カスパーゼ

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
S2228	Belnacasan (VX-765)	<1 mg/mL	100 mg/mL	100 mg/mL
S6899	Licochalcone D	-1 mg/mL	100 mg/mL	-1 mg/mL
S3267	Kaempferol-3-O-rutinoside	-1 mg/mL	100 mg/mL	-1 mg/mL
S6882	HI-TOPK-032	<1 mg/mL	4 mg/mL	<1 mg/mL
S8507	Z-YVAD-FMK	<1 mg/mL	100 mg/mL	<1 mg/mL
S0354	Alsterpaullone			' mg/mL
S2417	20-Hydroxyecdysone	<1 mg/mL	96 mg/mL	96 mg/mL
S7023	Z-VAD-FMK	<1 mg/mL	93 mg/mL	''<1 mg/mL
S7314	Z-IETD-FMK	<1 mg/mL	91 mg/mL	'<1 mg/mL
S7313	Z-LEHD-FMK TFA	44 mg/mL	100 mg/mL	''100 mg/mL
S7312	Z-DEVD-FMK	<1 mg/mL	100 mg/mL	'<1 mg/mL
S7311	Q-VD-Oph	<1 mg/mL	100 mg/mL	100 mg/mL
S8102	Z-VAD(OH)-FMK (Caspase Inhibitor VI)	<1 mg/mL	90 mg/mL	90 mg/mL
S7775	Emricasan	<1 mg/mL	100 mg/mL	'100 mg/mL
S9075	Mulberroside A	-1 mg/mL	100 mg/mL	-1 mg/mL
S7901	Ac-DEVD-CHO	100 mg/mL	-1 mg/mL	'-1 mg/mL
S5579	Chelidonic acid	-1 mg/mL	4 mg/mL	-1 mg/mL
S5584	Citronellol	31 mg/mL	<1 mg/mL	-1 mg/mL
S1029	Lenalidomide (CC-5013)	<1 mg/mL	52 mg/mL	<1 mg/mL
S2768	Dinaciclib (SCH727965)	<1 mg/mL	26 mg/mL	8 mg/mL
S2738	PAC-1	<1 mg/mL	78 mg/mL	16 mg/mL
S2891	GW441756	<1 mg/mL	25 mg/mL	<1 mg/mL
S3224	Cinobufagin	-1 mg/mL	100 mg/mL	-1 mg/mL
S3238	Resibufogenin	-1 mg/mL	100 mg/mL	-1 mg/mL
S3275	Senkyunolide I	-1 mg/mL	100 mg/mL	-1 mg/mL
S0913	4',5,7-Trimethoxyflavone	<1 mg/mL	62 mg/mL	15 mg/mL
S9634	Phenoxodiol (Haginin E)	<1 mg/mL	48 mg/mL	48 mg/mL
S2927	Apoptosis Activator 2	<1 mg/mL	61 mg/mL	<1 mg/mL
S7326	Tasisulam	<1 mg/mL	83 mg/mL	'83 mg/mL
S6501	NVP 231	<1 mg/mL	86 mg/mL	8 mg/mL
S9276	Alisol B	-1 mg/mL	95 mg/mL	-1 mg/mL
S2271	Berberine chloride	<1 mg/mL	40 mg/mL	<1 mg/mL
S2448	Gambogic Acid	<1 mg/mL	100 mg/mL	100 mg/mL
S9097	Alisol B Acetate	-1 mg/mL	100 mg/mL	-1 mg/mL
S5550	Ethyl gallate	-1 mg/mL	39 mg/mL	-1 mg/mL
S4353	Terfenadine	<1 mg/mL	94 mg/mL	27 mg/mL
S3865	Taurochenodeoxycholic acid	-1 mg/mL	99 mg/mL	-1 mg/mL
S3088	(±)-Methyl Jasmonate			' mg/mL

亜型選択性的な製品

Caspase製品

All (38) Caspase阻害剤(18) Caspase活性剤(19) Caspaseモジュレータ(1)

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S2228	Belnacasan (VX-765) Belnacasan (VX-765) is a potent and selective inhibitor of caspase-1 with K_i of 0.8 nM in a cell-free assay. Phase 2.	Cell Death Dis, 2021, 12(1):78 Life Sci, 2021, 269:119090 Cell, 2020, 30;181(3):637-652.e15.	(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.
S6899^新	Licochalcone D Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and MET activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage.
S3267^新	Kaempferol-3-O-rutinoside Kaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-rutinoside), a flavonoid extracted from Carthamus tinctorius, alters the shape and structure of injured neurons, decreases the number of apoptotic cells, down-regulates expression of p-JAK2, p-STAT3, caspase-3, and Bax and decreases Bax immunoredactivity, and increases Bcl-2 protein expression and immunoreactivity.
S6882^新	HI-TOPK-032 HI-TOPK-032 is a potent and specific inhibitor of TOPK. HI-TOPK-032 also reduces ERK-RSK phosphorylation, regulates of the abundance of p53, cleaved caspase-7, and cleaved PARP, and induces apoptosis in cancer cells.
S8507^新	Z-YVAD-FMK Z-YVAD-FMK is a cell-permeable and irreversible caspase-1 specific inhibitor with anti-inflammatory and anti-tumor activities.
S0354^新	Alsterpaullone Alsterpaullone (Alp, 9-Nitropaullone, NSC 705701) is a potent inhibitor of CDK with IC50 of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also acts as a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 of both 4 nM for GSK-3α and GSK-3β. Alsterpaullone induces apoptosis by activation of caspase-9. Alsterpaullone has antitumor activity and possesses potential for the treatment of neurodegenerative and proliferative disorders.
S2417	20-Hydroxyecdysone 20-Hydroxyecdysone (Ecdysterone, 20E, B-ecdysone, Commisterone) is a naturally occurring ecdysteroid hormone which controls the ecdysis (moulting) and metamorphosis of arthropods.20-Hydroxyecdysone (Ecdysterone, 20E) inhibits caspase activity and induces autophagy via the 20E nuclear receptor complex, EcR-USP.	PLoS Biol, 2019, 17(10):e3000145
S7023	Z-VAD-FMK Z-VAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor, blocks all features of apoptosis in THP.1 and Jurkat T-cells.	Nat Commun, 2021, 12(1):647 Autophagy, 2021, 1-14 Cancers (Basel), 2021, 13(2)E243	(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 (Caspase-8 Inhibitor) is a specific Caspase-8 inhibitor.	Nat Commun, 2021, 12(1):476 Cell Host Microbe, 2020, 8;27(4):556-570 e6 Signal Transduct Target Ther, 2020, 5(1):235	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 TFA Z-LEHD-FMK TFA (Caspase-9 Inhibitor) is a specific, irreversible Caspase-9 inhibitor.	Cell Death Dis, 2020, 27;11(4):295 Acta Pharmacol Sin, 2020, 26 Exp Ther Med, 2020, 20(4):3244-3252
S7312	Z-DEVD-FMK Z-DEVD-FMK (Caspase-3 Inhibitor) is a specific, irreversible Caspase-3 inhibitor, and also shows potent inhibition on caspase-6, caspase-7, caspase-8, and 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 is a potent pan-caspase inhibitor with IC50 ranged from 25 to 400 nM for caspases 1,3,8, and 9. Q-VD-OPh can inhibits HIV infection.	Haematologica, 2021, 10.3324/haematol.2020.259531 Nat Immunol, 2020, 21(5):546-554 Nat Commun, 2020, 24;11(1):1996	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) is an irreversible pan-caspase inhibitor.	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 (IDN-6556, PF 03491390, PF-03491390) is a potent irreversible pan-caspase inhibitor. Emricasan is an inhibitor of Zika virus infection.	Cell Death Differ, 2021, 10.1038/s41418-020-00685-9 Nature, 2020, 580(7803):391-395 Nat Immunol, 2020, 21(5):546-554
S9075	Mulberroside A Mulberroside A, isolated from the ethanol extract of Morus alba roots, is widely employed as an active ingredient in cosmetic products due to its anti-tyrosinase and anti-oxidant activities. Mulberroside A decreases the expressions of TNF-α, IL-1β and IL-6 and inhibits the activation of NALP3, caspase-1 and NF-κB and the phosphorylation of ERK, JNK and p38.
S7901	Ac-DEVD-CHO Ac-DEVD-CHO (Caspase-3 Inhibitor I, N-Ac-Asp-Glu-Val-Asp-CHO) is a potent aldehyde inhibitor of Group II caspases with Ki values of 0.2 nM and 0.3 nM for for caspase-3 and caspase-7, respectively. Weak inhibition for caspase-2.	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) is a secondary metabolite found in several plants with therapeutic potential in allergic disorders in experimental animals. Chelidonic acid inhibits IL-6 production by blocking NF-κB and caspase-1 in HMC-1 cells. Chelidonic acid is also an inhibitor of glutamate decarboxylase with Ki of 1.2 μM.
S5584	Citronellol Citronellol (Dihydrogeraniol, (±)-β-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) is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis.	Sci China Life Sci, 2021, 10.1007/s11427-020-1860-2 Nat Cell Biol, 2020, 22(5):526-533 Mol Cell, 2020, 5;77(5):1092-1106 e9	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) is a novel and potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM in cell-free assays, respectively. It also blocks thymidine (dThd) DNA incorporation. Dinaciclib induces apoptosis through the activation of caspases 8 and 9. Phase 3.	Eur J Cancer, 2021, 145:92-108 Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19	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 is a potent procaspase-3 activator with EC50 of 0.22 μM and the first small molecule known to directly activate procaspase-3 to caspase-3.	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 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2. GW441756 produces a relevant increase of caspase-3 that leads to apoptosis.	Cancer Res, 2020, canres.1992.2020 Mol Neurobiol, 2020, 10.1007/s12035-020-02156-1 Theranostics, 2020, 10(4):1649-1677	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.
S3224^新	Cinobufagin Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.
S3238^新	Resibufogenin Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.
S3275^新	Senkyunolide I Senkyunolide I (SEI, SENI) is an orally active compound isolated from Ligusticum chuanxiong with analgesic, anti-migraine, neuroprotective, anti-oxidation and anti-apoptosis activities. Senkyunolide I (SEI, SENI) up-regulates the phosphorylation of Erk1/2 and induces Nrf2 nuclear translocation with enhanced HO-1 and NQO1 expressions. Senkyunolide I (SEI, SENI) promotes the ratio of Bcl-2/Bax and inhibits the expressions of cleaved caspase 3 and caspase 9.
S0913^新	4',5,7-Trimethoxyflavone 4',5,7-Trimethoxyflavone (5,7,4'-Trimethoxyflavone, TMF) is a flavonoid isolated from Kaempferia parviflora (KP) that induces apoptosis. 4',5,7-Trimethoxyflavone increases sub-G1 phase, DNA fragmentation, annexin-V/PI staining and Bax/Bcl-xL ratio, activates caspase-3 and degrades poly (ADP-ribose) polymerase (PARP) protein.
S9634^新	Phenoxodiol (Haginin E) Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) is an isoflavone analog with antineoplastic activity that activates the caspase system, inhibits XIAP (X-linked inhibitor of apoptosis), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. Phenoxodiol also inhibits DNA topoisomerase II.
S2927	Apoptosis Activator 2 Apoptosis Activator 2 strongly induces caspase-3 activation, PARP cleavage, and DNA fragmentation which leads to the destruction of cells (Apaf-1 dependent) with IC50 of ~4 μM, inactive to HMEC, PREC, or MCF-10A cells.	Eur Rev Med Pharmacol Sci, 2020, 24(11):5925-5932
S7326	Tasisulam Tasisulam (LY573636) is an antitumor agent and an apoptosis inducer via the intrinsic pathway. Phase 3.	Skin Pharmacol Physiol, 2016, 29(6):281-290
S6501	NVP 231 NVP 231 is a novel CerK inhibitor that inhibits the catalytic activity of recombinant CerK in vitro with an IC50 of 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 is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.	Antiviral Res, 2020, 186:105000 Oncol Rep, 2018, 40(3):1525-1532 Shandong University, 2014, Haoran Cui
S2448	Gambogic Acid Gambogic Acid (Guttatic, Guttic) activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-X_L, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50 of 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μM, respectively.	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 (Phyllemblin, gallic acid ethyl ester), which could be found naturally in a variety of plant sources, is a food additive with antimicrobial activity
S4353	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.
S3865	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
S3088^新	(±)-Methyl Jasmonate (±)-Methyl Jasmonate (MeJA, Methyl jasmonate, Methyl 2-(3-oxo-2-(pent-2-en-1-yl)cyclopentyl)acetate), a phytohormone that acts as a vital cell regulator in plants, is a new candidate for the treatment of Inflammatory bowel diseases (IBDs), modulating the expression of the major classes of caspase-type protease families.

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S2228	Belnacasan (VX-765) Belnacasan (VX-765) is a potent and selective inhibitor of caspase-1 with K_i of 0.8 nM in a cell-free assay. Phase 2.	Cell Death Dis, 2021, 12(1):78 Life Sci, 2021, 269:119090 Cell, 2020, 30;181(3):637-652.e15.	(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.
S6899^新	Licochalcone D Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and MET activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage.
S3267^新	Kaempferol-3-O-rutinoside Kaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-rutinoside), a flavonoid extracted from Carthamus tinctorius, alters the shape and structure of injured neurons, decreases the number of apoptotic cells, down-regulates expression of p-JAK2, p-STAT3, caspase-3, and Bax and decreases Bax immunoredactivity, and increases Bcl-2 protein expression and immunoreactivity.
S6882^新	HI-TOPK-032 HI-TOPK-032 is a potent and specific inhibitor of TOPK. HI-TOPK-032 also reduces ERK-RSK phosphorylation, regulates of the abundance of p53, cleaved caspase-7, and cleaved PARP, and induces apoptosis in cancer cells.
S8507^新	Z-YVAD-FMK Z-YVAD-FMK is a cell-permeable and irreversible caspase-1 specific inhibitor with anti-inflammatory and anti-tumor activities.
S0354^新	Alsterpaullone Alsterpaullone (Alp, 9-Nitropaullone, NSC 705701) is a potent inhibitor of CDK with IC50 of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also acts as a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 of both 4 nM for GSK-3α and GSK-3β. Alsterpaullone induces apoptosis by activation of caspase-9. Alsterpaullone has antitumor activity and possesses potential for the treatment of neurodegenerative and proliferative disorders.
S2417	20-Hydroxyecdysone 20-Hydroxyecdysone (Ecdysterone, 20E, B-ecdysone, Commisterone) is a naturally occurring ecdysteroid hormone which controls the ecdysis (moulting) and metamorphosis of arthropods.20-Hydroxyecdysone (Ecdysterone, 20E) inhibits caspase activity and induces autophagy via the 20E nuclear receptor complex, EcR-USP.	PLoS Biol, 2019, 17(10):e3000145
S7023	Z-VAD-FMK Z-VAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor, blocks all features of apoptosis in THP.1 and Jurkat T-cells.	Nat Commun, 2021, 12(1):647 Autophagy, 2021, 1-14 Cancers (Basel), 2021, 13(2)E243	(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 (Caspase-8 Inhibitor) is a specific Caspase-8 inhibitor.	Nat Commun, 2021, 12(1):476 Cell Host Microbe, 2020, 8;27(4):556-570 e6 Signal Transduct Target Ther, 2020, 5(1):235	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 TFA Z-LEHD-FMK TFA (Caspase-9 Inhibitor) is a specific, irreversible Caspase-9 inhibitor.	Cell Death Dis, 2020, 27;11(4):295 Acta Pharmacol Sin, 2020, 26 Exp Ther Med, 2020, 20(4):3244-3252
S7312	Z-DEVD-FMK Z-DEVD-FMK (Caspase-3 Inhibitor) is a specific, irreversible Caspase-3 inhibitor, and also shows potent inhibition on caspase-6, caspase-7, caspase-8, and 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 is a potent pan-caspase inhibitor with IC50 ranged from 25 to 400 nM for caspases 1,3,8, and 9. Q-VD-OPh can inhibits HIV infection.	Haematologica, 2021, 10.3324/haematol.2020.259531 Nat Immunol, 2020, 21(5):546-554 Nat Commun, 2020, 24;11(1):1996	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) is an irreversible pan-caspase inhibitor.	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 (IDN-6556, PF 03491390, PF-03491390) is a potent irreversible pan-caspase inhibitor. Emricasan is an inhibitor of Zika virus infection.	Cell Death Differ, 2021, 10.1038/s41418-020-00685-9 Nature, 2020, 580(7803):391-395 Nat Immunol, 2020, 21(5):546-554
S9075	Mulberroside A Mulberroside A, isolated from the ethanol extract of Morus alba roots, is widely employed as an active ingredient in cosmetic products due to its anti-tyrosinase and anti-oxidant activities. Mulberroside A decreases the expressions of TNF-α, IL-1β and IL-6 and inhibits the activation of NALP3, caspase-1 and NF-κB and the phosphorylation of ERK, JNK and p38.
S7901	Ac-DEVD-CHO Ac-DEVD-CHO (Caspase-3 Inhibitor I, N-Ac-Asp-Glu-Val-Asp-CHO) is a potent aldehyde inhibitor of Group II caspases with Ki values of 0.2 nM and 0.3 nM for for caspase-3 and caspase-7, respectively. Weak inhibition for caspase-2.	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) is a secondary metabolite found in several plants with therapeutic potential in allergic disorders in experimental animals. Chelidonic acid inhibits IL-6 production by blocking NF-κB and caspase-1 in HMC-1 cells. Chelidonic acid is also an inhibitor of glutamate decarboxylase with Ki of 1.2 μM.
S5584	Citronellol Citronellol (Dihydrogeraniol, (±)-β-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.

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S1029	Lenalidomide (CC-5013) Lenalidomide (CC-5013) is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis.	Sci China Life Sci, 2021, 10.1007/s11427-020-1860-2 Nat Cell Biol, 2020, 22(5):526-533 Mol Cell, 2020, 5;77(5):1092-1106 e9	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) is a novel and potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM in cell-free assays, respectively. It also blocks thymidine (dThd) DNA incorporation. Dinaciclib induces apoptosis through the activation of caspases 8 and 9. Phase 3.	Eur J Cancer, 2021, 145:92-108 Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19	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 is a potent procaspase-3 activator with EC50 of 0.22 μM and the first small molecule known to directly activate procaspase-3 to caspase-3.	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 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2. GW441756 produces a relevant increase of caspase-3 that leads to apoptosis.	Cancer Res, 2020, canres.1992.2020 Mol Neurobiol, 2020, 10.1007/s12035-020-02156-1 Theranostics, 2020, 10(4):1649-1677	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.
S3224^新	Cinobufagin Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.
S3238^新	Resibufogenin Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.
S3275^新	Senkyunolide I Senkyunolide I (SEI, SENI) is an orally active compound isolated from Ligusticum chuanxiong with analgesic, anti-migraine, neuroprotective, anti-oxidation and anti-apoptosis activities. Senkyunolide I (SEI, SENI) up-regulates the phosphorylation of Erk1/2 and induces Nrf2 nuclear translocation with enhanced HO-1 and NQO1 expressions. Senkyunolide I (SEI, SENI) promotes the ratio of Bcl-2/Bax and inhibits the expressions of cleaved caspase 3 and caspase 9.
S0913^新	4',5,7-Trimethoxyflavone 4',5,7-Trimethoxyflavone (5,7,4'-Trimethoxyflavone, TMF) is a flavonoid isolated from Kaempferia parviflora (KP) that induces apoptosis. 4',5,7-Trimethoxyflavone increases sub-G1 phase, DNA fragmentation, annexin-V/PI staining and Bax/Bcl-xL ratio, activates caspase-3 and degrades poly (ADP-ribose) polymerase (PARP) protein.
S9634^新	Phenoxodiol (Haginin E) Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) is an isoflavone analog with antineoplastic activity that activates the caspase system, inhibits XIAP (X-linked inhibitor of apoptosis), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. Phenoxodiol also inhibits DNA topoisomerase II.
S2927	Apoptosis Activator 2 Apoptosis Activator 2 strongly induces caspase-3 activation, PARP cleavage, and DNA fragmentation which leads to the destruction of cells (Apaf-1 dependent) with IC50 of ~4 μM, inactive to HMEC, PREC, or MCF-10A cells.	Eur Rev Med Pharmacol Sci, 2020, 24(11):5925-5932
S7326	Tasisulam Tasisulam (LY573636) is an antitumor agent and an apoptosis inducer via the intrinsic pathway. Phase 3.	Skin Pharmacol Physiol, 2016, 29(6):281-290
S6501	NVP 231 NVP 231 is a novel CerK inhibitor that inhibits the catalytic activity of recombinant CerK in vitro with an IC50 of 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 is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.	Antiviral Res, 2020, 186:105000 Oncol Rep, 2018, 40(3):1525-1532 Shandong University, 2014, Haoran Cui
S2448	Gambogic Acid Gambogic Acid (Guttatic, Guttic) activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-X_L, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50 of 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μM, respectively.	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 (Phyllemblin, gallic acid ethyl ester), which could be found naturally in a variety of plant sources, is a food additive with antimicrobial activity
S4353	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.
S3865	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

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S3088^新	(±)-Methyl Jasmonate (±)-Methyl Jasmonate (MeJA, Methyl jasmonate, Methyl 2-(3-oxo-2-(pent-2-en-1-yl)cyclopentyl)acetate), a phytohormone that acts as a vital cell regulator in plants, is a new candidate for the treatment of Inflammatory bowel diseases (IBDs), modulating the expression of the major classes of caspase-type protease families.

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S3088^新

(±)-Methyl Jasmonate

(±)-Methyl Jasmonate (MeJA, Methyl jasmonate, Methyl 2-(3-oxo-2-(pent-2-en-1-yl)cyclopentyl)acetate), a phytohormone that acts as a vital cell regulator in plants, is a new candidate for the treatment of Inflammatory bowel diseases (IBDs), modulating the expression of the major classes of caspase-type protease families.