Bcl-2
Bcl-2产品
目录号 | 产品描述 | 文献引用 | 实验数据 |
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S1002 |
ABT-737ABT-737是一种BH3模拟抑制剂,作用于Bcl-xL,Bcl-2和Bcl-w,无细胞试验中EC50分别为78.7 nM,30.3 nM和197.8 nM;但对Mcl-1, Bcl-B及Bfl-1没有抑制作用。ABT-737可诱导线粒体通路的凋亡和线粒体自噬。Phase 2。 |
![]() ![]() Cardiomyocytes transduced with or without Ad-Mst1 were treated with ABT-737 (0, 0.1, 1, 10 uM) for 12 hours. Representative immunoblots with antibodies to p62/SQSTM1, LC3 and GAPDH are shown. |
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S1001 |
Navitoclax (ABT-263)Navitoclax (ABT-263)是一种有效的Bcl-xL,Bcl-2和Bcl-w抑制剂,无细胞试验中Ki分别为≤0.5 nM,≤1 nM和≤1 nM,但与Mcl-1和A1结合微弱。Phase 2。 |
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S1121 |
TW-37TW-37是一种新型的非肽类抑制剂,作用于重组Bcl-2,Bcl-xL和Mcl-1,无细胞试验中Ki分别为0.29 μM, 1.11 μM和0.26 μM。 |
![]() ![]() (a) H23 cells exposed for 0–24 h to TW-37 (10 uM) with and without ZVAD.fmk (50 uM) were monitored for apoptotic morphology using electron microscopy (scale bar, 5 mm). % PS positive cells indicate the percentage of apoptotic cells, characterised by PS externalisation.
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S8048 |
Venetoclax (ABT-199)Venetoclax (ABT-199, GDC-0199)是一种Bcl-2选择性抑制剂,无细胞试验中Ki为<0.01 nM,比作用于Bcl-xL和Bcl-w选择性高4800倍以上,对Mcl-1没有抑制活性。有研究证明 Venetoclax 在三阴性乳腺癌 MDA-MB-231 细胞中诱导细胞生长抑制,凋亡,细胞周期停滞和自噬。Phase 3。 |
![]() ![]() THP-1 cells were treated with cytarabine alone and in combination with ABT-199 for 8 h. Whole cell lysates were extracted and subjected to Western blotting, and probed with anti-γH2AX or -β-actin antibody. Densitometry for γH2AX expression was measured, normalized to β-actin, and graphed as fold change compared to the no drug control. The data are presented as mean ± standard error from at least 3 independent Western blots. * indicates p < 0.05.
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S3224New |
CinobufaginCinobufagin (Cinobufagine) 是 Venenum Bufonis 的活性成分,可抑制肿瘤发展。Cinobufagin 可提高 ATM 和 Chk2 并降低 CDC25C、CDK1 和 cyclin B。Cinobufagin 抑制 PI3K、AKT 和 Bcl-2,同时增加裂解的 caspase-9 和 caspase-3 水平。由此诱导细胞周期停滞在G2/M期及凋亡。 |
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S6852New |
GossypolGossypol (BL 193) 是一种从棉籽和根中分离出来的口服活性的多酚。Gossypol 是一种 5α-reductase 1 和 3α-hydroxysteroid dehydrogenase 的有效抑制剂,在无细胞试验中,对应的IC50值分别为3.33 μM和0.52 μM。Gossypol 还可抑制BH3肽与Bcl蛋白的结合,对 Bcl-XL 和 Bcl-2 的IC50值分别为0.4 μM和10 μM。Gossypol 在各种癌细胞中可诱导凋亡和细胞的生长抑制。 |
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S9665New |
Motixafortide (BL-8040)Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) 是一种 CXCR4 的拮抗剂,IC50值约为1 nM。BL-8040 通过改变的miR-15a/16-1的表达,下调 ERK、BCL-2、MCL-1 和 cyclin-D1,诱导AML胚的凋亡。 |
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S8924New |
DT2216DT2216 is a potent and selective degrader of BCL-XL based on PROTAC technology. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets. |
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S8758New |
VU661013VU661013 是一种新型有效的选择性的 MCL1 的抑制剂,在TR-FRET分析中,对人MCL-1的Ki值为97±30 pM的。但是 VU661013 不会显著地抑制BCL-xL或BCL-2,对应的Ki值 > 40μM 或 = 0.73μM。VU661013 可破坏了 BIM/MCL-1 联合的稳定性,可在AML中导致凋亡。 |
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S2812 |
(R)-(-)-Gossypol acetic acid(R)-(-)-Gossypol (AT-101) acetic acid 是醋酸棉酚的R-(-)对映体,与Bcl-2,Bcl-xL和Mcl-1结合,无细胞试验中Ki为0.32 μM,0.48 μM 和 0.18 μM;不抑制BIR3域和BID。AT-101 可同时诱导凋亡和一种细胞保护性的自噬。Phase 2。 |
![]() ![]() (B and C) assessment of antimigration capacity in each group by transwell migration assay. Abbreviations: CDDP, cisplatin; DMSO, dimethyl sulfoxide. |
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S1071 |
HA14-1HA14-1是一种Bcl-2表面口袋的非肽配体,IC50为9 μM左右。 |
![]() ![]() ABT-737, Obatoclax, and HA14-1 eradicated the H1975 early tumor prosurvival resistance against dual-TKIs inhibition by erlotinib/SU11274 (ERL/SU). The experiment was carried out with H1975 cells , cells were pretreated with dual EGFR-MET inhibitors here, i.e., erlotinib (1 μmol/L)/SU11274 (1 μmol/L). BH3-mimetic used in treatment days 7-9 were all 2 μmol/L in concentration. Top, crystal violet cell survival staining assay. Bottom, BH3-mimetic treatment of the dual ERL/SU-resistant tumor cells induced a proapoptotic response. |
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S2606 |
MifepristoneMifepristone (RU486, C-1073) 是一种异常活跃的孕激素受体 progesterone receptor 和糖皮质激素受体 glucocorticoid receptor 拮抗剂,IC50分别为0.2 nM和2.6 nM。Mifepristone 可促进细胞自噬和细胞凋亡,降低 Bcl-2 表达水平而增加Beclin1水平,并伴随Bcl-2和Beclin1之间的相互作用减弱。 |
![]() ![]() Myogenic differentiation assay to determine the GR specificity of DEX by using RU-486 (10 uM). Immunofluorescence detection of MyHC (red) and DAPI counterstaining of nuclei (blue) was used to detect myotubes. The scale bar is 50 um.
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S8061 |
SabutoclaxSabutoclax (BI-97C1) 是一种pan-Bcl-2抑制剂,作用于Bcl-xL, Bcl-2, Mcl-1和Bfl-1,IC50分别为0.31 μM, 0.32 μM, 0.20 μM和0.62 μM。 |
![]() ![]() (e) Abs (490 nm) was measured by MTS assay in siControl or siPTBP1 treated PC3 cells with DMSO, 1000 nM ABT737, or 100 nM Sabutoclax for 48 h, showing no significant change in cell viability following siPTBP1 treatment in DMSO control, ABT737, or Sabutoclax treated cells. (f) PC3 cells transfected with siControl or a mixture of two siPTBP1 were treated with 1000 nM ABT737 or 100 nM Sabutoclax combined with various doses of docetaxel for 48 h and cell viability was assessed by MTS assay. The viability of cells with 1000 nM ABT737 or 100 nM Sabutoclax alone was set as 100%. All data are presented as mean±S.E.M., n=3. The statistical significance was determined by unpaired student t-test where *P<0.05; **P<0.01; ***P<0.001.
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S8820 |
PTC596PTC596是第二代BMI-1抑制剂,可加速BMI-1的降解。PTC596 可下调 MCL-1 并诱导p53依赖性的线粒体的凋亡。处理套细胞淋巴瘤细胞72小时,IC50为68-340 nM。 |
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S8643 |
AZD5991AZD5991是MCL-1抑制剂,Ki值为0.13 nM。AZD5991对小鼠源Mcl-1的结合亲和力比对人源Mcl-1低25倍,而之比对大鼠源Mcl-1的亲和力低4倍。 |
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S7790 |
A-1210477A-1210477是一种有效的选择性MCL-1抑制剂,Ki和IC50分别为0.454 nM 和 26.2 nM,选择性比作用于其他Bcl-2家族成员高100多倍。 |
![]() ![]() U251 glioblastoma (F) or MeWo melanoma (G) cells were treated with selective BH-3 mimetics, GTPP or the combination of both for 24 h (U251) or 48 h (MeWo). Thereafter, cells were stained with annexin V and propidium iodide and analyzed by flow cytometry. Shown are representative flow plots.
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S8759 |
S55746S55746 (S 055746,BCL201)是一种新型的、具有口服活性的BCL-2特异性抑制剂,Ki值为1.3 nM。它对Bcl-XL的亲和力弱,而对MCL-1、BFL-1(BCL2A1/A1)没有显著结合。S55746对BCL-2的选择性是对BCL-XL的70-400倍。 |
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S2271 |
Berberine chlorideBerberine chloride 是异喹啉类生物碱的季铵盐。Berberine chloride 可激活 caspase 3 和 caspase 8,分裂 poly ADP-ribose polymerase (PARP) 和释放 cytochrome c。Berberine chloride 可降低 c-IAP1,Bcl-2 和 Bcl-XL 的表达。Berberine chloride 可通过 JNK 和 p38 MAPK 的持续磷酸化以及产生 ROS 来诱导凋亡。Berberine chloride 是一个 topoisomerase I 和 II 的双效抑制剂。Berberine chloride 也是一个潜在的自噬调节剂。 |
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S2448 |
Gambogic AcidGambogic Acid (Guttatic, Guttic) 激活caspases,EC50为0.78 - 1.64 μM,且完全抑制Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 和 Mcl-1,IC50分别为1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM 和 0.79 μM。 |
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S8383 |
S63845S63845是一种新型的、选择性的MCL-1抑制剂,Kd值为0.19 nM。对其他Bcl-2成员,如Bcl-2或Bcl-xL,没有明显结合能力。 |
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S5600 |
Flavokawain AFlavokawain A 是一种从 kava 提取的凋亡诱导剂和抗癌剂。 Flavokawain A 可以下调抗凋亡蛋白,例如 XIAP、 survivin 和 Bcl-xL,从而改变凋亡与抗凋亡分子之间的平衡、诱导肿瘤细胞死亡。 |
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S8177 |
BH3I-1BH3I-1是Bcl-XL-BH3 domain interaction抑制剂,Ki值为2.4 μM。它是一种Bcl-2家族蛋白的选择性抑制剂。 |
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S8865 |
BAI1BAI1是一种直接的BAX变构抑制剂,Kd值为15.0 ± 4 μM。 |
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S7800 |
A-1155463A-1155463是一种高度有效、选择性的BCL-XL抑制剂。其对BCL-XL的亲和力属于皮摩尔级别,对BCL-2、BCL-W(Ki=19 nM)、MCL-1(Ki>440 nM)的结合比对BCL-XL弱1000倍以上。 |
![]() ![]() Tumor growth rate (TGR) of tumors orthotopically implanted in rats on day 3, 7 and 10 compared to day 0. Rats were treated with doxorubicin, A-1155463 or a combination. Treatment with A-1155463 resulted in a significant decrease in TGR compared to control mice.
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S7801 |
A-1331852A-1331852是一种有效的、选择性的BCL-XL抑制剂,对Bcl-xL的Ki值小于0.01 nM,对Bcl-2, Bcl-W, MCL-1的Ki值分别为6 nM, 4 nM, 142 nM。它可能在治疗癌症、免疫和自体免疫疾病中有所作用。 |
![]() ![]() Cells were treated with 0.5 μM A-1331852 and 1.5 nM VCR (RD), 0.5 nM VCR (RH30) for 72 h. Apoptosis was determined by analysis of DNA fragmentation of PI-stained nuclei using flow cytometry. Mean and SD of three independent experiments performed in triplicate are shown; **P < 0.01.
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S7531 |
UMI-77UMI-77是一种选择性Mcl-1抑制剂,Ki为490 nM,表现出高于Bcl-2家族其它成员的选择性。 |
![]() ![]() U87 and A172 cells were treated with UMI-77 (8 μM) for 24h and further treated with TRAIL (30 ng/ml) for indicated period of time. Levels of apoptosis-associated proteins were analyzed by Western blot. GAPDH was used as a loading control. |
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S8836 |
S64315 (MIK665)S64315 (MIK665)是Mcl的抑制剂,Ki值为1.2 nM。它具有潜在的促凋亡和抗肿瘤活性。 |
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S6990New |
PhytohemagglutininPhytohemagglutinin (PHA, Phaseolus vulgaris agglutinin) 在毕赤酵母中利用天然信号肽或酿酒酵母α-因子前体序列表达,将蛋白质引导至分泌途径。Phytohemagglutinin 可通过增加凋亡蛋白 Bax 和激活 caspases-3 来诱导人HEp-2癌细胞的凋亡。 |
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S3238New |
ResibufogeninResibufogenin (Bufogenin, Recibufogenin) 是huachansu华蟾素中具有抗癌作用的成分,通过上调 receptor-interacting protein kinase 3 (RIP3) 和磷酸化 mixed lineage kinase domain-like protein 的Ser358位点来触发坏死病。Resibufogenin 可通过诱导 reactive oxygen species (ROS) 积累发挥细胞毒性作用。Resibufogenin 可诱导凋亡和 caspase-3 和 caspase-8 活性。Resibufogenin 增加 Bax/Bcl-2 表达,并抑制 cyclin D1、cyclin E、PI3K、p-AKT、p-GSK3β 和 β-catenin 的蛋白表达。 |
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S3275New |
Senkyunolide ISenkyunolide I (SEI, SENI) 是一种从 Ligusticum chuanxiong 中提取的口服活性化合物,具有止痛、抗偏头痛、神经保护、抗氧化和抗凋亡的活性。Senkyunolide I (SEI, SENI) 可上调 Erk1/2 的磷酸化,并诱导 Nrf2 的核易位,伴随着HO-1和NQO1的表达增强。Senkyunolide I (SEI, SENI) 可提高 Bcl-2/Bax 的比例,并抑制裂化的 caspase 3 和 caspase 9 的表达。 |
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S7105 |
BAM7BAM7是一种直接的,选择性的促凋亡Bax激动剂,EC50为3.3 μM。 |
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S8650 |
BTSA1BTSA1是BAX激活剂,与其N端激活位点以高亲和力和特异性结合,诱导BAX发生构象变化,引起BAC介导的凋亡反应。BTSA1在白血病细胞系和病患样本中有效地促进凋亡,而不影响健康细胞。 |
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S7747 |
Ro-3306RO-3306是一种ATP竞争性的选择性 CDK1 抑制剂,Ki 为20 nM,选择性是其他各种人类激酶的15倍多。RO-3306可增强p53介导的 Bax 激活和线粒体的凋亡。 |
![]() ![]() HeLa cells were untreated or treated with either colcemid (10 μg/ml for 16 h), RO-3306 (9 μM for 16 h), or both colcemid and RO-3306, as indicated. Cells were then lysed, and proteins were detected by Western analysis.
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S9276 |
Alisol BAlisol B, a triterpene from Alismatis rhizoma, induces Bax up-regulation and nuclear translocation, the activation of initiator caspase-8 and caspase-9, and executor caspase-3, suggesting the involvement of both extrinsic and intrinsic apoptosis pathways. |
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S5550 |
Ethyl gallateEthyl gallat (Phyllemblin, gallic acid ethyl ester), which could be found naturally in a variety of plant sources, is a food additive with antimicrobial activity. |
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S1057 |
Obatoclax Mesylate (GX15-070)Obatoclax Mesylate (GX15-070)是一种Bcl-2拮抗剂,无细胞试验中Ki为0.22 μM,可以协助抑制MCL-1介导的抗细胞凋亡作用。Phase 3。 |
![]() ![]() In vivo antitumor efficacies of AZD2281 and GX15-070 alone or in combination in a BxPC-3 xenograft model. Tumor specimens were fixed in 10% formalin, embedded in paraffin, and cut into 4 lm-thick slides for H&E, PCNA, and CD34 staining.
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S7100New |
WEHI-539 HClWEHI-539 HCl (WEHI-539 hydrochloride) 对BCL-XL具有高亲和力(IC50=1.1 nM)和选择性,能有效地杀伤细胞。它对Bcl-XL的亲和性是对其他BCL-2家族成员的400倍。 |
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S7849 |
BDA-366BDA-366是Bcl2-BH4的小分子拮抗剂,能与BH4高亲和力、高选择性地结合。它与Bcl2直接高亲和力结合,Ki值为3.3 ± 0.73 nM。 |
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S7126 |
Marinopyrrole A (Maritoclax)Marinopyrrole A (Maritoclax)是一种选择性的Mcl-1拮抗剂。它能够结合Mcl-1,而不是Bcl-XL,引起其发生蛋白酶体降解。Maritoclax能够破坏Bim和Mcl-1的相互作用,IC50为10.1 μM。 |
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S3245New |
NodakenetinNodakenetin (NANI) 是从Angelica decursiva中分离出的植物性香豆素,可抑制 α-glucosidase、PTP1B、rat lens aldose reductase (RLAR)、AChE、BChE 和 β-site amyloid precursor protein cleaving enzyme 1 (BACE1)。Nodakenetin 可改变 Bax 和 Bcl-2 的蛋白质表达,并促进线粒体凋亡。Nodakenetin 具有抗肿瘤活性。 |
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S3267New |
Kaempferol-3-O-rutinosideKaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-rutinoside) 是从 Carthamus tinctorius 中提取的黄酮,可改变受伤神经元的形状和结构,减少凋亡细胞,下调 p-JAK2、p-STAT3、caspase-3 和 Bax 的表达,并降低Bax免疫反应性,并增加 Bcl-2 蛋白表达和免疫反应性。 |
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S8199 |
LTX-315 (Ruxotemitide)LTX-315 (Ruxotemitide, Oncopore)是一种溶瘤肽,能通过Bax/Bak所调节的线体膜透化杀死癌细胞。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
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S1002 |
ABT-737ABT-737是一种BH3模拟抑制剂,作用于Bcl-xL,Bcl-2和Bcl-w,无细胞试验中EC50分别为78.7 nM,30.3 nM和197.8 nM;但对Mcl-1, Bcl-B及Bfl-1没有抑制作用。ABT-737可诱导线粒体通路的凋亡和线粒体自噬。Phase 2。 |
![]() ![]() Cardiomyocytes transduced with or without Ad-Mst1 were treated with ABT-737 (0, 0.1, 1, 10 uM) for 12 hours. Representative immunoblots with antibodies to p62/SQSTM1, LC3 and GAPDH are shown. |
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S1001 |
Navitoclax (ABT-263)Navitoclax (ABT-263)是一种有效的Bcl-xL,Bcl-2和Bcl-w抑制剂,无细胞试验中Ki分别为≤0.5 nM,≤1 nM和≤1 nM,但与Mcl-1和A1结合微弱。Phase 2。 |
![]() ![]() |
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S1121 |
TW-37TW-37是一种新型的非肽类抑制剂,作用于重组Bcl-2,Bcl-xL和Mcl-1,无细胞试验中Ki分别为0.29 μM, 1.11 μM和0.26 μM。 |
![]() ![]() (a) H23 cells exposed for 0–24 h to TW-37 (10 uM) with and without ZVAD.fmk (50 uM) were monitored for apoptotic morphology using electron microscopy (scale bar, 5 mm). % PS positive cells indicate the percentage of apoptotic cells, characterised by PS externalisation.
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S8048 |
Venetoclax (ABT-199)Venetoclax (ABT-199, GDC-0199)是一种Bcl-2选择性抑制剂,无细胞试验中Ki为<0.01 nM,比作用于Bcl-xL和Bcl-w选择性高4800倍以上,对Mcl-1没有抑制活性。有研究证明 Venetoclax 在三阴性乳腺癌 MDA-MB-231 细胞中诱导细胞生长抑制,凋亡,细胞周期停滞和自噬。Phase 3。 |
![]() ![]() THP-1 cells were treated with cytarabine alone and in combination with ABT-199 for 8 h. Whole cell lysates were extracted and subjected to Western blotting, and probed with anti-γH2AX or -β-actin antibody. Densitometry for γH2AX expression was measured, normalized to β-actin, and graphed as fold change compared to the no drug control. The data are presented as mean ± standard error from at least 3 independent Western blots. * indicates p < 0.05.
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S3224New |
CinobufaginCinobufagin (Cinobufagine) 是 Venenum Bufonis 的活性成分,可抑制肿瘤发展。Cinobufagin 可提高 ATM 和 Chk2 并降低 CDC25C、CDK1 和 cyclin B。Cinobufagin 抑制 PI3K、AKT 和 Bcl-2,同时增加裂解的 caspase-9 和 caspase-3 水平。由此诱导细胞周期停滞在G2/M期及凋亡。 |
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S6852New |
GossypolGossypol (BL 193) 是一种从棉籽和根中分离出来的口服活性的多酚。Gossypol 是一种 5α-reductase 1 和 3α-hydroxysteroid dehydrogenase 的有效抑制剂,在无细胞试验中,对应的IC50值分别为3.33 μM和0.52 μM。Gossypol 还可抑制BH3肽与Bcl蛋白的结合,对 Bcl-XL 和 Bcl-2 的IC50值分别为0.4 μM和10 μM。Gossypol 在各种癌细胞中可诱导凋亡和细胞的生长抑制。 |
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S9665New |
Motixafortide (BL-8040)Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) 是一种 CXCR4 的拮抗剂,IC50值约为1 nM。BL-8040 通过改变的miR-15a/16-1的表达,下调 ERK、BCL-2、MCL-1 和 cyclin-D1,诱导AML胚的凋亡。 |
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S8924New |
DT2216DT2216 is a potent and selective degrader of BCL-XL based on PROTAC technology. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets. |
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S8758New |
VU661013VU661013 是一种新型有效的选择性的 MCL1 的抑制剂,在TR-FRET分析中,对人MCL-1的Ki值为97±30 pM的。但是 VU661013 不会显著地抑制BCL-xL或BCL-2,对应的Ki值 > 40μM 或 = 0.73μM。VU661013 可破坏了 BIM/MCL-1 联合的稳定性,可在AML中导致凋亡。 |
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S2812 |
(R)-(-)-Gossypol acetic acid(R)-(-)-Gossypol (AT-101) acetic acid 是醋酸棉酚的R-(-)对映体,与Bcl-2,Bcl-xL和Mcl-1结合,无细胞试验中Ki为0.32 μM,0.48 μM 和 0.18 μM;不抑制BIR3域和BID。AT-101 可同时诱导凋亡和一种细胞保护性的自噬。Phase 2。 |
![]() ![]() (B and C) assessment of antimigration capacity in each group by transwell migration assay. Abbreviations: CDDP, cisplatin; DMSO, dimethyl sulfoxide. |
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S1071 |
HA14-1HA14-1是一种Bcl-2表面口袋的非肽配体,IC50为9 μM左右。 |
![]() ![]() ABT-737, Obatoclax, and HA14-1 eradicated the H1975 early tumor prosurvival resistance against dual-TKIs inhibition by erlotinib/SU11274 (ERL/SU). The experiment was carried out with H1975 cells , cells were pretreated with dual EGFR-MET inhibitors here, i.e., erlotinib (1 μmol/L)/SU11274 (1 μmol/L). BH3-mimetic used in treatment days 7-9 were all 2 μmol/L in concentration. Top, crystal violet cell survival staining assay. Bottom, BH3-mimetic treatment of the dual ERL/SU-resistant tumor cells induced a proapoptotic response. |
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S2606 |
MifepristoneMifepristone (RU486, C-1073) 是一种异常活跃的孕激素受体 progesterone receptor 和糖皮质激素受体 glucocorticoid receptor 拮抗剂,IC50分别为0.2 nM和2.6 nM。Mifepristone 可促进细胞自噬和细胞凋亡,降低 Bcl-2 表达水平而增加Beclin1水平,并伴随Bcl-2和Beclin1之间的相互作用减弱。 |
![]() ![]() Myogenic differentiation assay to determine the GR specificity of DEX by using RU-486 (10 uM). Immunofluorescence detection of MyHC (red) and DAPI counterstaining of nuclei (blue) was used to detect myotubes. The scale bar is 50 um.
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S8061 |
SabutoclaxSabutoclax (BI-97C1) 是一种pan-Bcl-2抑制剂,作用于Bcl-xL, Bcl-2, Mcl-1和Bfl-1,IC50分别为0.31 μM, 0.32 μM, 0.20 μM和0.62 μM。 |
![]() ![]() (e) Abs (490 nm) was measured by MTS assay in siControl or siPTBP1 treated PC3 cells with DMSO, 1000 nM ABT737, or 100 nM Sabutoclax for 48 h, showing no significant change in cell viability following siPTBP1 treatment in DMSO control, ABT737, or Sabutoclax treated cells. (f) PC3 cells transfected with siControl or a mixture of two siPTBP1 were treated with 1000 nM ABT737 or 100 nM Sabutoclax combined with various doses of docetaxel for 48 h and cell viability was assessed by MTS assay. The viability of cells with 1000 nM ABT737 or 100 nM Sabutoclax alone was set as 100%. All data are presented as mean±S.E.M., n=3. The statistical significance was determined by unpaired student t-test where *P<0.05; **P<0.01; ***P<0.001.
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S8820 |
PTC596PTC596是第二代BMI-1抑制剂,可加速BMI-1的降解。PTC596 可下调 MCL-1 并诱导p53依赖性的线粒体的凋亡。处理套细胞淋巴瘤细胞72小时,IC50为68-340 nM。 |
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S8643 |
AZD5991AZD5991是MCL-1抑制剂,Ki值为0.13 nM。AZD5991对小鼠源Mcl-1的结合亲和力比对人源Mcl-1低25倍,而之比对大鼠源Mcl-1的亲和力低4倍。 |
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S7790 |
A-1210477A-1210477是一种有效的选择性MCL-1抑制剂,Ki和IC50分别为0.454 nM 和 26.2 nM,选择性比作用于其他Bcl-2家族成员高100多倍。 |
![]() ![]() U251 glioblastoma (F) or MeWo melanoma (G) cells were treated with selective BH-3 mimetics, GTPP or the combination of both for 24 h (U251) or 48 h (MeWo). Thereafter, cells were stained with annexin V and propidium iodide and analyzed by flow cytometry. Shown are representative flow plots.
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S8759 |
S55746S55746 (S 055746,BCL201)是一种新型的、具有口服活性的BCL-2特异性抑制剂,Ki值为1.3 nM。它对Bcl-XL的亲和力弱,而对MCL-1、BFL-1(BCL2A1/A1)没有显著结合。S55746对BCL-2的选择性是对BCL-XL的70-400倍。 |
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S2271 |
Berberine chlorideBerberine chloride 是异喹啉类生物碱的季铵盐。Berberine chloride 可激活 caspase 3 和 caspase 8,分裂 poly ADP-ribose polymerase (PARP) 和释放 cytochrome c。Berberine chloride 可降低 c-IAP1,Bcl-2 和 Bcl-XL 的表达。Berberine chloride 可通过 JNK 和 p38 MAPK 的持续磷酸化以及产生 ROS 来诱导凋亡。Berberine chloride 是一个 topoisomerase I 和 II 的双效抑制剂。Berberine chloride 也是一个潜在的自噬调节剂。 |
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S2448 |
Gambogic AcidGambogic Acid (Guttatic, Guttic) 激活caspases,EC50为0.78 - 1.64 μM,且完全抑制Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 和 Mcl-1,IC50分别为1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM 和 0.79 μM。 |
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S8383 |
S63845S63845是一种新型的、选择性的MCL-1抑制剂,Kd值为0.19 nM。对其他Bcl-2成员,如Bcl-2或Bcl-xL,没有明显结合能力。 |
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S5600 |
Flavokawain AFlavokawain A 是一种从 kava 提取的凋亡诱导剂和抗癌剂。 Flavokawain A 可以下调抗凋亡蛋白,例如 XIAP、 survivin 和 Bcl-xL,从而改变凋亡与抗凋亡分子之间的平衡、诱导肿瘤细胞死亡。 |
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S8177 |
BH3I-1BH3I-1是Bcl-XL-BH3 domain interaction抑制剂,Ki值为2.4 μM。它是一种Bcl-2家族蛋白的选择性抑制剂。 |
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S8865 |
BAI1BAI1是一种直接的BAX变构抑制剂,Kd值为15.0 ± 4 μM。 |
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S7800 |
A-1155463A-1155463是一种高度有效、选择性的BCL-XL抑制剂。其对BCL-XL的亲和力属于皮摩尔级别,对BCL-2、BCL-W(Ki=19 nM)、MCL-1(Ki>440 nM)的结合比对BCL-XL弱1000倍以上。 |
![]() ![]() Tumor growth rate (TGR) of tumors orthotopically implanted in rats on day 3, 7 and 10 compared to day 0. Rats were treated with doxorubicin, A-1155463 or a combination. Treatment with A-1155463 resulted in a significant decrease in TGR compared to control mice.
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S7801 |
A-1331852A-1331852是一种有效的、选择性的BCL-XL抑制剂,对Bcl-xL的Ki值小于0.01 nM,对Bcl-2, Bcl-W, MCL-1的Ki值分别为6 nM, 4 nM, 142 nM。它可能在治疗癌症、免疫和自体免疫疾病中有所作用。 |
![]() ![]() Cells were treated with 0.5 μM A-1331852 and 1.5 nM VCR (RD), 0.5 nM VCR (RH30) for 72 h. Apoptosis was determined by analysis of DNA fragmentation of PI-stained nuclei using flow cytometry. Mean and SD of three independent experiments performed in triplicate are shown; **P < 0.01.
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S7531 |
UMI-77UMI-77是一种选择性Mcl-1抑制剂,Ki为490 nM,表现出高于Bcl-2家族其它成员的选择性。 |
![]() ![]() U87 and A172 cells were treated with UMI-77 (8 μM) for 24h and further treated with TRAIL (30 ng/ml) for indicated period of time. Levels of apoptosis-associated proteins were analyzed by Western blot. GAPDH was used as a loading control. |
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S8836 |
S64315 (MIK665)S64315 (MIK665)是Mcl的抑制剂,Ki值为1.2 nM。它具有潜在的促凋亡和抗肿瘤活性。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
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S6990New |
PhytohemagglutininPhytohemagglutinin (PHA, Phaseolus vulgaris agglutinin) 在毕赤酵母中利用天然信号肽或酿酒酵母α-因子前体序列表达,将蛋白质引导至分泌途径。Phytohemagglutinin 可通过增加凋亡蛋白 Bax 和激活 caspases-3 来诱导人HEp-2癌细胞的凋亡。 |
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S3238New |
ResibufogeninResibufogenin (Bufogenin, Recibufogenin) 是huachansu华蟾素中具有抗癌作用的成分,通过上调 receptor-interacting protein kinase 3 (RIP3) 和磷酸化 mixed lineage kinase domain-like protein 的Ser358位点来触发坏死病。Resibufogenin 可通过诱导 reactive oxygen species (ROS) 积累发挥细胞毒性作用。Resibufogenin 可诱导凋亡和 caspase-3 和 caspase-8 活性。Resibufogenin 增加 Bax/Bcl-2 表达,并抑制 cyclin D1、cyclin E、PI3K、p-AKT、p-GSK3β 和 β-catenin 的蛋白表达。 |
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S3275New |
Senkyunolide ISenkyunolide I (SEI, SENI) 是一种从 Ligusticum chuanxiong 中提取的口服活性化合物,具有止痛、抗偏头痛、神经保护、抗氧化和抗凋亡的活性。Senkyunolide I (SEI, SENI) 可上调 Erk1/2 的磷酸化,并诱导 Nrf2 的核易位,伴随着HO-1和NQO1的表达增强。Senkyunolide I (SEI, SENI) 可提高 Bcl-2/Bax 的比例,并抑制裂化的 caspase 3 和 caspase 9 的表达。 |
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S7105 |
BAM7BAM7是一种直接的,选择性的促凋亡Bax激动剂,EC50为3.3 μM。 |
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S8650 |
BTSA1BTSA1是BAX激活剂,与其N端激活位点以高亲和力和特异性结合,诱导BAX发生构象变化,引起BAC介导的凋亡反应。BTSA1在白血病细胞系和病患样本中有效地促进凋亡,而不影响健康细胞。 |
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S7747 |
Ro-3306RO-3306是一种ATP竞争性的选择性 CDK1 抑制剂,Ki 为20 nM,选择性是其他各种人类激酶的15倍多。RO-3306可增强p53介导的 Bax 激活和线粒体的凋亡。 |
![]() ![]() HeLa cells were untreated or treated with either colcemid (10 μg/ml for 16 h), RO-3306 (9 μM for 16 h), or both colcemid and RO-3306, as indicated. Cells were then lysed, and proteins were detected by Western analysis.
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S9276 |
Alisol BAlisol B, a triterpene from Alismatis rhizoma, induces Bax up-regulation and nuclear translocation, the activation of initiator caspase-8 and caspase-9, and executor caspase-3, suggesting the involvement of both extrinsic and intrinsic apoptosis pathways. |
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S5550 |
Ethyl gallateEthyl gallat (Phyllemblin, gallic acid ethyl ester), which could be found naturally in a variety of plant sources, is a food additive with antimicrobial activity. |
目录号 | 产品描述 | 文献引用 | 实验数据 |
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S1057 |
Obatoclax Mesylate (GX15-070)Obatoclax Mesylate (GX15-070)是一种Bcl-2拮抗剂,无细胞试验中Ki为0.22 μM,可以协助抑制MCL-1介导的抗细胞凋亡作用。Phase 3。 |
![]() ![]() In vivo antitumor efficacies of AZD2281 and GX15-070 alone or in combination in a BxPC-3 xenograft model. Tumor specimens were fixed in 10% formalin, embedded in paraffin, and cut into 4 lm-thick slides for H&E, PCNA, and CD34 staining.
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S7100New |
WEHI-539 HClWEHI-539 HCl (WEHI-539 hydrochloride) 对BCL-XL具有高亲和力(IC50=1.1 nM)和选择性,能有效地杀伤细胞。它对Bcl-XL的亲和性是对其他BCL-2家族成员的400倍。 |
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S7849 |
BDA-366BDA-366是Bcl2-BH4的小分子拮抗剂,能与BH4高亲和力、高选择性地结合。它与Bcl2直接高亲和力结合,Ki值为3.3 ± 0.73 nM。 |
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S7126 |
Marinopyrrole A (Maritoclax)Marinopyrrole A (Maritoclax)是一种选择性的Mcl-1拮抗剂。它能够结合Mcl-1,而不是Bcl-XL,引起其发生蛋白酶体降解。Maritoclax能够破坏Bim和Mcl-1的相互作用,IC50为10.1 μM。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
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S3245New |
NodakenetinNodakenetin (NANI) 是从Angelica decursiva中分离出的植物性香豆素,可抑制 α-glucosidase、PTP1B、rat lens aldose reductase (RLAR)、AChE、BChE 和 β-site amyloid precursor protein cleaving enzyme 1 (BACE1)。Nodakenetin 可改变 Bax 和 Bcl-2 的蛋白质表达,并促进线粒体凋亡。Nodakenetin 具有抗肿瘤活性。 |
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S3267New |
Kaempferol-3-O-rutinosideKaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-rutinoside) 是从 Carthamus tinctorius 中提取的黄酮,可改变受伤神经元的形状和结构,减少凋亡细胞,下调 p-JAK2、p-STAT3、caspase-3 和 Bax 的表达,并降低Bax免疫反应性,并增加 Bcl-2 蛋白表达和免疫反应性。 |
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S8199 |
LTX-315 (Ruxotemitide)LTX-315 (Ruxotemitide, Oncopore)是一种溶瘤肽,能通过Bax/Bak所调节的线体膜透化杀死癌细胞。 |