MM-589 |
| Katalog-Nr.GC33278 |
MM-589 ist ein potenter Inhibitor der WD-WiederholungsdomÄne 5 (WDR5) und der Protein-Protein-Interaktion bei gemischter LeukÄmie (MLL). MM-589 bindet an WDR5 mit einem IC50 von 0,90 nM und hemmt die MLL H3K4 Methyltransferase-AktivitÄt mit einem IC50 von 12,7 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2097887-20-0
Sample solution is provided at 25 µL, 10mM.
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MM-589 is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM[1].
MM-589 binds to WDR5 with high affinity (IC50=0.90 nM, Ki <1 nM) and potently inhibits the MLL HMT activity (IC50=12.7 nM)[1].MM-589 (0.01-10 µM, 4 days or 7 days) potently and selectively inhibits cell growth in human leukemia cell lines harboring MLL translocations[1].|| Cell Viability Assay[1]||Cell Line:|MV4-11 and MOLM-13|Concentration:|0.1, 1, 10 μM|Incubation Time:|4 days or 7 days|Result:|MM-589 potently inhibits MV4-11 and MOLM-13 cell growth with IC50s of 0.25 and 0.21 μM, respectively. MM-589 has much weaker activity in the inhibition of cell growth of the HL-60 cell line with an IC50 of 8.6 μM[1].
MM-589 has excellent microsomal stability in human, mouse, and rat microsomes (T1/2 > 60 min). Further optimization of MM-589 may yield a new therapy for acute leukemia[1].
[1]. Karatas H, et al. Discovery of a Highly Potent, Cell-Permeable Macrocyclic Peptidomimetic (MM-589) Targeting the WD Repeat Domain 5 Protein (WDR5)-Mixed Lineage Leukemia (MLL) Protein-Protein Interaction. J Med Chem. 2017 Jun 22;60(12):4818-4839.
| Cas No. | 2097887-20-0 | SDF | |
| Canonical SMILES | O=C(NCC[C@](NC(C(C)C)=O)(C)C1=O)[C@H](NC([C@@H](NC([C@H](CCCNC(NC)=N)N1)=O)CC)=O)C2=CC=CC=C2 | ||
| Formula | C28H44N8O5 | M.Wt | 572.7 |
| Löslichkeit | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.7461 mL | 8.7306 mL | 17.4611 mL |
| 5 mM | 349.2 μL | 1.7461 mL | 3.4922 mL |
| 10 mM | 174.6 μL | 873.1 μL | 1.7461 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)
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