Apoptosis

There are many forms of cell death, most of which can be triggered by a variety of stimuli and physiological conditions. The often compared are apoptosis and necrosis. Apoptosis has become the focus of research area due to its complex nature and the different roles of maintaining healthy and self-sustaining biological entities. On the other hand, necrosis is a form of cell damage against acute external injury and trauma, leading to passive cell death and causing an inflammatory response. [1]

The BCl-2 family has been identified as its important role in apoptosis. The BH domain promotes interaction of family members with one another and may be indicative of pro-apoptotic or anti-apoptotic functions. Usually the BCL-2 family have been classified into one of three subfamilies; anti-apoptosis,  BH3 only (pro-apoptotic) and pro-apoptotic proteins. The great promise for cancer therapy has been shown in recent research about BCL-2 targeting.[2]

In the cell cycle, apoptosis acts as a fail-safe measure to prevent fidelity and proliferation quality. Although a certain degree of genetic variation is allowed and evolution is promoted, regenerative cells with extensive genetic errors and cell damage are subject to apoptosis. P53 is the Key role in the cell cycle system which  initiate the apoptosis in certain cell types. P53 is a widely studied tumor suppressor. The p53 tumor suppressor gene is most frequently mutated in cancer cells (mutation occurs in more than 50% of human cancers) [3], which makes the restriction mechanism ineffective. Tumorigenesis is likely to commence when the p53-based preventive system loses its function completely.

Expression of stimuli, such as DNA damage, hypoxia and activation of certain oncoproteins (eg, Myc, Ras) are dependent on the apoptotic pathway of p53 [4]. The transactivation function of p53 plays an important role in inducing apoptosis, the pro-apoptotic proteins, Bax and lgF-Bp3, are transcriptional targets of p53.[5] As a well-known tumor suppressor, p53 is recognized for its ability to initiate apoptosis in the cell cycle and its ability to induce cell arrest and DNA repair in regenerative cells. In addition to p53, there are many other cell cycle regulators that can affect apoptosis (eg, pRb, p21).

Many studies have emphasized the importance of apoptosis in the self-defense mechanism or immune system. The immune system is responsible for rendering the host resistant to a variety of external pathogens. Apoptosis is an integral part of the immune system and helps maintain the homeostasis of the immune system.  Secondly, the immune system relies on apoptosis to eliminate unwanted functional maturation of T cells and B cells [6].  Finally, apoptosis confers cytotoxicity to certain cell types (ie, cytotoxic T lymphocytes and natural killer cells). A well-coordinated disruption protocol allows these cells to destroy target cells while the target cells remain intact. Cytotoxic T lymphocytes (CTLs) can induce target cell death in two ways, one of which involves perforin and granzymes.

  • Majno G. and Joris I. (1995) Apoptosis, oncosis, and necrosis. An overview of cell death. Am. J. Pathol. 146, 3–15
  • Zhiqing Liu, et al. Drug Discov Today. 2016 Jun; 21(6): 989–996.
  • Wang X.W. and Harris C.C. (1997) p53 tumor-suppressor gene: clues to molecular carcinogenesis. J. Cell. Physiol. 173, 247–255 10.1002/(SICI)1097-4652(199711)173:2%3c247::AID-JCP30%3e3.0.CO;2-A.
  • Levine A.J. (1997) p53, the cellular gatekeeper for growth and division. Cell 88, 323–331 10.1016/S0092-8674(00)81871-1.
  • Owen-Schaub LB,et al. Owen-Schaub LB,Wild-type human p53 and a temperature-sensitive mutant induce Fas/APO-1 expression. Mol Cell Biol. 1995 Jun; 15(6):3032-40.
  • Russell J.H. (1995) Activation-induced death of mature T cells in the regulation of immune responses. Curr. Opin. Immunol. 7, 382–388 10.1016/0952-7915(95)80114-6.

产品 101 到 150 共 198个

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  1. CP 31398 2HCl

    Catalog No. A13522
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    p53 stabilizer
    CP 31398 2HCl已显示出可作为p53的稳定剂,并促进癌细胞系中p53的活性。 了解更多
  2. CP 31398 dihydrochloride

    Catalog No. A15346
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    p53 stabilizer
    CP 31398 dihydrochloride是p53稳定剂。在具有突变型或野生型p53的癌细胞系中稳定p53的活性构象并提高p53的活性。在体内抑制小的人类肿瘤异种移植物的生长。 了解更多
  3. NSC59984

    Catalog No. A13413
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    P53 Activator
    NSC59984通过MDM2和泛素蛋白酶体途径诱导突变p53蛋白降解。大多数癌细胞中NSC59984的EC50明显低于正常细胞,p53-null HCT116细胞的EC50为8.38 uM。 了解更多
  4. RG7112

    Catalog No. A11523
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    selective p53-MDM2 抑制剂
    RG7112是首个临床小分子MDM2抑制剂,HTRF IC50为18 nM,设计用于占据MDM2的p53结合口袋。 了解更多
  5. PK11007

    Catalog No. A16833
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    p53 activator
    PK11007是一种抗p53药物,可通过两个表面暴露的半胱氨酸的选择性烷基化来稳定野生型和突变型p53,而不会损害其DNA结合活性。它不仅通过重新激活p53发挥抗肿瘤功能,还通过其他细胞机制发挥作用,例如将细胞ROS升高至毒性水平并激活UPR。 了解更多
  6. CBL-0137

    Catalog No. A16836
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    p53 activator / NF-κB 抑制剂
    CBL0137 (CBL-0137)在基于细胞的p53和NF-kB报告基因检测中分别激活p53和抑制NF-kB,EC50为0.37 uM和0.47 uM。它还抑制组蛋白伴侣FACT(促进染色质转录复合物)。 了解更多
  7. Pifithrin-β

    Catalog No. A22006
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    p53 inhibitor
    Pifithrin-β (PFT β) is a potent p53 inhibitor with an IC50 of 23 μM. 了解更多
  8. Pifithrin-alpha

    Catalog No. A12451
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    p53 抑制剂
    Pifithrin-alpha是p53介导的细胞凋亡和p53依赖性基因转录(如细胞周期蛋白G,p21/waf1和mdm2表达)的可逆抑制剂。 了解更多
  9. Pifithrin-u

    Catalog No. A12449
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    p53 抑制剂
    Pifithrin-u通过降低p53与抗凋亡蛋白Bcl-2和Bcl-XL的亲和力来抑制p53与线粒体的结合。 了解更多
  10. NSC 319726

    Catalog No. A12930
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    p53R175 activator
    NSC 319726是突变体p53R175的有效和选择性激活剂。 了解更多
  11. p53 and MDM2 proteins-interaction-inhibitor chiral

    Catalog No. A15201
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    p53-MDM2 interaction 抑制剂
    p53和MDM2蛋白相互作用抑制剂手性是p53和MDM2蛋白之间相互作用的抑制剂。 了解更多
  12. p53 and MDM2 proteins-interaction-inhibitor racemic

    Catalog No. A15202
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    p53-MDM2 interaction 抑制剂
    p53和MDM2蛋白相互作用抑制剂消旋体是p53和MDM2蛋白之间相互作用的抑制剂。 了解更多
  13. MIRA-1

    Catalog No. A15348
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    p53 inducer
    MIRA-1恢复突变型p53的野生型构象,功能和DNA结合活性。诱导p21,MDM2和PUMA的p53转录反式激活。 了解更多
  14. NSC 146109 hydrochloride

    Catalog No. A15349
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    p53 activator
    NSC 146109 hydrochloride是激活p53依赖性转录的细胞渗透性,基因型选择性抗肿瘤剂。 了解更多
  15. PhiKan 083

    Catalog No. A15350
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    p53 stabilizer
    PhiKan 083是p53稳定剂;在与功能性DNA/蛋白质相互作用区域不同的位点,突变型(Y220C)p53优先结合野生型p53。 了解更多
  16. RETRA hydrochloride

    Catalog No. A15351
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    mutant p53 Reactivator
    RETRA hydrochloride是一种抗肿瘤剂,在体内外均以突变的p53和p73依赖性方式抑制肿瘤细胞的生长。 了解更多
  17. SJ 172550

    Catalog No. A15352
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    MDMX 抑制剂
    SJ 172550是第一种MD50抑制剂,EC50为0.84 uM;与MDMX可逆结合,并有效杀死其中放大了MDMX表达的成视网膜细胞瘤细胞。 了解更多
  18. WR 1065

    Catalog No. A15353
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    P53/p21waf-1/MDM2 activator
    WR 1065是一种氨磷汀(Ethyol)的去磷酸化代谢产物,可防止受到辐射的直接和延迟影响。 了解更多
  19. JNJ 26854165

    Catalog No. A10491
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    p53 activator
    JNJ-26854165是P53激活剂之一,与AraC或阿霉素协同作用,诱导P53介导的凋亡,可能为急性白血病的治疗提供新的治疗途径。 了解更多
  20. Pifithrin-beta

    Catalog No. A12450
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    p53 抑制剂
    Pifithrin-beta是p53的小分子抑制剂。 了解更多
  21. Tenovin-6

    Catalog No. A12305
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    p53 activator
    Tenovin-6是tenovin-1的类似物。Tenovin-6在体外抑制纯化的人SIRT1、SIRT2和SIRT3的蛋白脱乙酰酶活性,IC50值分别为21、10和67 uM。 了解更多
  22. Apoptosis Activator 2

    Catalog No. A11944
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    Apoptosis Activator
    Apoptosis Activator 2 强烈诱导caspase-3激活,PARP裂解和DNA片段化,导致细胞破坏(依赖Apaf-1),IC50为约4μM,对HMEC,PREC或MCF-10A细胞无效。 了解更多
  23. Z-FA-FMK

    Catalog No. A14284
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    Irreversible Cysteine Protease 抑制剂
    Z-FA-FMK是不可逆的半胱氨酸蛋白酶抑制剂。 了解更多
  24. 25-hydroxy Cholesterol

    Catalog No. A13704
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    25-hydroxy Cholesterol是一种衍生自膳食胆固醇的侧链取代氧固醇,可抑制固醇调节元件结合蛋白(SREBPs)的裂解,从而抑制各种细胞类型中的内源性胆固醇合成。 了解更多
  25. Boc-D-FMK

    Catalog No. A15392
    Caspase 抑制剂
    BOC-D-FMK是Caspase-3的新型抑制剂。 了解更多
  26. Emricasan

    Catalog No. A11394
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    Caspase inhibitor
    Emricasan is a first-in-class caspase inhibitor in clinical trials for the treatment of liver diseases. 了解更多
  27. Z-YVAD-FMK

    Catalog No. A16317
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    Caspase-1 抑制剂
    Z-YVAD-FMK是有效的细胞渗透性和caspase-1不可逆抑制剂。 了解更多
  28. Z-VAD(OH)-FMK

    Catalog No. A16340
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    Caspase 抑制剂
    Z-VAD(OH)-FMK是所有胱天蛋白酶的不可逆三肽抑制剂。 了解更多
  29. Z-FA-FMK

    Catalog No. A16381
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    Cysteine protease 抑制剂
    Z-FA-FMK是半胱氨酸蛋白酶的不可逆抑制剂。 了解更多
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    MX1013

    Catalog No. A17218
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    pan-caspase inhibitor
    MX1013 is a dipeptide pan-caspase inhibitor that inhibits caspase-1, caspase-3, and caspase-6, 7, 8, and 9. 了解更多
  30. Nivocasan (GS-9450)

    Catalog No. A14100
    Caspase 抑制剂
    Nivocasan (GS-9450)是一种新型的caspase抑制剂,已在纤维化/凋亡动物模型中证明了其肝保护活性。 了解更多
  31. Z-WEHD-FMK

    Catalog No. A14916
    Caspase 抑制剂
    Z-WEHD-FMK是不可逆抑制caspase-5和相关caspase活性的合成肽。 了解更多
  32. Caspase-3/7 Inhibitor I

    Catalog No. A14919
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    Caspase-3/7 抑制剂
    Caspase-3/7 Inhibitor I是caspase-3(Ki = 60 nM)和caspase-7(Ki = 170 nM)的有效,细胞可渗透且可逆的有效抑制剂。 了解更多
  33. Ac-LEHD-AFC

    Catalog No. A15291
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    Fluorogenic caspase substrate
    Ac-LEHD-AFC,荧光半胱天冬酶底物。caspase-9底物的类似物LEHD-AFC。 了解更多
  34. AZ 10417808

    Catalog No. A15294
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    Caspase-3 抑制剂
    AZ 10417808,caspase-3的选择性非肽抑制剂(Ki = 247 nM);相对于半胱氨酸蛋白酶1、2、6、7和8(Ki> 10 uM)显示的选择性> 40倍。 了解更多
  35. PETCM

    Catalog No. A15308
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    Caspase-3 activator
    PETCM是caspase-3的激活剂,也是HeLa细胞质中凋亡小体形成的刺激物。 了解更多
  36. Ac-IEPD-AFC

    Catalog No. A15319
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    Fluorogenic caspase substrate
    Ac-LEHD-AFC是caspase-4,caspase-5和caspase-9的荧光底物。 了解更多
  37. Ac-DEVD-CHO

    Catalog No. A15816
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    Caspase 抑制剂
    Ac-DEVD-CHO是醛肽和CPP32/Apopain抑制剂。 了解更多
  38. Z-VEID-FMK

    Catalog No. A12611
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    Caspase-6 抑制剂
    Z-VEID-FMK是caspase-6 / Mch2的特异性识别序列。 Z-VEID-FMK是不可逆地抑制VEID依赖性胱天蛋白酶(例如caspase-6)活性的合成肽。 抑制剂被设计为甲酯,以促进细胞渗透性。 了解更多
  39. Z-VDVAD-FMK

    Catalog No. A12637
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    Caspase-2 抑制剂
    Z-VDVAD-FMK是caspase-2的细胞渗透性不可逆抑制剂。半胱天冬酶抑制剂在研究生物学过程中起重要作用。 了解更多
  40. Z-DQMD-FMK

    Catalog No. A12697
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    Caspase-3 抑制剂
    Z-DQMD-FMK是不可逆地抑制Caspase-3活性的合成肽。 了解更多
  41. Z-IETD-FMK

    Catalog No. A12800
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    caspase 8 抑制剂
    Z-IETD-FMK是caspase 8的特异性抑制剂。 了解更多
  42. EP1013

    Catalog No. A11212
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    caspase inhibitor
    EP1013 is a broad-spectrum caspase selective inhibitor, used in the research of type 1 diabetes. 了解更多
  43. BOC-D-FMK

    Catalog No. A11356
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    caspase inhibitor
    Boc-D-FMK is a cell-permeable, irreversible and broad spectrum caspase inhibitor; inhibits apoptosis stimulated by TNF-α with an IC50 of 39 ?M. 了解更多
  44. ML132

    Catalog No. A21557
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    caspase 1 inhibitor
    ML132 (NCGC 00185682) is a potent and selective caspase 1 inhibitor with an IC50 of 0.316 nM. 了解更多
  45. PAC-1

    Catalog No. A11090
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    Caspase activator
    PAC-1是procaspase-3的激活剂,可诱导癌细胞凋亡,EC50为2.08μM。 了解更多
  46. Q-VD-OPh hydrate

    Catalog No. A14915
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    Caspase 抑制剂
    Q-VD-OPh hydrate是一种选择性,脑和细胞可渗透的,高效且不可逆的caspase-3(IC50 = 25nm),caspase-1(IC50 = 50nM),caspase-8(IC50 = 100nM)和caspase-9抑制剂 (IC50 = 430nM)。 了解更多
  47. Ivachtin

    Catalog No. A15300
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    Caspase-3 抑制剂
    Ivachtin是一种有效的,细胞可渗透的,可逆的,非竞争性的Caspase-3抑制剂(IC50 = 23 nM)。 了解更多
  48. Z-LEHD-FMK

    Catalog No. A14358
    Caspase-9 抑制剂
    Z-LEHD-FMK是一种不可逆抑制caspase-9和相关caspase活性的合成肽。 了解更多
  49. LY573636 (Tasisulam)

    Catalog No. A13070
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    Apoptosis inducer
    LY573636 (Tasisulam)是一种有效的抗肿瘤剂,在体外和体内引起多种人实体瘤的生长停滞和凋亡。LY573636诱导的凋亡通过线粒体靶向机制发生。 了解更多

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