ID-8DYRK inhibitor CAS# 147591-46-6 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 147591-46-6 | SDF | Download SDF |
| PubChem ID | 791637 | Appearance | Powder |
| Formula | C16H14N2O4 | M.Wt | 298.29 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 47 mg/mL (157.56 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 1-(4-methoxyphenyl)-2-methyl-3-nitroindol-6-ol | ||
| SMILES | CC1=C(C2=C(N1C3=CC=C(C=C3)OC)C=C(C=C2)O)[N+](=O)[O-] | ||
| Standard InChIKey | VVZNWYXIOADGSW-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C16H14N2O4/c1-10-16(18(20)21)14-8-5-12(19)9-15(14)17(10)11-3-6-13(22-2)7-4-11/h3-9,19H,1-2H3 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Sustains self-renewal and pluripotency of mouse embryonic stem cells (ESCs) in vitro. Stimulates proliferation at a steady rate (observed in serum-free media supplemented with 10 μM over a 30 day period). |
ID-8 Dilution Calculator
ID-8 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.3524 mL | 16.7622 mL | 33.5244 mL | 67.0488 mL | 83.8111 mL |
| 5 mM | 0.6705 mL | 3.3524 mL | 6.7049 mL | 13.4098 mL | 16.7622 mL |
| 10 mM | 0.3352 mL | 1.6762 mL | 3.3524 mL | 6.7049 mL | 8.3811 mL |
| 50 mM | 0.067 mL | 0.3352 mL | 0.6705 mL | 1.341 mL | 1.6762 mL |
| 100 mM | 0.0335 mL | 0.1676 mL | 0.3352 mL | 0.6705 mL | 0.8381 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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ID-8 is a small molecule inhibitor of DYRK [1].
Dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) is an enzyme that catalyzes autophosphorylation on tyrosine and serine/threonine residues.
ID-8 is a small molecule DYRK inhibitor. In HES2 cells, ID-8 (0.5 μM) increased hESC survival by 1.1%. The combination of ID-8 and Wnt3a increased survival by 1.7% and completely inhibited Wnt-induced morphological differentiation. Also, ID-8 significantly reduced the expression of differentiation marker gene GATA6, GSC, SOX17 and CDX2 induced by Wnt. In hESCs, ID-8 increased Wnt-mediated hESC proliferation and survival via inhibition of DYRKs. Also, DYRK family is direct targets of ID-8 [1]. In embryonic stem cells (ESCs), ID-8 (10 μM) stimulated proliferation in culture without MEFs, serum or LIF. The ID-8 induced ESCs showed the ability to form all three germ layer-derived tissues, such as liver, neurons and muscles. Also, ID-8 increased ESC differentiation and the levels of Nanog, Sox2 and Rex-1 [2]. In mouse ESCs cultured in serum-free medium, ID-8 maintained their self-renewal and pluripotency [3].
References:
[1]. Hasegawa K, Yasuda SY, Teo JL, et al. Wnt signaling orchestration with a small molecule DYRK inhibitor provides long-term xeno-free human pluripotent cell expansion. Stem Cells Transl Med, 2012, 1(1): 18-28.
[2]. Miyabayashi T, Yamamoto M, Sato A, et al. Indole derivatives sustain embryonic stem cell self-renewal in long-term culture. Biosci Biotechnol Biochem, 2008, 72(5): 1242-1248.
[3]. Firestone AJ, Chen JK. Controlling destiny through chemistry: small-molecule regulators of cell fate. ACS Chem Biol, 2010, 5(1): 15-34.
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Molecular pathways involved in response to ionizing radiation of ID-8 mouse ovarian cancer cells expressing exogenous full-length Brca1 or truncated Brca1 mutant.[Pubmed:11494042]
Int J Oncol. 2001 Sep;19(3):599-607.
BRCA1 germline mutations have been linked to the development of hereditary breast and ovarian cancers. Recent studies suggest that BRCA1 may function in the regulation of basic cellular processes, including gene transcription, and sensing and/or repair of DNA damage. To further delineate the BRCA1 upstream and downstream steps involved in its role in the cellular response to ionizing radiation, we compared the effects of expression of an exogenous full-length Brca1 with those of a truncated Brca1 mutant in the ID-8 mouse ovarian cancer cell line after irradiation. We found that expression of both full-length and truncated Brca1 increased resistance to ionizing radiation. Expression of truncated, but not full-length, Brca1 then allowed us to identify new potential downstream targets of mutated BRCA1 like MAPK/ERK pathway members and also key genes involved in mutated BRCA1 signaling pathway response to ionizing radiation such as p53 and p21WAF1/CIP1. We therefore established an in vitro mouse model for studying the molecular effects of human BRCA1 germline mutations.
Indole derivatives sustain embryonic stem cell self-renewal in long-term culture.[Pubmed:18460821]
Biosci Biotechnol Biochem. 2008 May;72(5):1242-8.
Embryonic stem cells (ESCs), which have characteristics such as self-renewal, indefinite proliferation, and pluripotency, are thought to hold great promise for regenerative medicine. ESCs are generally cultured on mouse embryonic fibroblast (MEF) or MEF conditioned medium (MEF-CM). However, for therapeutic applications, it is preferable for ESCs to be cultured under chemically defined conditions. Here, we report synthetic compounds that allow expansion of undifferentiated mouse ESCs in the absence of MEF, Leukemia Inhibitory Factor (LIF), and Fetal Bovine Serum (FBS). ESCs cultured for more than 30 d in a serum-free medium supplemented with indole derivertives retained their characteristic morphology and expressed markers such as SSEA-1, OCT3/4, Rex-1, Sox2, and Nanog. They consistently differentiated into many types of cells, including neurons, muscle cells, and hepatocytes. These results indicate that our compounds provide a more efficient and safer large-scale culture system for pluripotent ESCs, and hence might contribute to the use of ESCs in therapeutic applications.
