KMI169
Based on 1 Customer Validation
KMI169 is a potent and selective inhibitor targeting lysine methyl-transferase (KMT9) (IC50 = 0.05 μM, Kd = 0.025 μM). KMI169 functions as a bi-substrate inhibitor targeting the cofactor S-5’-adenosyl-L-methionine (SAM) and substrate binding pockets of KMT9. KMI169 can downregulate target genes involved in cell cycle regulation and impair proliferation of tumor cells by inhibiting KMT9. KMI169 is a valuable tool to probe cellular KMT9 functions and can be research for combating diseases including prostate, lung, colon, and invasive bladder cancer.
For research use only. We do not sell to patients.
- Purity: 98.00%
- Formula: C31H31Cl2N7O2
- Molecular Weight:604.53
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Storage:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
KMT9[1]
KMI169 (30 μM) only results in a 60% maximum inhibition against PRMT5, suggesting KMI169 does not target cellular PRMT5[1].
KMI169 (500 nM, 3 d) reduces the levels of H4K12mel, but does not alter histone markers such as H3K4me2, H3K9me2, and H4K20mel in PC-3M prostate tumor cells[1].
KMI169 (0.2-1 μM, 7 d) impairs proliferation of castration- and Enzalutamide (HY-70002)-resistant prostate cancer cell lines such as PC-3M, DU145, LNCaP-abl, and LNCaP-abl EnzaR, whereas proliferation of HepG2 and PANC-1 cells are not affected[1].
KMI169 (360 nM, 4 d) reduces mRNA levels for a selection of genes including MYB, AURKB, FOXA1, CDK2, BIRC5, E2F1, E2F8, CDC6, and LIG1[1].
KMI169 strongly reduces the proliferation of various cell lines such as J82 cells with a GI50 of 371 nM and RT-112 cells with a GI50 of 320 nM, as well as impairing proliferation of 5637, CAL-29, and UM-UC-3 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Prostate cancer cell lines PC-3M and LNCaP-abl
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Concentration:0.2-1 μM
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Incubation Time:7 d
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Result:Revealed strong stabilization of endogenous KMT9.
Did not stabilize PRMT5 under the same conditions.
Strongly suppressed the proliferation of PC-3M cells with a GI50 of 150 nM.
Chemical Information
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Appearance Solid
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Molecular Weight 604.53
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Formula C31H31Cl2N7O2
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Color White to off-white
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SMILES
NC1=C2C(C3=NN(C=C3Cl)CC4=CC=CC=C4)=CN([C@@H]5C[C@H](C6=CC(CN7CCC7)=CC=C6)[C@@H](O)[C@H]5O)C2=NC(Cl)=N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL (165.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.5 mg/mL (4.14 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Wang S, et al. Structure-guided design of a selective inhibitor of the methyltransferase KMT9 with cellular activity. Nat Commun. 2024 Jan 2;15(1):43. [Content Brief]
[2]. Totonji, S., et., (2024). Lysine Methyltransferase 9 (KMT9) Is an Actionable Target in Muscle-Invasive Bladder Cancer. Cancers, 16(8), 1532. [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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6542 mL | 8.2709 mL | 16.5418 mL | 41.3544 mL |
| 5 mM | 0.3308 mL | 1.6542 mL | 3.3084 mL | 8.2709 mL | |
| 10 mM | 0.1654 mL | 0.8271 mL | 1.6542 mL | 4.1354 mL | |
| 15 mM | 0.1103 mL | 0.5514 mL | 1.1028 mL | 2.7570 mL | |
| 20 mM | 0.0827 mL | 0.4135 mL | 0.8271 mL | 2.0677 mL | |
| 25 mM | 0.0662 mL | 0.3308 mL | 0.6617 mL | 1.6542 mL | |
| 30 mM | 0.0551 mL | 0.2757 mL | 0.5514 mL | 1.3785 mL | |
| 40 mM | 0.0414 mL | 0.2068 mL | 0.4135 mL | 1.0339 mL | |
| 50 mM | 0.0331 mL | 0.1654 mL | 0.3308 mL | 0.8271 mL | |
| 60 mM | 0.0276 mL | 0.1378 mL | 0.2757 mL | 0.6892 mL | |
| 80 mM | 0.0207 mL | 0.1034 mL | 0.2068 mL | 0.5169 mL | |
| 100 mM | 0.0165 mL | 0.0827 mL | 0.1654 mL | 0.4135 mL |
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