Apoptosis is a distinctive form of cell death exhibiting specific morphological and biochemical characteristics, including cell membrane blebbing, chromatin condensation, genomic DNA fragmentation, and exposure of specific phagocytosis signaling molecules on the cell surface. Cells undergoing apoptosis differ from those dying through necrosis. Necrotic cells are usually recognized by the immune system as a danger signal and, thus, resulting in inflammation; in contrast, apoptotic death is quiet and orderly.
There are two major pathways of apoptotic cell death induction: The intrinsic pathway, also called the Bcl-2-regulated or mitochondrial pathway, is activated by various developmental cues or cytotoxic insults, such as viral infection, DNA damage and growth-factor deprivation, and is strictly controlled by the BCL-2 family of proteins. The extrinsic or death-receptor pathway is triggered by ligation of death receptors (members of the tumor necrosis factor (TNF) receptor family, such as Fas or TNF receptor-1 (TNFR1)) that contain an intracellular death domain, which can recruit and activate caspase-8 through the adaptor protein Fas-associated death domain (FADD; also known as MORT1) at the cell surface. This recruitment causes subsequent activation of downstream (effector) caspases, such as caspase-3, -6 or -7, without any involvement of the BCL-2 family.
Studies suggest that alterations in cell survival contribute to the pathogenesis of a number of human diseases, including cancer, viral infections, autoimmune diseases, neurodegenerative disorders, and AIDS (acquired immunodeficiency syndrome). Treatments designed to specifically alter the apoptotic threshold may have the potential to change the natural progression of some of these diseases.
| Cat. No. | Product Name | CAS No. | Purity | Chemical Structure |
|---|---|---|---|---|
| KM11653 |
Domatinostat tosylate
Domatinostat tosylate (4SC-202) 是一种 I 型 HDAC 抑制剂，能够抑制 HDAC1，HDAC2，和 HDAC3 的活性，IC50 值分别为 1.20 μM，1.12 μM 和 0.57 μM；同时能够抑制组蛋白赖氨酸特异性脱甲基酶1 (Lysine specific demethylase 1) 的活性。 |
1186222-89-8 | 98% |
|
| KM7457 |
Doxorubicin hydrochloride
Doxorubicin (Hydroxydaunorubicin) hydrochloride是一种具有细胞毒性的蒽环类抗生素，是一种抗癌化疗试剂。Doxorubicin hydrochloride 是一种有效的人类 DNA topoisomerase I 和 topoisomerase II 抑制剂，IC50 分别为 0.8 μM 和 2.67 μM。Doxorubicin hydrochloride 可降低 AMPK 及其下游靶蛋白乙酰辅酶 A 羧化酶的磷酸化。还可诱导凋亡 (apoptosis) 和自噬。 |
25316-40-9 | 98% |
|
| KM13147 |
Dp44mT
Dp44mT是具有选择性抗癌活性的铁螯合剂 (iron chelator)。 |
152095-12-0 | ≥98% |
|
| KM17386 |
DPBQ
DPBQ 以多倍体特异性方式激活 p53 并触发凋亡 (apoptosis)，但不抑制拓扑异构酶或结合 DNA。DPBQ 引起 p53 的表达和磷酸化，这种作用是四倍体细胞特有的。 |
7029-89-2 | ≥98% |
|
| KM3005 |
DPN
DPN (Diarylpropionitrile) 是一种非甾体雌激素受体 ERβ 选择性配体，其 EC50 值为 0.85 nM。DPN 在许多神经系统疾病具有神经保护作用。 |
1428-67-7 | 98% |
|
| KM19173 |
Dracorhodin perchlorate
Dracorhodin perchlorate (Dracohodin perochlorate) 是来源于天然药物血竭的一种天然产物。Dracorhodin perchlorate 能抑制细胞增殖，诱导细胞周期阻滞和凋亡。 |
125536-25-6 | 98% |
|
| KM10254 |
Droloxifene
Droloxifene，Tamoxifen 衍生物，是一种具有口服活性和选择性的雌激素受体 (estrogen receptor) 调节剂。Droloxifene 具有抗雌激素和抗植入作用。Droloxifene 诱导 MCF-7 细胞 p53 表达及凋亡。Droloxifene 预防去卵巢大鼠骨丢失。 |
82413-20-5 | 98% |
|
| KM8387 |
Droxinostat
Droxinostat(NS41080)是HDAC3，HDAC6和HDAC8抑制剂，IC50分别为16.9，2.47和1.46 μM。 |
99873-43-5 | 98% |
|
| KM11244 |
DT2216
DT2216 是一种 PROTAC 类的有效的，选择性的 BCL-XL (Bcl-2 家族成员) 降解剂。DT2216 通过募集 Von Hippel-Lindau (VHL) E3 泛素连接酶来降解 BCR-ABL 蛋白。DT2216 可以抑制各种 BCL-XL 依赖性白血病和癌细胞，但对血小板的毒性要小得多。 |
2365172-42-3 | 98% |
|
| KM8135 |
Dubermatinib
Dubermatinib (TP-0903) 是具有高效性和选择性的Axl受体酪氨酸激酶抑制剂，IC50值为27 nM。 |
1341200-45-0 | 98% |
|
| KM4654 |
Dutasteride
Dutasteride (GG745)是5α 还原酶同工酶 (5α-reductase isozymes) 抑制剂，还可能因其结构域DHT相似对雄激素受体 (AR) 产生脱靶效应。 |
164656-23-9 | 98% |
|
| KM2907 |
E64FC26
E64FC26 是蛋白质二硫键异构酶 (PDI) 家族的一种有效的泛抑制剂，对 PDIA1、PDIA3、PDIA4、TXNDC5 和 PDIA6 的 IC50 分别为 1.9、20.9、25.9、16.3 和 25.4 μM。E64FC26 显示抗骨髓瘤活性。 |
2285446-62-8 | 98% |
|
| KM5485 |
EB-3D
EB-3D 是有效的选择性胆碱激酶 α (ChoKα) 抑制剂，对 ChoKα1 的 IC50 值为 1 μM。EB-3D 对 ChoKα 表达、AMPK 激活、细胞凋亡 (apoptosis)、内质网应激和脂质代谢有影响。EB-3D 在一组T-白血病细胞系中显示出强大的抗增殖活性。具有抗癌活性。 |
1839150-63-8 | 98% |
|
| KP1391 | EB1 | 42951-68-8 |
|
|
| KM6951 |
EC359
EC359 是一种有效的，选择性的，高亲和力的和口服的生物利用度白血病抑制因子受体 (LIFR) 抑制剂，其 Kd 值为 10.2 nM，可直接与 LIFR 相互作用以有效阻断 LIF/LIFR 相互作用。 |
2012591-09-0 | 98% |
|
| KM18269 |
Ecdysone
Ecdysone (α-Ecdysone) 是昆虫和草药中的主要类固醇激素，可以激活盐皮质激素受体 (MR) 并诱导细胞凋亡 (apoptosis)。Ecdysone 通过其活性代谢物 20-羟基蜕皮激素 (Crustecdysone; 20E; ) 在协调发育过渡和体内稳态睡眠调节中起重要作用。 |
3604-87-3 |
|
|
| KM16305 |
Echinocystic acid
Echinocystic acid是从皂角的果实中提取出来的五环三萜，有很强的抗氧化，抗炎症和抗肿瘤的特性。 |
510-30-5 | ≥98% |
|
| KM5822 |
Ecteinascidin 770
Ecteinascidin 770 (ET-770)是具有抗癌活性的1,2,3,4-四氢异喹啉生物碱，抑制U373MG cells的IC50值为4.83 nM。 |
114899-80-8 | 98% |
|
| KM18881 |
Edaravone
Edaravone 是一种新颖的，有效的自由基清除剂，能够抑制大鼠与 MMP-9 有关的脑出血。 |
89-25-8 | 98% |
|
| KM19313 |
Edaravone D5
Edaravone D5 是 Edaravone 的氘代标记物。Edaravone 是一种有效的自由基清除剂，能够抑制大鼠与 MMP-9 有关的脑出血。 |
1228765-67-0 |
|
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