Caspase

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研究领域

抑制剂选择性比较

特异性亚型抑制剂

Caspase产品

所有产品 Caspase抑制剂(15) Caspase激活剂(17) Caspase调节剂(2)

目录号	产品描述	文献引用	实验数据
S2228	Belnacasan (VX-765) Belnacasan (VX-765)是一种有效的选择性caspase-1抑制剂，无细胞试验中K_i为0.8 nM。Phase 2。	Cell, 2020, 30;181(3):637-652.e15. Cell, 2020, 30;181(3):637-652e15 EMBO J, 2020, 18;39(10):e103758	(D and E) Caspase-1 inhibitors (Ac-YVAD-CMK and VX765) were added during the induction of trastuzumab-dependent BT-474 (red) or rituximab-dependent Raji cell phagocytosis (green). MFI of PD-L1 (D) and IDO (E) in macrophages are as indicated.
S3267^New	Kaempferol-3-O-rutinoside Kaempferol-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。
S3275^New	Senkyunolide I Senkyunolide 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。
S2417	20-Hydroxyecdysone 20-Hydroxyecdysone (Ecdysterone, 20E, B-ecdysone, Commisterone) 是一种自然发生的蜕皮激素，控制节肢动物的蜕皮和变态。20-Hydroxyecdysone (Ecdysterone, 20E) 可抑制 caspase 活性并通过20E核受体复合体 EcR-USP 来诱导自噬。
S7023	Z-VAD-FMK Z-VAD-FMK是一种细胞渗透性的，不可逆泛caspase抑制剂，在THP.1 和 Jurkat T细胞中阻断细胞凋亡的所有特性。	Nature, 2020, 577(7788):109-114 Cell, 2020, 19;180(6):1081-1097.e24. cell, 2020, 180(1):64-78.e16	(A and B) Western blot analysis examining the effect of zVAD-fmk on the icaritin-induced apoptosis. The caspase inhibitor zVAD-fmk could significantly decrease the icaritin-induced cleaved caspase-3 expression. β-Actin protein levels indicate that an equal amount of protein was loaded into each lane.n=3. Mean±SD. bP<0.05, compared to the control group. eP<0.05, compared to the icaritin-treated group.
S7314	Z-IETD-FMK Z-IETD-FMK是一种特异性Caspase-8抑制剂。	Cell Host Microbe, 2020, 8;27(4):556-570 e6 Biochem Pharmacol, 2020, 10.1016/j.bcp.2020.113914 Biomolecules, 2020, 10(2)	The caspase-8 inhibitors do not rescue NB4 cells from TPEN-triggered apoptosis. NB4 cells were pre-treated with 50 μM Z-ITED-FMK or 100 μM Ac-IETD-CHO for 1 h, and then treated with 5 μM TPEN for 24 h. (A) Cell morphology was observed and recorded using an optical microscope. The scale bar represents 20 μm. A partiallty enlarged view was shown in the lower left corner of every picture. (B) Apoptosis rate was measured with Annexin V/PI dual staining by flow cytometry.
S7313	Z-LEHD-FMK Z-LEHD-FMK (Caspase-9 Inhibitor) 是一种具有细胞透性、不可逆的Caspase-9抑制剂，有助于细胞生存。	Cell Death Dis, 2020, 27;11(4):295 Acta Pharmacol Sin, 2020, 26 Cancers (Basel), 2019, 11(9)
S7312	Z-DEVD-FMK Z-DEVD-FMK是一种特异性，不可逆的Caspase-3抑制剂，也能有效抑制caspase-6， caspase-7， caspase-8和caspase-10。	Cell, 2020, 19;180(6):1081-1097.e24 Cancer Res, 2020, 10.1158/0008-5472.CAN-19-1784 Cell Rep, 2020, 19;31(7):107667	(J,K)After pre-treated with Caspase-3 inhibitor Z-DEVD-FMK 50μM, the apoptotic rates of cells induced by E Platinum in BGC-823, MGC-803, and SGC-7901 cells were detected by Annexin V/PI double-staining assay. Ann.V-/PI- as healthy cells, Ann.+/PI- as early apoptotic cells, Ann.+/PI+ probably as late apoptotic cells. Data were shown as means SD for three independent experiments (P<0.05 and *P<0.01 compared with control, ##P<0.01 compared to Z-DEVD-FMK+40 μM E Platinum group with treatment of 40 μM E Platinum).
S7311	Q-VD-Oph Q-VD-OPh 是一种有效的pan-caspase抑制剂，作用于caspases 1， 3， 8和9，IC50范围在25到400 nM之间，有效抑制与细胞凋亡相关的末端caspase激活，底物裂解，及DNA梯状条带形成。Q-VD-OPh 可抑制HIV感染。	Nat Immunol, 2020, 21(5):546-554 Nat Commun, 2020, 24;11(1):1996 Cell Rep, 2020, 21;31(3):107547	UA and Q-VD-Oph attenuated TNF-α-induced unclear translocation of NF-κB (C) and P-STAT3(S727) (D) in BEAS-2B cells.
S8102	Z-VAD(OH)-FMK (Caspase Inhibitor VI) Z-VAD-FMK (Caspase Inhibitor VI)是一类不可逆的泛caspase抑制剂。	Nat Commun, 2019, 10(1):4040 Cell Host Microbe, 2018, 24(5):689-702 Autophagy, 2018, 14(5):778-795	Effect on the RAS of CFZ, z-VAD-fmk, or CFZ+z-VAD-fmk treatments administered 5 or 12 days after C26 inoculation and control groups. Serum levels of a renin and b ANGII. c The mRNA expression of ATF2. d Western blot analysis of ATF2 and pATF2. e pATF2-to-ATF2 ratio. Significant differences were detected between most of the groups, with the exceptionsof (A and B) CP and UT (D) and ZP and ZT (#); and (C and E) CP and UP (*), CT and UT (#), and HC, ZP, ZT and CC (&). ZP:z-VAD-fmk.
S7775	Emricasan Emricasan 是有效的、不可逆的泛半胱天冬酶（pan-caspase）抑制剂。Emricasan 也是寨卡病毒感染的抑制剂。	Nature, 2020, 580(7803):391-395 Nat Immunol, 2020, 21(5):546-554 Immunity, 2020, 22 pii: S1074-7613(20)30160-6
S9075	Mulberroside A Mulberroside A 是从 Morus alba 根的乙醇提取物中分离出的，具有抗酪氨酸酶和抗氧化活性，并被广泛用作化妆品中的活性成分。Mulberroside A 降低 TNF-α、IL-1β 和 IL-6 的表达并抑制 NALP3、caspase-1 和 NF-κB 的激活以及 ERK、JNK 和 p38 的磷酸化。
S7901	Ac-DEVD-CHO Ac-DEVD-CHO是Group II caspases的有效抑制剂，对caspase-3和caspase-7的Ki值分别为0.2 nM和1.6 nM。对caspase-2制剂效果弱，Ki值为1.7 μM。	J Exp Med, 2020, 6;217(7) pii: e20191453 Gene, 2020, 732:144339 Nat Commun, 2019, 10(1):3051	Microwave (MW) hyperthermia triggers cell death through caspase-3-mediated apoptosis. H460, PC-9 and H1975 cells were treated with or without Ac-DEVD-CHO for 3 h prior to MW hyperthermia (43°C for 90 min), then allowed to recover at 37°C until 24 h. (A) Cell viability was determined by CCK-8 assay. Data are expressed as the means ± SEM of 3 independent experiments. P<0.05 vs. the control group, *P<0.01 vs. the control group.
S5579	Chelidonic acid Chelidonic acid (Jerva acid, Jervaic acid, γ-Pyrone-2,6-dicarboxylic acid) 是在几种植物中发现的次级代谢产物，对实验动物的过敏性疾病具有治疗潜力。Chelidonic acid 通过阻断HMC-1细胞中的 NF-κB 和 caspase-1 来抑制 IL-6 的产生。Chelidonic acid 也是 glutamate decarboxylase 的抑制剂，其Ki值为1.2 μM。
S5584	Citronellol Citronellol, a constituent of rose and geranium oils, is used in perfumes and insect repellents. Citronellol can cause necrotic apoptosis of NCI-H1299 cells by up-regulating TNF-α, RIP1 / RIP3 activities, and down-regulating caspase-3 / caspase-8 activities. Citronellol also results in a biphasic increase in ROS production at 1 h and at 12 h in NCI-H1299 cells.
S1029	Lenalidomide (CC-5013) Lenalidomide (CC-5013)是一种TNF-α分泌抑制剂，在PBMCs中IC50为13 nM。Lenalidomide (CC-5013) 是 ubiquitin E3 ligase cereblon (CRBN) 的配体，它通过CRBN-CRL4泛素连接酶引起两个淋巴样转录因子IKZF1和IKZF3的选择性泛素化和降解。Lenalidomide 可促进 cleaved caspase-3 的表达、抑制 VEGF 的表达并诱导凋亡。	Nat Cell Biol, 2020, 22(5):526-533 Mol Cell, 2020, 5;77(5):1092-1106 e9 Nat Commun, 2020, 17;11(1):359	Effect of lenalidomide treatment (50 mg/kg/day, p.o. for 3 days) on expression of tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), Fas, Fas ligand (FasL), and cleaved caspase-3 in myocardium from lean and ob/ob mice. (a) Representative gel blots of TNF-α, IL-6, Fas, FasL, cleaved caspase-3 and α-Tubulin (as loading control) using specific antibodies. (b) TNF-α.
S2768	Dinaciclib (SCH727965) Dinaciclib (SCH727965, PS-095760) 是一种新型有效的CDK抑制剂，作用于CDK2，CDK5，CDK1和CDK9，无细胞试验中IC50分别为1 nM，1 nM，3 nM和4 nM。它也会阻断胸甘(dThd) DNA整合。Dinaciclib 可通过激活caspases 8和caspases 9来诱导细胞凋亡。Phase 3。	Cancer Cell, 2020, 13;37(4):599-617 e7 EMBO Mol Med, 2020, e11099 Clin Cancer Res, 2020, 10.1158/1078-0432.CCR-19-2706	CDK4/6 inhibition has potent cytostatic effect in HER2-positive models. The indicated cells were treated with PD-0332991 (1 uM) or Dinaciclib (1 uM) for 96 hours and plates were stained with crystal violet.
S2738	PAC-1 PAC-1是一种有效的procaspase-3（酶原-3）激活剂，EC50为0.22 μM，是第一个已知的直接激活酶原e-3为caspase-3的小分子。	J Hazard Mater, 2020, 18;396:122605 Cell Death Dis, 2020, 11(6):482 G3 (Bethesda), 2020, 4;10(5):1585-1597	The effects of PAC-1 (activator of ROS) administration on the newborn pups' weight and the plasma IGF-1 and ROS levels in graviditas gp91phox-/- mice. The values are presented as the means ± SD derived from six animals. *P<0.05 in comparison to the non-treatment mice.
S2891	GW441756 GW441756 是一种有效的，选择性的TrkA抑制剂，IC50为2 nM，对c-Raf1和CDK2几乎没有抑制活性。GW441756 可增加caspase-3并诱导凋亡。	Theranostics, 2020, 10(4):1649-1677 Cancers, 2019, 11(6) Front Cell Neurosci, 2019, 13:332	Thermal latency and mechanical allodynia were normalized in the RTXw1 + 4MC group (n= 6). In these mice, thermal hypoalgesia reappeared within 2 days of GW441756 injection (D). GW441756 did not affect mechanical thresholds (E) in the RTXw1 + 4MC group. (F, G) The diagrams show behavioral responses of naïve mice to either gambogic amide (open square, n = 6) or GW441756 (open circle, n =6). Gambogic amide induced mild thermal hyperalgesia within 2 days of injection but GW441756 did not affect thermal latencies (F). Both gambogic amide and GW441756 did not affect mechanical responses. P < 0.05, P < 0.01, and **P < 0.001: paired t-test comparing preinjection vs. postinjection effects. #P < 0.05, ##P < 0.01, and ###P < 0.001: between drugs and saline treatments.
S3238^New	Resibufogenin Resibufogenin (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。
S6899^New	Licochalcone D
S9634^New	Phenoxodiol (Haginin E) Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) 是一种具有抗肿瘤活性的异黄酮类似物，可激活 caspase 系统，抑制 XIAP (X-linked inhibitor of apoptosis)，并破坏 FLICE inhibitory protein (FLIP) 的表达，从而导致肿瘤细胞凋亡。Phenoxodiol 也抑制 DNA topoisomerase II。
S4353^New	Terfenadine Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.
S2927	Apoptosis Activator 2 Apoptosis Activator 2强诱导caspase-3激活， PARP分裂， DNA断裂，导致细胞破坏(Apaf-1依赖性的)，IC50约为4 μM，抑制HMEC， PREC和MCF-10A细胞活性。	Eur Rev Med Pharmacol Sci, 2020, 24(11):5925-5932
S7326	Tasisulam Tasisulam是一种抗肿瘤剂，是通过内源途径导致细胞凋亡的诱导物。 Phase 3	Skin Pharmacol Physiol, 2016, 29(6):281-290
S6501	NVP 231 NVP 231是新型CerK抑制剂，在体外抑制重组CerK的催化活性，IC50为12 nM。
S9276	Alisol B Alisol 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.
S2271	Berberine chloride Berberine 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。	Oncol Rep, 2018, 40(3):1525-1532 Shandong University, 2014, Haoran Cui
S2448	Gambogic Acid Gambogic 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。	Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-0775
S9097	Alisol B Acetate Alisol B acetate, 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.
S5550	Ethyl gallate Ethyl gallat, which could be found naturally in a variety of plant sources, is a food additive with antimicrobial activity.
S3865	Taurochenodeoxycholic acid Taurochenodeoxycholic acid (Taurochenodeoxycholic acid (Taurochenodeoxycholate, TCDCA, Chenodeoxycholyltaurine)), a bile acid formed in the liver of most species, is used as a cholagogue and choleretic.	Microbiome, 2019, 7(1):145
S3224^New	Cinobufagin Cinobufagin (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。
S6882^New	HI-TOPK-032 HI-TOPK-032 是一种有效的、特异性的 TOPK 的抑制剂。HI-TOPK-032 还可以降低 ERK-RSK 磷酸化，调节 p53、裂化的 caspase-7 和裂化的 PARP 的丰度，并在癌细胞中诱导凋亡。

目录号	产品描述	文献引用	实验数据
S2228	Belnacasan (VX-765) Belnacasan (VX-765)是一种有效的选择性caspase-1抑制剂，无细胞试验中K_i为0.8 nM。Phase 2。	Cell,2020, 30;181(3):637-652.e15. Cell,2020, 30;181(3):637-652e15 EMBO J,2020, 18;39(10):e103758	(D and E) Caspase-1 inhibitors (Ac-YVAD-CMK and VX765) were added during the induction of trastuzumab-dependent BT-474 (red) or rituximab-dependent Raji cell phagocytosis (green). MFI of PD-L1 (D) and IDO (E) in macrophages are as indicated.
S3267^New	Kaempferol-3-O-rutinoside Kaempferol-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。
S3275^New	Senkyunolide I Senkyunolide 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。
S2417	20-Hydroxyecdysone 20-Hydroxyecdysone (Ecdysterone, 20E, B-ecdysone, Commisterone) 是一种自然发生的蜕皮激素，控制节肢动物的蜕皮和变态。20-Hydroxyecdysone (Ecdysterone, 20E) 可抑制 caspase 活性并通过20E核受体复合体 EcR-USP 来诱导自噬。
S7023	Z-VAD-FMK Z-VAD-FMK是一种细胞渗透性的，不可逆泛caspase抑制剂，在THP.1 和 Jurkat T细胞中阻断细胞凋亡的所有特性。	Nature,2020, 577(7788):109-114 Cell,2020, 19;180(6):1081-1097.e24. cell,2020, 180(1):64-78.e16	(A and B) Western blot analysis examining the effect of zVAD-fmk on the icaritin-induced apoptosis. The caspase inhibitor zVAD-fmk could significantly decrease the icaritin-induced cleaved caspase-3 expression. β-Actin protein levels indicate that an equal amount of protein was loaded into each lane.n=3. Mean±SD. bP<0.05, compared to the control group. eP<0.05, compared to the icaritin-treated group.
S7314	Z-IETD-FMK Z-IETD-FMK是一种特异性Caspase-8抑制剂。	Cell Host Microbe,2020, 8;27(4):556-570 e6 Biochem Pharmacol,2020, 10.1016/j.bcp.2020.113914 Biomolecules,2020, 10(2)	The caspase-8 inhibitors do not rescue NB4 cells from TPEN-triggered apoptosis. NB4 cells were pre-treated with 50 μM Z-ITED-FMK or 100 μM Ac-IETD-CHO for 1 h, and then treated with 5 μM TPEN for 24 h. (A) Cell morphology was observed and recorded using an optical microscope. The scale bar represents 20 μm. A partiallty enlarged view was shown in the lower left corner of every picture. (B) Apoptosis rate was measured with Annexin V/PI dual staining by flow cytometry.
S7313	Z-LEHD-FMK Z-LEHD-FMK (Caspase-9 Inhibitor) 是一种具有细胞透性、不可逆的Caspase-9抑制剂，有助于细胞生存。	Cell Death Dis,2020, 27;11(4):295 Acta Pharmacol Sin,2020, 26 Cancers (Basel),2019, 11(9)
S7312	Z-DEVD-FMK Z-DEVD-FMK是一种特异性，不可逆的Caspase-3抑制剂，也能有效抑制caspase-6， caspase-7， caspase-8和caspase-10。	Cell,2020, 19;180(6):1081-1097.e24 Cancer Res,2020, 10.1158/0008-5472.CAN-19-1784 Cell Rep,2020, 19;31(7):107667	(J,K)After pre-treated with Caspase-3 inhibitor Z-DEVD-FMK 50μM, the apoptotic rates of cells induced by E Platinum in BGC-823, MGC-803, and SGC-7901 cells were detected by Annexin V/PI double-staining assay. Ann.V-/PI- as healthy cells, Ann.+/PI- as early apoptotic cells, Ann.+/PI+ probably as late apoptotic cells. Data were shown as means SD for three independent experiments (P<0.05 and *P<0.01 compared with control, ##P<0.01 compared to Z-DEVD-FMK+40 μM E Platinum group with treatment of 40 μM E Platinum).
S7311	Q-VD-Oph Q-VD-OPh 是一种有效的pan-caspase抑制剂，作用于caspases 1， 3， 8和9，IC50范围在25到400 nM之间，有效抑制与细胞凋亡相关的末端caspase激活，底物裂解，及DNA梯状条带形成。Q-VD-OPh 可抑制HIV感染。	Nat Immunol,2020, 21(5):546-554 Nat Commun,2020, 24;11(1):1996 Cell Rep,2020, 21;31(3):107547	UA and Q-VD-Oph attenuated TNF-α-induced unclear translocation of NF-κB (C) and P-STAT3(S727) (D) in BEAS-2B cells.
S8102	Z-VAD(OH)-FMK (Caspase Inhibitor VI) Z-VAD-FMK (Caspase Inhibitor VI)是一类不可逆的泛caspase抑制剂。	Nat Commun,2019, 10(1):4040 Cell Host Microbe,2018, 24(5):689-702 Autophagy,2018, 14(5):778-795	Effect on the RAS of CFZ, z-VAD-fmk, or CFZ+z-VAD-fmk treatments administered 5 or 12 days after C26 inoculation and control groups. Serum levels of a renin and b ANGII. c The mRNA expression of ATF2. d Western blot analysis of ATF2 and pATF2. e pATF2-to-ATF2 ratio. Significant differences were detected between most of the groups, with the exceptionsof (A and B) CP and UT (D) and ZP and ZT (#); and (C and E) CP and UP (*), CT and UT (#), and HC, ZP, ZT and CC (&). ZP:z-VAD-fmk.
S7775	Emricasan Emricasan 是有效的、不可逆的泛半胱天冬酶（pan-caspase）抑制剂。Emricasan 也是寨卡病毒感染的抑制剂。	Nature,2020, 580(7803):391-395 Nat Immunol,2020, 21(5):546-554 Immunity,2020, 22 pii: S1074-7613(20)30160-6
S9075	Mulberroside A Mulberroside A 是从 Morus alba 根的乙醇提取物中分离出的，具有抗酪氨酸酶和抗氧化活性，并被广泛用作化妆品中的活性成分。Mulberroside A 降低 TNF-α、IL-1β 和 IL-6 的表达并抑制 NALP3、caspase-1 和 NF-κB 的激活以及 ERK、JNK 和 p38 的磷酸化。
S7901	Ac-DEVD-CHO Ac-DEVD-CHO是Group II caspases的有效抑制剂，对caspase-3和caspase-7的Ki值分别为0.2 nM和1.6 nM。对caspase-2制剂效果弱，Ki值为1.7 μM。	J Exp Med,2020, 6;217(7) pii: e20191453 Gene,2020, 732:144339 Nat Commun,2019, 10(1):3051	Microwave (MW) hyperthermia triggers cell death through caspase-3-mediated apoptosis. H460, PC-9 and H1975 cells were treated with or without Ac-DEVD-CHO for 3 h prior to MW hyperthermia (43°C for 90 min), then allowed to recover at 37°C until 24 h. (A) Cell viability was determined by CCK-8 assay. Data are expressed as the means ± SEM of 3 independent experiments. P<0.05 vs. the control group, *P<0.01 vs. the control group.
S5579	Chelidonic acid Chelidonic acid (Jerva acid, Jervaic acid, γ-Pyrone-2,6-dicarboxylic acid) 是在几种植物中发现的次级代谢产物，对实验动物的过敏性疾病具有治疗潜力。Chelidonic acid 通过阻断HMC-1细胞中的 NF-κB 和 caspase-1 来抑制 IL-6 的产生。Chelidonic acid 也是 glutamate decarboxylase 的抑制剂，其Ki值为1.2 μM。
S5584	Citronellol Citronellol, a constituent of rose and geranium oils, is used in perfumes and insect repellents. Citronellol can cause necrotic apoptosis of NCI-H1299 cells by up-regulating TNF-α, RIP1 / RIP3 activities, and down-regulating caspase-3 / caspase-8 activities. Citronellol also results in a biphasic increase in ROS production at 1 h and at 12 h in NCI-H1299 cells.

目录号	产品描述	文献引用	实验数据
S1029	Lenalidomide (CC-5013) Lenalidomide (CC-5013)是一种TNF-α分泌抑制剂，在PBMCs中IC50为13 nM。Lenalidomide (CC-5013) 是 ubiquitin E3 ligase cereblon (CRBN) 的配体，它通过CRBN-CRL4泛素连接酶引起两个淋巴样转录因子IKZF1和IKZF3的选择性泛素化和降解。Lenalidomide 可促进 cleaved caspase-3 的表达、抑制 VEGF 的表达并诱导凋亡。	Nat Cell Biol, 2020, 22(5):526-533 Mol Cell, 2020, 5;77(5):1092-1106 e9 Nat Commun, 2020, 17;11(1):359	Effect of lenalidomide treatment (50 mg/kg/day, p.o. for 3 days) on expression of tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), Fas, Fas ligand (FasL), and cleaved caspase-3 in myocardium from lean and ob/ob mice. (a) Representative gel blots of TNF-α, IL-6, Fas, FasL, cleaved caspase-3 and α-Tubulin (as loading control) using specific antibodies. (b) TNF-α.
S2768	Dinaciclib (SCH727965) Dinaciclib (SCH727965, PS-095760) 是一种新型有效的CDK抑制剂，作用于CDK2，CDK5，CDK1和CDK9，无细胞试验中IC50分别为1 nM，1 nM，3 nM和4 nM。它也会阻断胸甘(dThd) DNA整合。Dinaciclib 可通过激活caspases 8和caspases 9来诱导细胞凋亡。Phase 3。	Cancer Cell, 2020, 13;37(4):599-617 e7 EMBO Mol Med, 2020, e11099 Clin Cancer Res, 2020, 10.1158/1078-0432.CCR-19-2706	CDK4/6 inhibition has potent cytostatic effect in HER2-positive models. The indicated cells were treated with PD-0332991 (1 uM) or Dinaciclib (1 uM) for 96 hours and plates were stained with crystal violet.
S2738	PAC-1 PAC-1是一种有效的procaspase-3（酶原-3）激活剂，EC50为0.22 μM，是第一个已知的直接激活酶原e-3为caspase-3的小分子。	J Hazard Mater, 2020, 18;396:122605 Cell Death Dis, 2020, 11(6):482 G3 (Bethesda), 2020, 4;10(5):1585-1597	The effects of PAC-1 (activator of ROS) administration on the newborn pups' weight and the plasma IGF-1 and ROS levels in graviditas gp91phox-/- mice. The values are presented as the means ± SD derived from six animals. *P<0.05 in comparison to the non-treatment mice.
S2891	GW441756 GW441756 是一种有效的，选择性的TrkA抑制剂，IC50为2 nM，对c-Raf1和CDK2几乎没有抑制活性。GW441756 可增加caspase-3并诱导凋亡。	Theranostics, 2020, 10(4):1649-1677 Cancers, 2019, 11(6) Front Cell Neurosci, 2019, 13:332	Thermal latency and mechanical allodynia were normalized in the RTXw1 + 4MC group (n= 6). In these mice, thermal hypoalgesia reappeared within 2 days of GW441756 injection (D). GW441756 did not affect mechanical thresholds (E) in the RTXw1 + 4MC group. (F, G) The diagrams show behavioral responses of naïve mice to either gambogic amide (open square, n = 6) or GW441756 (open circle, n =6). Gambogic amide induced mild thermal hyperalgesia within 2 days of injection but GW441756 did not affect thermal latencies (F). Both gambogic amide and GW441756 did not affect mechanical responses. P < 0.05, P < 0.01, and **P < 0.001: paired t-test comparing preinjection vs. postinjection effects. #P < 0.05, ##P < 0.01, and ###P < 0.001: between drugs and saline treatments.
S3238^New	Resibufogenin Resibufogenin (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。
S6899^New	Licochalcone D
S9634^New	Phenoxodiol (Haginin E) Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) 是一种具有抗肿瘤活性的异黄酮类似物，可激活 caspase 系统，抑制 XIAP (X-linked inhibitor of apoptosis)，并破坏 FLICE inhibitory protein (FLIP) 的表达，从而导致肿瘤细胞凋亡。Phenoxodiol 也抑制 DNA topoisomerase II。
S4353^New	Terfenadine Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.
S2927	Apoptosis Activator 2 Apoptosis Activator 2强诱导caspase-3激活， PARP分裂， DNA断裂，导致细胞破坏(Apaf-1依赖性的)，IC50约为4 μM，抑制HMEC， PREC和MCF-10A细胞活性。	Eur Rev Med Pharmacol Sci, 2020, 24(11):5925-5932
S7326	Tasisulam Tasisulam是一种抗肿瘤剂，是通过内源途径导致细胞凋亡的诱导物。 Phase 3	Skin Pharmacol Physiol, 2016, 29(6):281-290
S6501	NVP 231 NVP 231是新型CerK抑制剂，在体外抑制重组CerK的催化活性，IC50为12 nM。
S9276	Alisol B Alisol 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.
S2271	Berberine chloride Berberine 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。	Oncol Rep, 2018, 40(3):1525-1532 Shandong University, 2014, Haoran Cui
S2448	Gambogic Acid Gambogic 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。	Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-0775
S9097	Alisol B Acetate Alisol B acetate, 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.
S5550	Ethyl gallate Ethyl gallat, which could be found naturally in a variety of plant sources, is a food additive with antimicrobial activity.
S3865	Taurochenodeoxycholic acid Taurochenodeoxycholic acid (Taurochenodeoxycholic acid (Taurochenodeoxycholate, TCDCA, Chenodeoxycholyltaurine)), a bile acid formed in the liver of most species, is used as a cholagogue and choleretic.	Microbiome, 2019, 7(1):145

目录号	产品描述	文献引用	实验数据
S3224^New	Cinobufagin Cinobufagin (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。
S6882^New	HI-TOPK-032 HI-TOPK-032 是一种有效的、特异性的 TOPK 的抑制剂。HI-TOPK-032 还可以降低 ERK-RSK 磷酸化，调节 p53、裂化的 caspase-7 和裂化的 PARP 的丰度，并在癌细胞中诱导凋亡。

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S3224^New

Cinobufagin

Cinobufagin (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。

S6882^New

HI-TOPK-032

HI-TOPK-032 是一种有效的、特异性的 TOPK 的抑制剂。HI-TOPK-032 还可以降低 ERK-RSK 磷酸化，调节 p53、裂化的 caspase-7 和裂化的 PARP 的丰度，并在癌细胞中诱导凋亡。

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