URMC-099
Based on 7 publication(s) in Google Scholar
URMC-099 is an orally bioavailable and potent mixed lineage kinase type 3 (MLK3) (IC50=14 nM) inhibitor with with excellent blood-brain barrier penetration properties.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.69%
- No. CAS: 1229582-33-5
- Fòrmula: C27H27N5
- Peso molecular:421.54
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) URMC-099
More- Cell Death Dis. 2020 Jul 24;11(7):574. [Abstract]
- J Ethnopharmacol. 2021 Jun 28:274:114078. [Abstract]
- Cell Mol Life Sci. 2023 Jan 17;80(2):43. [Abstract]
- J Biol Chem. 2022 Aug;298(8):102263. [Abstract]
- Neurosci Lett. 2023 Jan 10:793:136990. [Abstract]
- University of Minnesota. 2025.
- bioRxiv. 2023 Sep 12:2023.09.09.557001. [Abstract]
Actividad biológica
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LRRK2 11 nM (IC50) |
FLT3 4 nM (IC50) |
FLT1 39 nM (IC50) |
ABL1 (T315I) 3 nM (IC50) |
ABL1 6.8 nM (IC50) |
SGK 67 nM (IC50) |
SGK1 201 nM (IC50) |
AurA 108 nM (IC50) |
AurB 123 nM (IC50) |
AurC 290 nM (IC50) |
IKKβ 257 nM (IC50) |
IKKα 591 nM (IC50) |
TNFα 460 nM (IC50) |
ROCK1 1030 nM (IC50) |
ROCK2 111 nM (IC50) |
CDK1 1125 nM (IC50) |
CDK2 1180 nM (IC50) |
TRKA 85 nM (IC50) |
c-MET 177 nM (IC50) |
TRKB 217 nM (IC50) |
IGF1R 307 nM (IC50) |
LCK 333 nM (IC50) |
MEKK2 661 nM (IC50) |
SYK 731 nM (IC50) |
AMPK 1512 nM (IC50) |
JNK1 3280 nM (IC50) |
SRC 4330 nM (IC50) |
ZAP70 5050 nM (IC50) |
ERK2 6290 nM (IC50) |
P38α 12050 nM (IC50) |
CYP3A4 16.2 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| BV-2 | IC50 |
0.46 μM
Compound: 1, URMC-099
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Inhibition of MLK3 in mouse BV2 cells assessed as inhibition of LPS-induced TNFalpha release after 8 hrs by ELISA
Inhibition of MLK3 in mouse BV2 cells assessed as inhibition of LPS-induced TNFalpha release after 8 hrs by ELISA
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[PMID: 24044867] |
| HEK293 | IC50 |
21 μM
Compound: 1, URMC-099
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Inhibition of human ERG tail current transfected in HEK293 cells by patch clamp assay
Inhibition of human ERG tail current transfected in HEK293 cells by patch clamp assay
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[PMID: 24044867] |
The effect of URMC-099 (URMC099) on the in vitro growth of the "brain homing" MDA-MB-231 BR cells expressing eGFP (eGFP8.4) and their parental cell line, MDA-MB-231 is tested. The cells are treated with either 200 nM URMC-099 or vehicle alone. Cells treated with URMC-099 grow at a similar rate to those treated with vehicle. Cell viability is >99% in all cases[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1229582-33-5
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Appearance Solid
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Peso molecular 421.54
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Fòrmula C27H27N5
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Color Off-white to yellow
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SMILES
CN(CC1)CCN1CC(C=C2)=CC=C2C3=CN=C4C(C(C5=CC=C(NC=C6)C6=C5)=CN4)=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
Pyroptosis and ferroptosis induced by mixed lineage kinase 3 (MLK3) signaling in cardiomyocytes are essential for myocardial fibrosis in response to pressure overload. [Abstract]2020 Jul 24;11(7):574. PMID: 32710001 -
J Ethnopharmacol
Xinyang Tablet inhibits MLK3-mediated pyroptosis to attenuate inflammation and cardiac dysfunction in pressure overload. [Abstract]2021 Jun 28:274:114078. PMID: 33798659 -
Cell Mol Life Sci
Opposing USP19 splice variants in TGF-β signaling and TGF-β-induced epithelial-mesenchymal transition of breast cancer cells. [Abstract]2023 Jan 17;80(2):43. PMID: 36646950 -
J Biol Chem
Phosphorylation of mixed lineage kinase MLK3 by cyclin-dependent kinases CDK1 and CDK2 controls ovarian cancer cell division. [Abstract]2022 Aug;298(8):102263. PMID: 35843311 -
Neurosci Lett
Murine cytomegalovirus employs the mixed lineage kinases family to regulate the spiral ganglion neuron cell death and hearing loss. [Abstract]2023 Jan 10:793:136990. PMID: 36455693 -
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bioRxiv
Multiplexed single-cell lineage tracing of mitotic kinesin inhibitor resistance in glioblastoma. [Abstract]2023 Sep 12:2023.09.09.557001. PMID: 37745469
Solvente y solubilidad
DMSO : ≥ 33 mg/mL (78.28 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.93 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.93 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
MDA-MB-231, MCF10A, HS578t and MDA-MB-231 EGFP8.4 cells are seeded in a 24 well plate at an initial density of 5.0×104 cells/mL in 0.5 mL of media. The cells are treated with either 200 µM of URMC-099 or vehicle (0.002% DMSO). Cell number in each well is measured by trypsinizing the cells and counting them with a hematocytometer. The viability is tested by trypan blue dye exclusion. Each condition is tested in triplicate[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
6 to 8 week old female nu/nu mice are injected intraperitoneally with URMC-099 at a dose of 10 mg/kg, or vehicle, twice daily for 20 days. On day 21 mice are sacrificed by CO2 suffocation. Brains are removed and fixed with 4% formaldehyde in PBS overnight, then transferred to 30% sucrose in PBS. The brains are then quickly frozen by immersing into isopentane cooled on dry ice. The frozen brains are sectioned coronally every 30 micrometers. Eight sections starting at bregma 2.0 and separated by 360 µm are mounted on glass slides for tumor evaluation under the microscope. The number of brain metastasis (BM) is counted by examining eGFP signals under a fluorescence microscope at 20× magnification[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (285 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Goodfellow VS, et al. Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. J Med Chem. 2013 Oct 24;56(20):8032-48. [Content Brief]
[2]. Rhoo KH, et al. Pharmacologic inhibition of MLK3 kinase activity blocks the in vitro migratory capacity of breast cancer cells but has no effect on breast cancer brain metastasis in a mouse xenograft model. PLoS One. 2014 Sep 29;9(9):e108487. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3723 mL | 11.8613 mL | 23.7225 mL | 59.3064 mL |
| 5 mM | 0.4745 mL | 2.3723 mL | 4.7445 mL | 11.8613 mL | |
| 10 mM | 0.2372 mL | 1.1861 mL | 2.3723 mL | 5.9306 mL | |
| 15 mM | 0.1582 mL | 0.7908 mL | 1.5815 mL | 3.9538 mL | |
| 20 mM | 0.1186 mL | 0.5931 mL | 1.1861 mL | 2.9653 mL | |
| 25 mM | 0.0949 mL | 0.4745 mL | 0.9489 mL | 2.3723 mL | |
| 30 mM | 0.0791 mL | 0.3954 mL | 0.7908 mL | 1.9769 mL | |
| 40 mM | 0.0593 mL | 0.2965 mL | 0.5931 mL | 1.4827 mL | |
| 50 mM | 0.0474 mL | 0.2372 mL | 0.4745 mL | 1.1861 mL | |
| 60 mM | 0.0395 mL | 0.1977 mL | 0.3954 mL | 0.9884 mL |
URMC-099 Related Classifications
HY-12599 Related Classifications
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