2. Epigenetics
  3. Epigenetic Reader Domain
  4. Menin-MLL inhibitor-22

Menin-MLL inhibitor-22 (compound C20) is an orally active inhibitor of the interaction between menin and mixed lineage leukemia (MLL) (IC50=7 nM). Menin-MLL inhibitor-22 binds menin protein and inhibits cancer cell growth (MV4 cells, IC50=0.3 μM). Menin is a putative tumor suppressor associated with multiple endocrine neoplasia type 1 (MEN-1 syndrome).

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Menin-MLL inhibitor-22 Chemical Structure

Menin-MLL inhibitor-22 Chemical Structure

CAS No. : 2851841-61-5

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Based on 1 publication(s) in Google Scholar

Menin-MLL inhibitor-22 Related Antibodies

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Description

Menin-MLL inhibitor-22 (compound C20) is an orally active inhibitor of the interaction between menin and mixed lineage leukemia (MLL) (IC50=7 nM). Menin-MLL inhibitor-22 binds menin protein and inhibits cancer cell growth (MV4 cells, IC50=0.3 μM). Menin is a putative tumor suppressor associated with multiple endocrine neoplasia type 1 (MEN-1 syndrome)[1].

In Vitro

Menin-MLL inhibitor-22 (1 μM; 60 min) possesses good stability and low clearance rate in liver microsomes[1].
Menin-MLL inhibitor-22 (1 and 10 μM; 24 h) inhibits MLL-r Leukemia cells MV4;11 growth and (0.1-10 μM; 24 h) decreases the expression of the HOXA9 and MEIS1 induced by menin-MLL interaction[1].
Menin-MLL inhibitor-22 (1, and 10 μM; 7 d) increases the amount of CD11b, a differentiation marker of myeloid cells, indicating a reverse the differentiation arrest of MLL-r leukemia cells[1].
Menin-MLL inhibitor-22 (1, and 10 μM; 24 h) induces cell apoptosis and G0/G1 cell cycle arrest[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Menin-MLL inhibitor-22 Related Antibodies

RT-PCR[1]

Cell Line: MLL-r Leukemia cells MV4;11
Concentration: 0.1, 1, and 10 μM
Incubation Time: 24 hours
Result: Reversed the over-expressing HOXA9 and MEIS1 induced by menin-MLL interaction, decreased the level of HOXA9 and MEIS1.

Apoptosis Analysis[1]

Cell Line: MLL-r Leukemia cells MV4;11
Concentration: 1, and 10 μM
Incubation Time: 24 hours
Result: Decreased in the population of cells in the S and G2/M phases, arrested cell cycle at G0/G1 phase.
In Vivo

Menin-MLL inhibitor-22 (6 mg/kg and 30 mg/kg; p.o.; every second day for 16 days) shows potent antitumor activity in the MV4;11 subcutaneous xenograft models of MLL-rearranged leukemia[1].

Pharmacokinetic Properties in SD Rats[1]

Route Dose (mg/kg) Tmax (h) T1/2 (h) MRT (h) Cmax (ng/mL) AUC0-t (ng·h/mL) AUC0-∞ (ng·h/mL) Cltotal (mL/h/kg) Vss (L/kg) F (%)
i.v. 5 N/A 17.5 7.1 1187 1700 2495 2056 49.3
p.o. 15 7.3 15.5 12.0 56.7 863.7 1476 10730 23 16.9

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb/C nude mice bearing MV4;11 cell xenografts[1]
Dosage: 6 mg/kg, 30 mg/kg
Administration: Oral gavage; every second day for 16 days
Result: Reduced the volume of tumor in mice.
Molecular Weight

565.73

Formula

C29H39N7O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC=C(N2CC(CN3CCC(NC4=NC=NC5=CC=C(N=C54)OCCN(C)C)CC3)C2)C=C1)(C6CC6)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (220.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7676 mL 8.8381 mL 17.6763 mL
5 mM 0.3535 mL 1.7676 mL 3.5353 mL
View the 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

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. 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 1.7676 mL 8.8381 mL 17.6763 mL 44.1907 mL
5 mM 0.3535 mL 1.7676 mL 3.5353 mL 8.8381 mL
10 mM 0.1768 mL 0.8838 mL 1.7676 mL 4.4191 mL
15 mM 0.1178 mL 0.5892 mL 1.1784 mL 2.9460 mL
20 mM 0.0884 mL 0.4419 mL 0.8838 mL 2.2095 mL
25 mM 0.0707 mL 0.3535 mL 0.7071 mL 1.7676 mL
30 mM 0.0589 mL 0.2946 mL 0.5892 mL 1.4730 mL
40 mM 0.0442 mL 0.2210 mL 0.4419 mL 1.1048 mL
50 mM 0.0354 mL 0.1768 mL 0.3535 mL 0.8838 mL
60 mM 0.0295 mL 0.1473 mL 0.2946 mL 0.7365 mL
80 mM 0.0221 mL 0.1105 mL 0.2210 mL 0.5524 mL
100 mM 0.0177 mL 0.0884 mL 0.1768 mL 0.4419 mL
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Menin-MLL inhibitor-22 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Menin-MLL inhibitor-222851841-61-5Epigenetic Reader Domainmultiple endocrine neoplasia type 1MEN-1 syndrometumor suppressorInhibitorinhibitorinhibit

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