Caspase

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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(9) Caspase激活剂(5)

产品目录	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。	MBio, 2019, 10(1) Front Immunol, 2019, 10:1872 Front Immunol, 2019, 10:268	(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.
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 Mol Cell Endocrinol, 2020, 499:110595 Nature, 2019, 573(7774):439-444	(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。	Cancers (Basel), 2019, 11(9) Front Immunol, 2019, 10:268 Biochem Biophys Res Commun, 2019, 513(4):1063-1069	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。	Cancers (Basel), 2019, 11(9) Int J Oncol, 2019, 54(6):1969-1980 Cancer Biol Ther, 2014, 15(6):758-67
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。	J Cell Physiol, 2020, 235(3):2911-2924 Cancer Cell, 2019, 35(5):798-815 Cancer Cell, 2019, 35(5):798-815.e5	(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。	Int J Cancer, 2019, 10.1002/ijc.32615 PLoS Pathog, 2019, 15(8):e1007991 Aging (Albany NY), 2019, 11(2):771-782	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。	Int J Cancer, 2019, 10.1002/ijc.32799 Nephron, 2019, 10.1159/000499506 Oncotarget, 2019, 10(62):6691-6712
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。	Nat Commun, 2019, 10(1):3051 Nat Commun, 2019, 10(1):1655 Nat Commun, 2018, 9(1):1680	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.
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。	Cell Death Discov, 2018, 4:107 Biol Med, 2015, 10.4172/0974-8369.1000259	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.
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。
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
S2448	Gambogic Acid Gambogic Acid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.

产品目录	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。	MBio,2019, 10(1) Front Immunol,2019, 10:1872 Front Immunol,2019, 10:268	(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.
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 Mol Cell Endocrinol,2020, 499:110595 Nature,2019, 573(7774):439-444	(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。	Cancers (Basel),2019, 11(9) Front Immunol,2019, 10:268 Biochem Biophys Res Commun,2019, 513(4):1063-1069	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。	Cancers (Basel),2019, 11(9) Int J Oncol,2019, 54(6):1969-1980 Cancer Biol Ther,2014, 15(6):758-67
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。	J Cell Physiol,2020, 235(3):2911-2924 Cancer Cell,2019, 35(5):798-815 Cancer Cell,2019, 35(5):798-815.e5	(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。	Int J Cancer,2019, 10.1002/ijc.32615 PLoS Pathog,2019, 15(8):e1007991 Aging (Albany NY),2019, 11(2):771-782	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。	Int J Cancer,2019, 10.1002/ijc.32799 Nephron,2019, 10.1159/000499506 Oncotarget,2019, 10(62):6691-6712
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。	Nat Commun,2019, 10(1):3051 Nat Commun,2019, 10(1):1655 Nat Commun,2018, 9(1):1680	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.

产品目录	产品描述	文献引用	实验数据
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。	Cell Death Discov, 2018, 4:107 Biol Med, 2015, 10.4172/0974-8369.1000259	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.
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。
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
S2448	Gambogic Acid Gambogic Acid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.

Tags: Caspases apoptosis | Caspase inhibition | Caspase activation | Caspase activity | Caspase pathway | Caspase phosphorylation | Caspase cleavage | Caspase activity assay | Procaspase activation | Caspase inhibitor in vivo | Caspase inhibitor clinical trial | Caspase-independent apoptosis | Caspase-dependent apoptosis | Caspase inhibitor review