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Technical Data
| Formula | C10H10N2O2S |
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| Molecular Weight | 222.26 | CAS No. | 327036-89-5 | |
| Solubility (25°C)* | In vitro | DMSO | 44.5 mg/mL (200.21 mM) | |
| Ethanol | 44.5 mg/mL (200.21 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | TDZD-8 (NP 01139) is a non-ATP competitive GSK-3β inhibitor with IC50 of 2 μM; minimal inhibitory effect observed on CDK1, casein kinase II, PKA and PKC. | ||
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| Targets |
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| In vitro | TDZD-8 acts as a noncompetitive inhibitor of ATP or GS-1 binding. TDZD-8 shows no inhibition of PKA, PKC, Cdk-1/cyclin B or CK-II in kinase assays. [1] TDZD-8 specifically induces cell death of primary leukemia specimens. TDZD-8 ablates leukemia progenitor and stem cells. TDZD-8 treatment induces oxidative stress. TDZD-8 induces cell death with extremely rapid cell death kinetics showing loss of membrane integrity. TDZD-8 inhibits PKC and FLT3 in primary AML specimens. [2] |
Protocol (from reference)
References
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Customer Product Validation
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Data from [Data independently produced by , , Int Immunopharmacol. 2017, 43:164-171.]
Selleck's TDZD-8 has been cited by 8 publications
| β-Catenin and SOX2 Interaction Regulate Visual Experience-Dependent Cell Homeostasis in the Developing Xenopus Thalamus [ Int J Mol Sci, 2023, 24(17)13593] | PubMed: 37686400 |
| GSK-3β inhibition alleviates arthritis pain via reducing spinal mitochondrial reactive oxygen species level and inflammation [ PLoS One, 2023, 18(4):e0284332] | PubMed: 37058473 |
| Glycogen synthase kinase-3β inhibition decreases inflammation and relieves cancer induced bone pain via reducing Drp1-mediated mitochondrial damage [ J Cell Mol Med, 2022, 26(14):3965-3976] | PubMed: 35689386 |
| The VRK1 chromatin kinase regulates the acetyltransferase activity of Tip60/KAT5 by sequential phosphorylations in response to DNA damage [ Biochim Biophys Acta Gene Regul Mech, 2022, 1865(8):194887] | PubMed: 36280132 |
| Activation of NRF2 ameliorates oxidative stress and cystogenesis in autosomal dominant polycystic kidney disease [ Sci Transl Med, 2020, 12(554):eaba3613] | PubMed: 32727915 |
| AMPK/GSK3β/β-catenin cascade–triggered overexpression of CEMIP promotes migration and invasion in anoikis-resistant prostate cancer cells by enhancing metabolic reprogramming [Zhang P FASEB J, 2018, 32(7):3924-3935] | PubMed: 29505302 |
| Identifying Host Regulators and Inhibitors of Liver Stage Malaria Infection Using Kinase Activity Profiles [ Nat Commun, 2017, 1;8(1):1232] | PubMed: 29089541 |
| Purinergic P2X7 receptor mediates acetaldehyde-induced hepatic stellate cells activation via PKC-dependent GSK3β pathway [Wu X Int Immunopharmacol, 2017, 43:164-171] | PubMed: 28061416 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.