GlpBio

Apoptosis

Apoptosis(凋亡)

FKBP (FK506-binding protein) is one of two major immunophilins and most of FKBP family members bind FK506 and show peptidylprolyl cis/trans isomerase (PPIase) activity. Small size FKBP family members contain only FK506-binding domain, while FKBPs with large molecular weights possess extra domains such as tetratricopeptide repeat domains, calmodulin binding and transmembrane motifs. FKBPs are involved in several biochemical processes including protein folding, receptor signaling, protein trafficking and transcription. FKBP family proteins play important functional roles in the T-cell activation, when complexed with their ligands.

FK506-binding proteins 1a and 1b (FKBP1a/1b) are immunophilin proteins that bind the immunosuppressant agent FK506 and AY 22989. FKBP12 is a ubiquitous abundant protein that acts as a receptor for FK506, binds tightly to intracellular calcium release channels and to the transforming growth factor β (TGF-β) type I receptor.

研究方向

Apoptosis 相关产品(777)

  • GC61776 structure
    GC61776Ingenol 3,20-dibenzoate
    CAS: 59086-90-7
    纯度: >99.00%

    Ingenol3,20-dibenzoate是一种有效的蛋白激酶C(PKC)亚型选择性激动剂。Ingenol3,20-dibenzoate诱导nPKC-delta、-epsilon和-theta和PKC-mu从胞质部分选择性转移到颗粒组分，并通过从头合成大分子诱导形态上典型的凋亡(apoptosis)。Ingenol3,20-dibenzoate可促进NK细胞产生IFN-γ和脱颗粒，尤其是当NSCLC细胞刺激NK细胞时。

  • GC61777 structure
    GC61777RWJ-56110 dihydrochloride
    CAS: 2387505-58-8

    RWJ-56110dihydrochloride是一种有效的、选择性的、拟肽抑制剂，抑制PAR-1激活和内化(结合IC50=0.44uM)，对PAR-2,PAR-3和PAR-4无影响。RWJ-56110dihydrochloride抑制由SFLLRN-NH2 (IC50=0.16μM)和凝血酶(IC50=0.34μM)诱导的血小板聚集，相对于U46619具有相当的选择性。RWJ-56110dihydrochloride在体内阻断血管生成和新血管的形成。RWJ-56110dihydrochloride诱导细胞凋亡(apoptosis)。

  • GC61799 structure
    GC61799Paeoniflorigenone
    CAS: 80454-42-8
    纯度: >98.00%

    Paeoniflorigenone是从牡丹皮中提取的一种有效成分，具有选择性诱导肿瘤细胞凋亡(apoptosis)和抗增殖作用。

  • GC61809 structure
    GC61809Olanzapine D3
    CAS: 786686-79-1
    纯度: >99.00%

    OlanzapineD3(LY170053D3)是Olanzapine的氘代物。Olanzapine是一种选择性单胺能拮抗剂，高亲和力结合5-羟色胺H1，5HT2A/2C，5HT3，5HT6(Ki分别为7、4、11、57和5nM)，多巴胺D1-4(Ki=11-31nM)，毒蕈碱M1-5(Ki=1.9-25nM)和肾上腺素α1受体(Ki=19nM)。Olanzapine是一种非典型的抗精神病剂。

  • GC61865 structure
    GC61865Cearoin
    CAS: 52811-37-7
    纯度: >98.00%

    Cearoin 通过促进 ROS 产生和激活 ERK 来增强自噬 (autophagy) 和诱导细胞凋亡(apoptosis)。

  • GC61896 structure
    GC61896trans-Chalcone
    CAS: 614-47-1

    Trans-Chalcone, the backbone of flavonoids, also is a potent fatty acid synthase (FAS) with IC50 of 17.1 μg/mL, and α-amylase inhibitor, causes cellcycle arrest and induces apoptosis in the breastcancer cell line MCF-7, exerting antifungal and anticancer activities.

  • GC61945 structure
    GC61945PR-924
    CAS: 1416709-79-9

    PR-924 是一种选择性三肽环氧酮免疫蛋白酶亚单位 LMP-7 的抑制剂，IC50 为 22 nM。PR-924 共价修饰蛋白酶体的 N 端苏氨酸活性位点。PR-924 在多发性骨髓瘤细胞中抑制细胞生长并触发凋亡 (apoptosis)，并具有抗肿瘤活性。

  • GC61948 structure
    GC61948Inecalcitol
    CAS: 163217-09-2
    纯度: >98.00%

    Inecalcitol (TX 522) 是一种独特的维生素 D3 类似物，是一种具有口服活性维生素 D 受体 (VDR) 激动剂。Inecalcitol 可诱导细胞凋亡 (apoptosis)，并具有有效的抗癌活性。

  • GC61995 structure
    GC61995PKCβ inhibitor 1
    CAS: 257879-35-9
    纯度: >98.00%

    A PKCβ Inhibitor

  • GC62033 structure
    GC620333α-Hydroxy pravastatin sodium
    CAS: 81093-43-8

    A metabolite of pravastatin

  • GC62104 structure
    GC62104WM-3835
    CAS: 2229025-70-9
    纯度: >98.00%

    WM-3835 is a novel and high-specific small molecule Lysine Acetyltransferase 7 (KAT7, MYST2, HBO1) inhibitor, able to potently suppressed OS cell proliferation and migration, and leads to apoptosis activation.

  • GC62111 structure
    GC62111PND-1186 hydrochloride
    CAS: 1356154-94-3
    纯度: >98.50%

    A potent FAK inhibitor

  • GC62125 structure
    GC62125PD-1/PD-L1-IN-10
    CAS: 2487550-41-2
    纯度: >99.00%

    PD-1/PD-L1-IN-10 (compound B2) 是具有口服活性的 PD-1/PD-L1 抑制剂 (IC50 of 2.7 nM)，具有抗肿瘤活性。

  • GC62164 structure
    GC62164BAY1082439
    CAS: 1375469-38-7
    纯度: >99.00%

    An inhibitor of PI3Kα, PI3Kβ, and PI3Kδ

  • GC62167 structure
    GC62167Fluorizoline
    CAS: 1362243-70-6
    纯度: >99.50%

    Fluorizoline 选择性地直接结合到 prohibitin 1 (PHB1) 和 2 (PHB2)，并诱导凋亡。Fluorizoline 通过上调 NOXA 和 BIM 降低慢性淋巴细胞性白血病 (CLL) 细胞的活力。Fluorizoline 以 p53 非依赖性方式发挥抗肿瘤作用。

  • GC62174 structure
    GC62174ON1231320
    CAS: 1312471-39-8
    纯度: >98.00%

    ON1231320 (7ao), an arylsulfonyl pyrido-pyrimidinone, is a highly specific inhibitor of polo like kinase 2 (PLK2). It also blocks tumor cell cycle progression in the G2/M phase in mitosis and causes apoptosis.

  • GC62191 structure
    GC62191TD52
    CAS: 1798328-24-1
    纯度: >99.00%

    A derivative of erlotinib

  • GC62192 structure
    GC62192COG1410
    CAS: 878009-24-6
    纯度: >98.00%

    COG1410 是一种载脂蛋白 E 的衍生肽。COG1410 在小鼠颅脑损伤 (TBI) 模型中发挥神经保护和抗炎作用。COG1410 可用于神经系统疾病的研究。

  • GC62193 structure
    GC62193(1S,2S)-Bortezomib
    CAS: 1132709-14-8
    纯度: >96.00%

    (1S,2S)-Bortezomib 是 Bortezomib 的对映异构体。Bortezomib 是一种细胞渗透性、可逆性和选择性的蛋白酶体抑制剂，通过靶向苏氨酸残基有效抑制 20S 蛋白酶体 (Ki 为 0.6 nM)。Bortezomib 破坏细胞周期、诱导细胞凋亡以及抑制核因子 NF-κB。Bortezomib 是一种抗癌药物，也是第一种用于人类的蛋白酶体抑制剂。

  • GC62203 structure
    GC62203Falcarindiol
    CAS: 55297-87-5
    纯度: >99.00% / >98.00%

    Falcarindiol (FAD, (3R,8S)-Falcarindiol, FaDOH) is a natural polyacetylene compound found rich in many plants of the Umbelliferae family. Falcarindiol suppresses LPS-stimulated expression of inducible nitric oxide synthase (iNOS), tumor necrosis factor alpha (TNFα), interleukin-6 (IL-6), and interleukin-1 beta (IL-1β). Falcarindiol attenuates the LPS-induced activation of JNK, ERK, STAT1, and STAT3 signaling molecules.

  • GC62222 structure
    GC62222DB2313
    CAS: 2170606-74-1
    纯度: >98.00%

    DB2313是一种强效的转录因子PU.1抑制剂，IC 50 为14nM。

  • GC62242 structure
    GC62242Sideroxylin
    CAS: 3122-87-0

    Sideroxylin 是一种从 Callistemon lanceolatus 中分离的 C-甲基化黄酮，对金黄色葡萄球菌具有抗菌活性。Sideroxylin 可抑制卵巢癌细胞增殖并诱导凋亡 (apoptosis)，导致 DNA 断裂，线粒体膜去极化，产生活性氧 (ROS)。

  • GC62246 structure
    GC62246G5-7
    CAS: 939681-36-4
    纯度: >99.50%

    G5-7 is an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2.

  • GC62252 structure
    GC62252Mefuparib hydrochloride
    CAS: 1449746-00-2
    纯度: >98.00%

    Mefuparib hydrochloride (MPH) 是一种具有口服活性的，底物竞争性和选择性的 PARP1/2 抑制剂，IC50 分别为 3.2 nM 和 1.9 nM。Mefuparib hydrochloride 诱导细胞凋亡 (apoptosis)，并在体内外具有显着的抗癌活性。