| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg | |||
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| Other Sizes |
| Targets |
MEIS (Myeloid Ecotropic Insertion Site) transcription factors
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|---|---|
| ln Vitro |
The PBX-Luc reporter is not substantially inhibited by MEISi-2[1]. Hematopoietic stem cell self-renewal and maintenance are induced by MEISi-2 in a MEIS-dependent manner[1]. MEIS target gene expression is downregulated by MEISi-2[1]. -2 stimulates human (CD34+, CD133+, and ALDHhi cells) and murine (LSKCD34low cells) HSC self-renewal ex vivo[1].
MEISi-2 is a selective inhibitor of MEIS, a key regulator of hematopoietic stem cell (HSC) self-renewal. MEIS proteins are homeobox transcription factors that regulate gene expression during development and hematopoiesis. Inhibition of MEIS disrupts HSC self-renewal and differentiation, making MEISi-2 a valuable tool for studying hematopoiesis, stem cell biology, and cancer. The compound was developed for research into heart injury, hematopoietic problems, bone marrow transplantation, and cancer. |
| ln Vivo |
MEISi-2 (10 µM; ip; at day 1, day 4 and day 7) functionally suppresses MEIS in vivo, therefore they induces c-Kit+ cells, Sca1+ cells, CD150+ cells, LSK HSPCs, LSKCD34low HSC content and LSKCD150+CD48- HSC content[1]. MEISi-2 down-regulates Meis1 expression, Hif-2α, and critical CDKI gene expression including p16, p19, p19ARF[1].
In vitro studies of MEISi-2 evaluate its effects on hematopoietic stem cell self-renewal and differentiation. MEIS inhibition disrupts the balance between self-renewal and differentiation in HSCs, affecting hematopoietic progenitor cell populations. The compound's effects on cell proliferation, differentiation, and gene expression are assessed in relevant cell types. |
| Enzyme Assay |
MEIS activity and inhibition are assessed by measuring MEIS target gene expression using qRT-PCR or RNA-seq. MEIS-DNA binding is measured using chromatin immunoprecipitation (ChIP) assays. The compound's ability to inhibit MEIS-mediated transcription is evaluated in reporter gene assays.
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| Cell Assay |
Cellular potency is evaluated in hematopoietic stem cells and progenitor cells by measuring the effects of MEISi-2 on self-renewal, differentiation, and proliferation. Cells are treated with the compound at various concentrations, and cell population dynamics are analyzed by flow cytometry. Gene expression changes are assessed to confirm MEIS pathway modulation.
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| Animal Protocol |
Animal/Disease Models: 4-6 week-old balb/c (Bagg ALBino) mouse[1]
Doses: 10 µM/100 µL Route of Administration: intraperitoneal (ip)injection, at day 1, day 4 and day 7 Experimental Results: Modulated HSC pool. In vivo efficacy is evaluated in animal models of heart injury, hematopoietic disorders, and cancer. MEISi-2 is administered via appropriate routes at various doses. Hematopoietic stem cell function, tissue repair, and tumor growth are assessed. Pharmacodynamic biomarkers are measured to confirm target engagement and pathway modulation. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for MEISi-2 are limited as the compound is primarily used as a research tool. The compound is soluble in DMSO (100 mg/mL). Detailed PK parameters such as half-life, clearance, and bioavailability are available from preclinical studies.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for MEISi-2 are limited as the compound is primarily used for research purposes. Standard laboratory safety precautions should be observed during handling. The compound is not intended for human therapeutic use and has not been evaluated in formal toxicology studies.
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| References | |
| Additional Infomation |
MEISi-2 is a research tool for studying MEIS function in hematopoiesis, stem cell biology, and cancer. MEIS proteins are key regulators of hematopoietic stem cell self-renewal and are implicated in leukemogenesis and other cancers. MEISi-2 was developed for research into heart injury, hematopoietic problems, bone marrow transplantation, and cancer. The compound has a molecular formula of C19H21ClN6OS and a molecular weight of 416.93.
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| Molecular Formula |
C19H21CLN6OS
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|---|---|
| Molecular Weight |
416.927640676498
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| Exact Mass |
452.095
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| CAS # |
2375595-72-3
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| PubChem CID |
155971208
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
29
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| Complexity |
634
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| Defined Atom Stereocenter Count |
0
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| SMILES |
NC1C2C=CSC=2NC(=O)C=1C1=NC2=CC=C(N3CCN(C)CC3)C=C2N1.Cl
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| Chemical Name |
4-Hydroxybenzoic acid 2-[(Z)-(2-oxo-1(2H)-naphthalenylidene)methyl]hydrazide
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| Synonyms |
MEISi 2MEISi-2 MEISi2
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~220.6 mM; with ultrasonication)
H2O: ~25 mg/mL (~55.1 mM; with ultrasonication) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.51 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.51 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3985 mL | 11.9924 mL | 23.9848 mL | |
| 5 mM | 0.4797 mL | 2.3985 mL | 4.7970 mL | |
| 10 mM | 0.2398 mL | 1.1992 mL | 2.3985 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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