Bcl-2
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 | ||
| S1002 | ABT-737 | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S1001 | Navitoclax (ABT-263) | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S1121 | TW-37 | <1 mg/mL | 115 mg/mL | 4 mg/mL |
| S8048 | Venetoclax (ABT-199, GDC-0199) | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S8759 | S55746 (S 055746,BCL201) | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S2812 | AT101 | <1 mg/mL | 116 mg/mL | 89 mg/mL |
| S8061 | Sabutoclax | <1 mg/mL | 100 mg/mL | 54 mg/mL |
| S7790 | A-1210477 | <1 mg/mL | 3 mg/mL | <1 mg/mL |
| S2448 | Gambogic Acid | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S8383 | S63845 | 100 mg/mL | ||
| S8177 | BH3I-1 | <1 mg/mL | 64 mg/mL | 13 mg/mL |
| S7800 | A-1155463 | <1 mg/mL | 80 mg/mL | <1 mg/mL |
| S7801 | A-1331852 | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S7531 | UMI-77 | <1 mg/mL | 93 mg/mL | 93 mg/mL |
| S7105 | BAM7 | <1 mg/mL | 2 mg/mL | <1 mg/mL |
| S1057 | Obatoclax Mesylate (GX15-070) | <1 mg/mL | 83 mg/mL | <1 mg/mL |
| S7849 | BDA-366 | <1 mg/mL | 84 mg/mL | 5 mg/mL |
| S7126 | Marinopyrrole A (Maritoclax) | <1 mg/mL | 100 mg/mL | 45 mg/mL |
| S8650 | BTSA1 | <1 mg/mL | 81 mg/mL | <1 mg/mL |
亜型選択性的な製品
Bcl-2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 |
|---|---|---|---|
| S1002 |
ABT-737ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. 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. |
|
| S1001 |
Navitoclax (ABT-263)Navitoclax (ABT-263) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤1 nM in cell-free assays, but binds more weakly to Mcl-1 and A1. Phase 2. |
KP cells (A) and A549 cells (B) were treated with increasing doses of ATN-224 alone or with the BCL2 inhibitor ABT-263, and cell death (96 hours) was determined.
|
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| S1121 |
TW-37TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 μM, 1.11 μM and 0.26 μM in cell-free assays, respectively. |
(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.
|
|
| S8048 |
Venetoclax (ABT-199, GDC-0199)Venetoclax (ABT-199, GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Phase 3. |
(C) OCI-AML2 cells were cultured for 1 day with or without the indicated doses of CB-839 and ABT-199; apoptosis was evaluated based on Annexin V staining. (D) MOLM-14 cells were cultured for 1 day with or without the indicated doses of CB-839 and ABT-199; apoptosis was evaluated based on Annexin-V staining. Histograms show data that are representative of 3 independent experiments. The response of the combination was compared with its single agents against the widely used Loewe model for drug-with-itself dose additivity using Chalice software26 and presented as an isobologram. *P < .05, **P < .01, ***P < .001.
|
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| S8759新 |
S55746 (S 055746,BCL201)S55746 (S 055746,BCL201) is a novel, orally active BCL-2 specific inhibitor (Ki = 1.3 nM) with poor affinity for BCL-XL and no significant binding to MCL-1, BFL-1 (BCL2A1/A1). The selectivity of S55746 for BCL-2 versus BCL-XL ranges from ~70 to 400 folds. |
||
| S2812 |
AT101AT101, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM in cell-free assays; does not inhibit BIR3 domain and BID. Phase 2. |
The cellular autophagy induced by the concentration of AT101 (5 μM) and APE1 siRNA was examined by confocal microscopy with the application of Cyto-IDr autophagy detection kit.
|
|
| S8061 |
SabutoclaxSabutoclax(BI-97C1) is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively. |
(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.
|
|
| S7790 |
A-1210477A-1210477 is a potent and selective MCL-1 inhibitor with Ki and IC50 of 0.454 nM and 26.2 nM, respectively, >100-fold selectivity over other Bcl-2 family members. |
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.
|
|
| 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. |
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| S8383 |
S63845S63845 is a new, selective MCL-1 inhibitor with the Kd value of 0.19 nM and has no discernible binding to the other BCL-2 members, BCL-2 or BCL-XL. |
||
| S8177 |
BH3I-1BH3I-1 is a Bcl-XL-BH3 domain interaction inhibitor with Ki of 2.4 μM (by fluorescence polarization ).It is a selective inhibitor of Bcl-2 family proteins. |
||
| S7800 |
A-1155463A-1155463, a highly potent and selective BCL-XL inhibitor, shows picomolar binding affinity to BCL-XL, and >1000-fold weaker binding to BCL-2 and related proteins BCL-W(Ki=19 nM) and MCL-1(Ki>440 nM). |
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.
|
|
| S7801 |
A-1331852A-1331852 is a potent and selectiveBCL-XL inhibitor and may be useful in the treatment of cancer, immune and autoimmune diseases. |
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.
|
|
| S7531 |
UMI-77UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family. |
(a) SVEC cells stably expressing FLAG-tBID 2A GFP-BCL-xL, FLAG-tBID 2A GFP-BCL-2 or FLAG-tBID 2A GFP-MCL-1 were transiently transfected with NOXA. Cell viability was analysed 24 h post-transfection by SYTOX Green dye exclusion and live-cell imaging using an IncuCyte imager. Error bars represent the s.e.m. of three independent experiments. (b) SVEC cells stably expressing FLAG-tBID 2A GFP-MCL-1 (MCL-1-dependent line) were treated with increasing concentrations of putative MCL-1 inhibitors UMI-77 or A-1210477. Cell viability was analysed 24 h post-treatment by SYTOX Green dye exclusion and live-cell imaging using an IncuCyte imager. Error bars represent the s.e.m. of three independent experiments. (c) MCL-1-dependent line was treated with UMI-77 or A-1210477 (both 10 μmol l−1) and analysed over time for cell viability by SYTOX Green dye exclusion and live-cell imaging using an IncuCyte imager. Error bars represent the s.e.m. of three independent experiments. (d,e) SVEC cells stably expressing FLAG-tBID 2A GFP-BCL-xL, FLAG-tBID 2A GFP-BCL-2 or FLAG-tBID 2A GFP-MCL-1 were treated with UMI-77 or A-1210477 (10 μM for 24 h) then cell viability was analysed by SYTOX Green dye exclusion and live-cell imaging using an IncuCyte imager (d) or by clonogenic survival assay (e). Error bars represent the s.e.m. of three independent experiments for d and s.d. of triplicate samples from a representative experiment carried out twice independently for e. In all cases, cells were treated with MCL-1 inhibitors in 3% FBS containing DMEM.
|
|
| S7105 |
BAM7BAM 7 is a direct and selective activator of proapoptotic Bax with EC50 of 3.3 μM. |
||
| S1057 |
Obatoclax Mesylate (GX15-070)Obatoclax Mesylate (GX15-070) is an antagonist of Bcl-2 with Ki of 0.22 μM in a cell-free assay, can assist in overcoming MCL-1 mediated resistance to apoptosis. 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.
|
|
| S7849 |
BDA-366BDA-366 is a small-molecule Bcl2-BH4 domain antagonist and binds BH4 with high affinity and selectivity. |
||
| S7126 |
Marinopyrrole A (Maritoclax)Marinopyrrole A (Maritoclax) is a selective Mcl-1 antagonist. It binds to Mcl-1, but not Bcl-XL, and targets Mcl-1 for proteasomal degradation. Maritoclax disrupts the interaction between Bim and Mcl-1 with an IC50 of 10.1 μM. |
||
| S8650 |
BTSA1BTSA1 is a pharmacologically optimized BAX activator that binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis. It effectively promotes apoptosis in leukemia cell lines and patient samples while sparing healthy cells. |
| 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 |
|---|---|---|---|
| S1002 |
ABT-737ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. 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. |
|
| S1001 |
Navitoclax (ABT-263)Navitoclax (ABT-263) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤1 nM in cell-free assays, but binds more weakly to Mcl-1 and A1. Phase 2. |
KP cells (A) and A549 cells (B) were treated with increasing doses of ATN-224 alone or with the BCL2 inhibitor ABT-263, and cell death (96 hours) was determined.
|
|
| S1121 |
TW-37TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 μM, 1.11 μM and 0.26 μM in cell-free assays, respectively. |
(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.
|
|
| S8048 |
Venetoclax (ABT-199, GDC-0199)Venetoclax (ABT-199, GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Phase 3. |
(C) OCI-AML2 cells were cultured for 1 day with or without the indicated doses of CB-839 and ABT-199; apoptosis was evaluated based on Annexin V staining. (D) MOLM-14 cells were cultured for 1 day with or without the indicated doses of CB-839 and ABT-199; apoptosis was evaluated based on Annexin-V staining. Histograms show data that are representative of 3 independent experiments. The response of the combination was compared with its single agents against the widely used Loewe model for drug-with-itself dose additivity using Chalice software26 and presented as an isobologram. *P < .05, **P < .01, ***P < .001.
|
|
| S8759新 |
S55746 (S 055746,BCL201)S55746 (S 055746,BCL201) is a novel, orally active BCL-2 specific inhibitor (Ki = 1.3 nM) with poor affinity for BCL-XL and no significant binding to MCL-1, BFL-1 (BCL2A1/A1). The selectivity of S55746 for BCL-2 versus BCL-XL ranges from ~70 to 400 folds. |
||
| S2812 |
AT101AT101, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM in cell-free assays; does not inhibit BIR3 domain and BID. Phase 2. |
The cellular autophagy induced by the concentration of AT101 (5 μM) and APE1 siRNA was examined by confocal microscopy with the application of Cyto-IDr autophagy detection kit.
|
|
| S8061 |
SabutoclaxSabutoclax(BI-97C1) is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively. |
(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.
|
|
| S7790 |
A-1210477A-1210477 is a potent and selective MCL-1 inhibitor with Ki and IC50 of 0.454 nM and 26.2 nM, respectively, >100-fold selectivity over other Bcl-2 family members. |
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.
|
|
| 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. |
||
| S8383 |
S63845S63845 is a new, selective MCL-1 inhibitor with the Kd value of 0.19 nM and has no discernible binding to the other BCL-2 members, BCL-2 or BCL-XL. |
||
| S8177 |
BH3I-1BH3I-1 is a Bcl-XL-BH3 domain interaction inhibitor with Ki of 2.4 μM (by fluorescence polarization ).It is a selective inhibitor of Bcl-2 family proteins. |
||
| S7800 |
A-1155463A-1155463, a highly potent and selective BCL-XL inhibitor, shows picomolar binding affinity to BCL-XL, and >1000-fold weaker binding to BCL-2 and related proteins BCL-W(Ki=19 nM) and MCL-1(Ki>440 nM). |
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.
|
|
| S7801 |
A-1331852A-1331852 is a potent and selectiveBCL-XL inhibitor and may be useful in the treatment of cancer, immune and autoimmune diseases. |
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.
|
|
| S7531 |
UMI-77UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family. |
(a) SVEC cells stably expressing FLAG-tBID 2A GFP-BCL-xL, FLAG-tBID 2A GFP-BCL-2 or FLAG-tBID 2A GFP-MCL-1 were transiently transfected with NOXA. Cell viability was analysed 24 h post-transfection by SYTOX Green dye exclusion and live-cell imaging using an IncuCyte imager. Error bars represent the s.e.m. of three independent experiments. (b) SVEC cells stably expressing FLAG-tBID 2A GFP-MCL-1 (MCL-1-dependent line) were treated with increasing concentrations of putative MCL-1 inhibitors UMI-77 or A-1210477. Cell viability was analysed 24 h post-treatment by SYTOX Green dye exclusion and live-cell imaging using an IncuCyte imager. Error bars represent the s.e.m. of three independent experiments. (c) MCL-1-dependent line was treated with UMI-77 or A-1210477 (both 10 μmol l−1) and analysed over time for cell viability by SYTOX Green dye exclusion and live-cell imaging using an IncuCyte imager. Error bars represent the s.e.m. of three independent experiments. (d,e) SVEC cells stably expressing FLAG-tBID 2A GFP-BCL-xL, FLAG-tBID 2A GFP-BCL-2 or FLAG-tBID 2A GFP-MCL-1 were treated with UMI-77 or A-1210477 (10 μM for 24 h) then cell viability was analysed by SYTOX Green dye exclusion and live-cell imaging using an IncuCyte imager (d) or by clonogenic survival assay (e). Error bars represent the s.e.m. of three independent experiments for d and s.d. of triplicate samples from a representative experiment carried out twice independently for e. In all cases, cells were treated with MCL-1 inhibitors in 3% FBS containing DMEM.
|
| 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 |
|---|---|---|---|
| S7105 |
BAM7BAM 7 is a direct and selective activator of proapoptotic Bax with EC50 of 3.3 μM. |
| 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 |
|---|---|---|---|
| S1057 |
Obatoclax Mesylate (GX15-070)Obatoclax Mesylate (GX15-070) is an antagonist of Bcl-2 with Ki of 0.22 μM in a cell-free assay, can assist in overcoming MCL-1 mediated resistance to apoptosis. Phase 3. |
2017, 551(7679):247-250 2015, 10.1038/nchembio.1986 2011, 71(13):4494-505 |
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.
|
| S7849 |
BDA-366BDA-366 is a small-molecule Bcl2-BH4 domain antagonist and binds BH4 with high affinity and selectivity. |
||
| S7126 |
Marinopyrrole A (Maritoclax)Marinopyrrole A (Maritoclax) is a selective Mcl-1 antagonist. It binds to Mcl-1, but not Bcl-XL, and targets Mcl-1 for proteasomal degradation. Maritoclax disrupts the interaction between Bim and Mcl-1 with an IC50 of 10.1 μM. |
2019, 33(2):319-332 |
| 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 |
|---|---|---|---|
| S8650 |
BTSA1BTSA1 is a pharmacologically optimized BAX activator that binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis. It effectively promotes apoptosis in leukemia cell lines and patient samples while sparing healthy cells. |
