflammatory cytokines IL-1β, IL-6, and TNF-α, and improves survival in polybacterial septic mice.

5,7-Dihydroxychromone (5,7-Dihydroxy-4H-Chromen-4-One) 是一种Cudrania tricuspidata 的提取物，通过激活 Nrf2 ARE 信号对 6-OHDA 诱导的氧化应激和细胞凋亡发挥神经保护作用。它抑制 6-OHDA 诱导的 SH-SY5Y 细胞中活化的caspase-3，caspase-9以及切割的PARP 表达。

AKN-028 acetate 是一种新型酪氨酸激酶 (TKI) 抑制剂，是一种有效的口服活性的 FMS 样受体酪氨酸激酶 3 (FLT3) 抑制剂，其 IC50值为 6 nM。AKN-028 acetate 抑制 FLT3 自磷酸化。AKN-028 acetate 诱导剂量依赖性的细胞毒性反应 (平均IC50=1 μM)。AKN-028 acetate 通过激活 caspase 3 诱导细胞凋亡 (apoptosis)。AKN-028 acetate 可用于急性髓系白血病 (AML) 的研究。

Mulberroside A 是桑中的一种主要活性成分，可降低TNF-α、IL-1β和IL-6的表达，抑制 NALP3、caspase-1 和 NF-κB 的激活以及 ERK、JNK 和 p38 的磷酸化 。它抑制蘑菇酪氨酸酶，具有抗炎和抗细胞凋亡作用。

AC-VEID-CHO (TFA) 是一种源自多肽的半胱天冬酶抑制剂，针对Caspase-6、Caspase-3和Caspase-7展示出优异的抑制效果，其IC50值分别为16.2 nM、13.6 nM和162.1 nM。该化合物常用于研究阿尔茨海默病、亨廷顿病等神经退行性疾病。

HDAC-IN-53是一种口服活性的选择性HDAC1-3抑制剂，其IC50分别为47 nM、125 nM和450 nM。该化合物不针对II类HDAC(HDAC4、5、6、7、9；IC50>10 μM)展现抑制作用。HDAC-IN-53能够诱导caspase依赖的细胞凋亡并在裸鼠中显著抑制人肿瘤异种移植物生长，同时抑制携带MC38结肠癌的免疫活性小鼠的肿瘤发展。

Fluorescein-6-carbonyl-Asp(OMe)-Glu(OMe)-Val-DL-Asp(OMe)-fluoromethylketone 是一种细胞渗透性且无毒的抑制剂，它能与活化的caspase-3在凋亡细胞内不可逆结合。该抑制剂的荧光强度可通过流式细胞仪、微孔板读数器或荧光显微镜检测。

Skullcapflavone I has anti-inflammatory and anti-allergic potential, it can significantly inhibit LPS stimulated NO and PGE(2) release in J774A.1 macrophages and inhibit LPS induced IL-6 production in a concentration dependent manner. Skullcapflavone I se