TW-37
Catalog No.S1121
Molecular Weight(MW): 573.7
TW-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.
9 Customer Reviews
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(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.
Cell Death Differ 2013 20, 1475-84. TW-37 purchased from Selleck.
(b) Whole-cell lysates of H23 cells exposed for 0–24 h to TW-37 (10 uM) were probed with antibodies against PARP and caspase-9. The appearance of both the p89 processed form of PARP and the p35 form of caspase-9 were characteristic of the intrinsic pathway of apoptosis.
Cell Death Differ 2013 20, 1475-84. TW-37 purchased from Selleck.
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(c) Whole-cell lysates of BAK-reconstituted and -deficient Jurkat cells exposed for 0–24 h to TW-37 (10 uM ) were probed as in B. % PS positive cells indicate the percentage of apoptotic cells, characterised by PS externalisation.
Cell Death Differ 2013 20, 1475-84. TW-37 purchased from Selleck.
(d) Electron micrographs of control and TW-37 (10 uM for 24 h); treated BAK-reconstituted and -deficient Jurkat cells reveal a dependence on BAK for TW-37- mediated apoptosis (scale bar, 5 um)
Cell Death Differ 2013 20, 1475-84. TW-37 purchased from Selleck.
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MCL-1 is a key anti-apoptotic BCL-2 family member that regulates ER membrane reorganisation. (a) Pan-BCL-2 family inhibitors induce ER membrane reorganisation more potently than BCL-2 and BCL-XL-specific inhibitors. Apogossypol (10 μM) and TW37 (20 μM) induced extensive membrane reorganisation, assessed by BAP31 staining in HeLa cells, within 4 h of exposure, whereas ABT-737 (20 μM) induced modest reorganisation after 8 h and the inactive enantiomer ABT-737E (20 μM) failed to induce reorganisation (scale bar, 20 μm).
Cell Death Differ 2012 19, 1896-907. TW-37 purchased from Selleck.
Cytotoxicity of TW-37 monotherapy. TTC549 cells and KP-MRTRY cells were seeded in 96-well plates, incubated for 24 h, treated with TW-37 (0-1,000 nM), and then analyzed. TW-37 IC50 values for the TTC549 and KP-MRT-RY cell lines were 554 and 588 nM, respectively.
J Cell Physiol, 2016, 231(9):1932-40. TW-37 purchased from Selleck.
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Sensitivity to ABT-199 and TW-37 in AML cell lines. Using ABT-199 and TW-37 to antagonise BCL-2 and MCL-1 respectively. The IC50s shown were obtained from alamar blue assays after treating 11 AML cell lines at a starting cell concentration of 2.5x105 /ml for 48 hours. Each cell line thawed is tested around the time of its final passage to authenticate its provenance using the Powerplex 16 kit to amplify short tandem repeats.
PLoS One, 2018, 13(1): e0190682. TW-37 purchased from Selleck.
MEF cells were treated for 24 hours with the Bcl-2 antagonists TW-37at the indicated doses.Acute survival was monitored by propidium iodide uptake assays(red lines).Long term survival(red line) was measured by replacing the drug-containing media with normal media and incubating the cells until visible colonies formed.Clonogenic survival is expressed relative to the numbers of colonies formed following 24 hours incubation in normal media(lacking drugs).
Dr. Christine Hawkins of La Trobe University. TW-37 purchased from Selleck.
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MDB-MA-231 cells were exposed to 30 um cisplatin in the absence or in thepresence of 100 nm TW-37.The cell were stained with Hoechst 33342,MitoTracker Red and Yo-pro-1.
Dr. Zhang of Tianjin Medical University. TW-37 purchased from Selleck.
Purity & Quality Control
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Biological Activity
| Description | TW-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. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Targets |
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| In vitro |
TW-37 targets the BH3-binding groove in Bcl-2 where proapoptotic Bcl-2 proteins bind, and shows higher affinity and selectivity for Bcl-2 and Mcl-1 over Bcl-xL with Ki values of 0.29 μM, 0.26 μM and 1.11 μM, respectively. [1] In vitro, TW-37 shows significant anti-proliferative and pro-apoptotic effect in a de novo chemo-resistant WSU-DLCL2 lymphoma cell line and primary cells obtained from a lymphoma patient without effects on normal peripheral blood lymphocytes. [1] TW-37 exhibits the inhibitory effect on both cell growth and cell death in endothelial cell with IC50 of approximately 1.8 μM without effect on the fibroblasts exposed to the same concentration range as the endothelial cells. In addition, TW37 also shows the anti-proliferation effects in MCF-7, LNCaP, and SLK tumor cell lines with the same or lower concentration range than those required to inhibit endothelial cell growth. [2] |
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| Cell Data |
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| In vivo | TW-37 shows a maximum tolerated dose (MTD) of 40 mg/kg for three i.v. injections in severe combined immunodeficient (SCID) mice when given alone, and enhances tumor inhibitory effect of cyclophosphamide-doxorubicin-vincristine-prednisone (CHOP) regimen. [1] TW-37, administrated by i.v. produces the antiangiogenic effect by decreasing the density of functional human microvessels in the severe combined immunodeficient mouse model of human angiogenesis. [2] The combination of TW-37 and MEK inhibitors synergistically block melanoma cell growth in mice by a significant reduction in tumor volume and tumor mass. [3] |
Protocol
| Kinase Assay:[1] |
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Fluorescence polarization-based binding assay for recombinant Bcl-2, Bcl-XL, and Mcl-1 protein : For this assay, the 21-residue BH3 peptide QEDIIRNIARHLAQVGDSMDR derived from Bid labeled with 6-carboxyfluorescein succinimidyl ester (FAM-Bid) and recombinant proteins derived from human Bcl-2,Bcl-X L,and Mcl-1 are employed. It is determined that FAM-Bid has a Ki of 11 nM to Bcl-2 protein,25 nM to Bcl-XL protein,and 5.7 nM to Mcl-1 protein. The competitive binding assay for Bcl-XL is same as that for Bcl-2 with the following exceptions: 30 nM Bcl-XL protein and 2.5 nM FAM-Bid peptide in the following assay buffer [50 mM Tris-Bis (pH 7.4) and 0.01% bovine gamma-globulin]. |
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| Cell Research:[2] |
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| Animal Research:[3] |
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Solubility (25°C)
| In vitro | DMSO | 115 mg/mL (200.45 mM) |
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| Ethanol | 4 mg/mL (6.97 mM) | |
| Water | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 30% propylene glycol, 5% Tween 80, 65% D5W For best results, use promptly after mixing. |
30 mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 573.7 |
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| Formula | C33H35NO6S |
| CAS No. | 877877-35-5 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
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