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) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S2228 | Belnacasan (VX-765) | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S2417 | 20-Hydroxyecdysone | <1 mg/mL | 96 mg/mL | 96 mg/mL |
| S4353 | Terfenadine | <1 mg/mL | 94 mg/mL | 27 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 | 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-FMK (Caspase Inhibitor VI) | <1 mg/mL | 90 mg/mL | 90 mg/mL |
| S7775 | Emricasan | <1 mg/mL | 100 mg/mL | '''100 mg/mL |
| S7901 | Ac-DEVD-CHO | 100 mg/mL | -1 mg/mL | -1 mg/mL |
| S5584 | Citronellol | 31 mg/mL | <1 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 |
| S2927 | Apoptosis Activator 2 | <1 mg/mL | 61 mg/mL | <1 mg/mL |
| S6501 | NVP 231 | <1 mg/mL | 86 mg/mL | 8 mg/mL |
| S7326 | Tasisulam | <1 mg/mL | 83 mg/mL | 83 mg/mL |
| S9276 | Alisol B | -1 mg/mL | 95 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 |
| S3865 | Taurochenodeoxycholic acid | -1 mg/mL | 99 mg/mL | -1 mg/mL |
亜型選択性的な製品
Caspase製品
| 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 Ki of 0.8 nM in a cell-free assay. Phase 2. |
(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.
|
|
| S2417 |
20-Hydroxyecdysone20-Hydroxyecdysone (Ecdysterone, 20E) is a naturally occurring ecdysteroid hormone which controls the ecdysis (moulting) and metamorphosis of arthropods. |
||
| S4353新 |
TerfenadineTerfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. |
||
| S7023 |
Z-VAD-FMKZ-VAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor, blocks all features of apoptosis in THP.1 and Jurkat T-cells. |
(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-FMKZ-IETD-FMK is a specific Caspase-8 inhibitor. |
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-FMKZ-LEHD-FMK is a specific, irreversible Caspase-9 inhibitor. |
||
| S7312 |
Z-DEVD-FMKZ-DEVD-FMK is a specific, irreversible Caspase-3 inhibitor, and also shows potent inhibition on caspase-6, caspase-7, caspase-8, and caspase-10. |
(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-OPhQ-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. |
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-FMK (Caspase Inhibitor VI)Z-VAD-FMK (Caspase Inhibitor VI) is an irreversible pan-caspase inhibitor. |
-FMK-S810201Z0220161121.gif)
-FMK-S810201Z0220161121.gif)
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 |
EmricasanEmricasan is a potent irreversible pan-caspase inhibitor. Emricasan is an inhibitor of Zika virus infection. |
||
| S7901 |
Ac-DEVD-CHOAc-DEVD-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. |
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.
|
|
| S5584 |
CitronellolCitronellol, a constituent of rose and geranium oils, is used in perfumes and insect repellents. |
||
| S2768 |
Dinaciclib (SCH727965)Dinaciclib (SCH727965) 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. |
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-1PAC-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. |
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 2Apoptosis 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. |
||
| S6501新 |
NVP 231NVP 231 is a novel CerK inhibitor that inhibits the catalytic activity of recombinant CerK in vitro with an IC50 of 12 nM. |
||
| S7326 |
TasisulamTasisulam is an antitumor agent and an apoptosis inducer via the intrinsic pathway. Phase 3. |
||
| 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. |
||
| S2448 |
Gambogic AcidGambogic Acid activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-XL, 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. |
||
| S9097 |
Alisol B AcetateAlisol 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 gallateEthyl gallat, which could be found naturally in a variety of plant sources, is a food additive with antimicrobial activity |
||
| S3865 |
Taurochenodeoxycholic acidTaurochenodeoxycholic acid, a bile acid formed in the liver of most species, is used as a cholagogue and choleretic. |
| 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 Ki of 0.8 nM in a cell-free assay. Phase 2. |
(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.
|
|
| S2417 |
20-Hydroxyecdysone20-Hydroxyecdysone (Ecdysterone, 20E) is a naturally occurring ecdysteroid hormone which controls the ecdysis (moulting) and metamorphosis of arthropods. |
||
| S4353新 |
TerfenadineTerfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. |
||
| S7023 |
Z-VAD-FMKZ-VAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor, blocks all features of apoptosis in THP.1 and Jurkat T-cells. |
(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-FMKZ-IETD-FMK is a specific Caspase-8 inhibitor. |
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-FMKZ-LEHD-FMK is a specific, irreversible Caspase-9 inhibitor. |
||
| S7312 |
Z-DEVD-FMKZ-DEVD-FMK is a specific, irreversible Caspase-3 inhibitor, and also shows potent inhibition on caspase-6, caspase-7, caspase-8, and caspase-10. |
(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-OPhQ-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. |
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-FMK (Caspase Inhibitor VI)Z-VAD-FMK (Caspase Inhibitor VI) is an irreversible pan-caspase inhibitor. |
-FMK-S810201Z0220161121.gif)
-FMK-S810201Z0220161121.gif)
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 |
EmricasanEmricasan is a potent irreversible pan-caspase inhibitor. Emricasan is an inhibitor of Zika virus infection. |
||
| S7901 |
Ac-DEVD-CHOAc-DEVD-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. |
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.
|
|
| S5584 |
CitronellolCitronellol, a constituent of rose and geranium oils, is used in perfumes and insect repellents. |
| 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 |
|---|---|---|---|
| S2768 |
Dinaciclib (SCH727965)Dinaciclib (SCH727965) 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. |
2020, 13;37(4):599-617 e7 2020, 10.1158/1078-0432.CCR-19-2706 2020, 2;9:e54954 |
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-1PAC-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. |
2020, 18;396:122605 2020, 4;10(5):1585-1597 2020, 6:1 |
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 2Apoptosis 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. |
||
| S6501新 |
NVP 231NVP 231 is a novel CerK inhibitor that inhibits the catalytic activity of recombinant CerK in vitro with an IC50 of 12 nM. |
||
| S7326 |
TasisulamTasisulam is an antitumor agent and an apoptosis inducer via the intrinsic pathway. Phase 3. |
2016, 29(6):281-290 |
|
| 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. |
||
| S2448 |
Gambogic AcidGambogic Acid activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-XL, 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. |
2019, 10.1158/1078-0432.CCR-19-0775 |
|
| S9097 |
Alisol B AcetateAlisol 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 gallateEthyl gallat, which could be found naturally in a variety of plant sources, is a food additive with antimicrobial activity |
||
| S3865 |
Taurochenodeoxycholic acidTaurochenodeoxycholic acid, a bile acid formed in the liver of most species, is used as a cholagogue and choleretic. |
2019, 7(1):145 |
