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 145 共 145个

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  1. NVP-CGM097

    Catalog No. A16326
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    MDM2 抑制剂
    NVP-CGM097是一种有效的选择性MDM2抑制剂。具有潜在抗肿瘤活性的口服生物利用型HDM2拮抗剂。 了解更多
  2. MX-69

    Catalog No. A16348
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    MDM2/XIAP 抑制剂
    MX-69是MDM2/XIAP抑制剂,用于癌症治疗。 了解更多
  3. HDM201

    Catalog No. A16834
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    MDM2 抑制剂
    HDM201是新型,高效且选择性的p53-Mdm2相互作用抑制剂,其对Mdm2的亲和常数在皮摩尔范围内,相对Mdm4的选择性比大于10000倍。 了解更多
  4. RO-5963

    Catalog No. A18813
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    MDM2/MDMX inhibitor
    RO-5963 is an inhibitor of the interaction of both MDM2 and MDMX with p53 with IC50s of ~17 nM and ~24 nM, respectively. 了解更多
  5. MI-1061

    Catalog No. A18450
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    MDM2 inhibitor
    MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53, induces apoptosis, and has anti-tumor activity. 了解更多
  6. Difopein

    Catalog No. A14917
    14-3-3 protein 抑制剂
    Difopein,R18肽的二聚体形式,以高亲和力与14.3.3蛋白结合。 了解更多
  7. GSK2656157

    Catalog No. A13577
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    PERK 抑制剂
    GSK2656157是PERK酶活性的ATP竞争性抑制剂,IC50为0.9 nmol/L。 对于PER(K)IC50值> 100 nmol/L,对300种激酶组合具有高度选择性。 了解更多
  8. Salubrinal

    Catalog No. A12676
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    eIF2α dephosphorylation 抑制剂
    Salubrinal是细胞磷酸酶复合物的可渗透细胞的选择性抑制剂,可将真核翻译起始因子2亚基α(eIF2α)磷酸化。保护细胞免受内质网应激诱导的细胞凋亡(EC50?15 μM)。 了解更多
  9. ISRIB

    Catalog No. A14302
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    PERK 抑制剂
    ISRIB是一种有效的选择性PERK抑制剂,IC50为5 nM。 了解更多
  10. GSK2606414

    Catalog No. A12792
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    PERK 抑制剂
    GSK2606414是口服有效的选择性PERK抑制剂,IC50为0.4 nM。 了解更多
  11. ISRIB (trans-isomer)

    Catalog No. A13816
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    PERK 抑制剂
    ISRIB (trans-isomer)是一种有效的选择性小分子PERK信号抑制剂(IC50?5 nM),可以有效逆转eIF2α磷酸化的作用。 了解更多
  12. YM155 (Sepantronium Bromide)

    Catalog No. A11002
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    Survivin 抑制剂
    YM155 (Sepantronium Bromide)是一种新型小分子存活蛋白抑制剂,IC50为0.54 nM,可抑制存活蛋白启动子活性。 了解更多
  13. GSK481

    Catalog No. A12615
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    RIP1 抑制剂
    GSK481是新型的RIP1抑制剂苯并a庚酮(BOAz)系列。受体相互作用蛋白激酶1(RIP1)已被认为是通过调节程序性坏死调节炎症的关键因素。已显示对该激酶的抑制作用可阻止细胞坏死,从而将RIP1确定为潜在治疗多种炎性疾病的可行靶标。 了解更多
  14. GSK583

    Catalog No. A16311
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    RIP2 kinase 抑制剂
    GSK583是RIP2激酶的高效抑制剂。 了解更多
  15. RIP2 kinase inhibitor 1

    Catalog No. A16312
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    RIP2 kinase 抑制剂
    RIP2 kinase inhibitor 1 是从专利WO/2014043446 A1(化合物实施例1)中提取的受体相互作用蛋白2(RIP2)激酶抑制剂。 了解更多
  16. RIP2 kinase inhibitor 2

    Catalog No. A16313
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    RIP2 kinase 抑制剂
    RIP2 kinase inhibitor 2 是从专利WO/2014043437 A1(化合物实施例9)中提取的受体相互作用蛋白2(RIP2)激酶抑制剂。 了解更多
  17. GSK963

    Catalog No. A18346
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    RIP1 kinase inhibitor
    GSK963 is a chiral, highly potent and selective inhibitor of RIP1 kinase, with an IC50 of 29 nM. GSK963 is a selective and potent inhibitor of necroptosis in murine and human cells in vitro. 了解更多
  18. HS-1371

    Catalog No. A18653
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    RIP3 inhibitor
    HS-1371 is a potent and ATP-competitive receptor-interacting protein kinase 3 (RIP3) inhibitor with an IC50 of 20.8?nM. 了解更多
  19. PK68

    Catalog No. A18582
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    RIPK1 inhibitor
    PK68 is a potent and selective type II inhibitor of receptor-interacting kinase 1 (RIPK1) with an IC50 of ~90?nM, displays inhibition of RIPK1-dependent necroptosis. 了解更多
  20. GSK-843

    Catalog No. A18526
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    RIPK3 inhibitor
    GSK-843 (GSK'843) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 8.6 nM, and inhibits kinase activity with an IC50 of 6.5 nM. 了解更多
  21. GSK3145095

    Catalog No. A19427
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    RIP1 kinase inhibitor
    GSK3145095 is a RIP1 kinase inhibitor with an IC50 of 6.3 nM . 了解更多
  22. GSK2982772

    Catalog No. A19380
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    RIP1 kinase inhibitor
    GSK2982772 is a potent, orally active and ATP competitive RIP1 kinase inhibitor with IC50 values of 16 nM and 20 nM for human and monkey RIP1, respectively. 了解更多
  23. GSK547

    Catalog No. A19073
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    RIP1 inhibitor
    GSK547 (GSK-547) is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIP1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer. 了解更多
  24. RIPK1-IN-3

    Catalog No. A19023
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    RIPK1 inhibitor
    RIPK1-IN-3 (Example 38), a RIPK1 inhibitor, extracted from patent WO2018148626A1, possesses anti-inflammatory proprieties. 了解更多
  25. RIPK1-IN-7

    Catalog No. A18940
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    RIPK1 inhibitor
    RIPK1-IN-7 is a potent and selective RIPK1 inhibitor with a Kd of 4 nM and an enzymatic IC50 of 11 nM. RIPK1-IN-7 exhibits excellent antimetastasis activity in the experimental B16 melanoma lung metastasis model. 了解更多
  26. RIPA-56

    Catalog No. A12473
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    RIP1 inhibitor
    RIPA-56 is a highly potent, selective, and metabolically stable inhibitor of receptor-interacting protein 1 (RIP1) with an IC50 of 13 nM. 了解更多
  27. WEHI-345

    Catalog No. A21012
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    RIPK2 inhibitor
    WEHI-345 is a potent and selective RIPK2 kinase inhibitor with an IC50 of 0.13 μM, which delays RIPK2 ubiquitylation and NF-κB activation on oligomerization domain (NOD) stimulation. 了解更多
  28. RIPK1-IN-4

    Catalog No. A21029
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    RIP1 kinase inhibitor
    RIPK1-IN-4 (compound 8) is a potent and selective type II kinase inhibitor of receptor interacting protein 1 (RIP1) kinase and binds to a DLG-out inactive form of RIP1 with an IC50s of 16 nM and 10 nM for RIP1 and ADP-Glo kinase. 了解更多
  29. Nec-4

    Catalog No. A21033
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    RIP1 inhibitor
    Nec-4, a tricyclic derivative, is a potent receptor interacting protein 1 (RIP1) inhibitor, with an IC50 of 2.6 μM, Ki of 0.46 μM. 了解更多
  30. NQDI 1

    Catalog No. A12838
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    ASK1 抑制剂
    NQDI 1是细胞凋亡信号调节激酶1(ASK1,MAP3K5)的选择性抑制剂(IC50 = 3 μM,Ki = 500 nM)。 了解更多
  31. Selonsertib

    Catalog No. A15991
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    ASK1 抑制剂
    Selonsertib是一种凋亡信号调节激酶1(ASK1)的口服生物利用抑制剂,具有潜在的抗炎,抗肿瘤和抗纤维化活性。 了解更多
  32. Regorafenib (BAY 73-4506)

    Catalog No. A10250
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    VEGFR 抑制剂
    Regorafenib (BAY 73-4506)是一种多激酶抑制剂,IC50为17、40和69 nM c-KIT,VEGFR2,B-Raf。Regorafenib(BAY 73-4506)是一种针对肿瘤及其脉管系统的口服生物利用型多激酶抑制剂。 了解更多
  33. Danusertib (PHA-739358)

    Catalog No. A10715
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    Aurora 抑制剂
    Danusertib (PHA-739358)是Aurora A/B/C的Aurora激酶抑制剂,在无细胞分析中的IC50为13 nM/79nM/61 nM,对Abl,TrkA,c-RET和FGFR1以及更低的浓度具有中等效力 对Lck,VEGFR2/3,c-Kit,CDK2等有效。 了解更多
  34. TG101209

    Catalog No. A11180
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    JAK2 抑制剂
    TG101209是一种新型的JAK2抑制剂,无细胞试验中IC50为6 nM,对Flt3和RET作用效果稍弱,IC50分别为25 nM和17 nM,作用于JAK2比作用于JAK3选择性高30倍左右,对JAK2V617F和MPLW515L/K突变型敏感。在多发性骨髓瘤中具有显着的体外活性,并且对CD45+骨髓瘤细胞显示出优先的细胞毒性。 了解更多
  35. RPI-1

    Catalog No. A13832
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    Ret kinase 抑制剂
    RPI-1是一种竞争性强效ATP依赖性Ret激酶抑制剂。 了解更多
  36. Regorafenib monohydrate

    Catalog No. A15218
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    Tyrosine kinase 抑制剂
    Regorafenib monohydrate是VEGFR1/VEGFR2/VEGFR3/PDGFRβ/Kit/RET和Raf-1的多靶点抑制剂,IC50分别为13 nM/4.2 nM/46 nM/22 nM/7 nM/1.5 nM和2.5 nM。 了解更多
  37. RET-IN-1

    Catalog No. A19015
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    RET inhibitor
    RET-IN-1 is a RET kinase inhibitor extracted from patent WO2018071447A1, Compound Example 552, has IC50s of 1 nM, 7 nM, and 101 nM for RET (WT), RET (V804M) , and RET (G810R), respectively . 了解更多
  38. Regorafenib Hydrochloride

    Catalog No. A11546
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    VEGFR1/2/3/PDGFRβ/Kit/RET/Raf-1 inhibitor
    Regorafenib Hydrochloride is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively. 了解更多
  39. cis-Pralsetinib

    Catalog No. A21586
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    RET inhibitor
    cis-Pralsetinib (cis-BLU-667) is a highly potent and selective inhibitor of rearranged during transfection (RET), with IC50s ranging from 0.3 to 0.4 nM for WT RET and four enzyme variants (V804L, V804M, M918T, CCDC6-RET), and with broad, robust and anti-tumor activity against multiple RET-driven solid tumor types. 了解更多
  40. BBT594

    Catalog No. A21039
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    RET inhibitor
    BBT594 is a potent receptor tyrosine kinase RET inhibitor, used for cancer treatment. 了解更多
  41. CID 2011756

    Catalog No. A12416
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    PKD 抑制剂
    CID 2011756是一种蛋白激酶D(PKD)抑制剂(PKD2,PKD3和PKD1的IC50值分别为0.6、0.7和3.2μM)。 了解更多
  42. kb NB 142-70

    Catalog No. A12423
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    PKD 抑制剂
    kb NB 142-70是一种选择性蛋白激酶D(PKD)抑制剂(PKD1、2和3的IC50值分别为28.3、58.7和53.2 nM)。 了解更多
  43. CID 755673

    Catalog No. A13804
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    PKD 抑制剂
    CID755673是一种具有细胞活性的泛PKD1/2/3抑制剂,IC50值分别为180 nM,280nM,以及227 nM。 了解更多
  44. CID 797718

    Catalog No. A13809
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    PKD1 抑制剂
    CID797718是CID755673(Adooq目录号A13804)的结构类似物。它是效力降低10倍的PKD1抑制剂,IC50值为7.0+/-0.8 uM。 了解更多
  45. CRT-0066101

    Catalog No. A16318
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    PKD 抑制剂
    CRT-0066101是有效,选择性的蛋白激酶D(PKD)抑制剂;抑制所有PKD同工型(PKD1,PKD3和PKD2的IC50值分别为1、2和2.5 nM)。 了解更多

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