| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
ZM-39923 (ZM-39923) is a novel and potent inhibitor of Janus kinase-JAK1/3 with potential anti-inflammatory activity. It inhibits JAK1/3 with pIC50s of 4.4/7.1, and shows little/no activity against JAK2 and modestly potency to EGFR; also found to be sensitive to transglutaminase.
| ln Vitro |
ZM39923 is a pIC50 of 7.1 JAK3 inhibitor. ZM39923 (compound 7) has no discernible inhibitory effect on tyrosine kinases Lck and CDK4 (pIC50<5.0), but it exhibits weak inhibitory effects on EGF-R and JAK1 (pIC50 are 5.6, 4.4, respectively) [1]. ZM39923 directly acts on purified TGM2, inhibiting the Ca2+-activated form of TGM2, and inhibits tissue transglutaminase (TGM2) with an IC50 of 10 nM[2]. ZM39923 has a similar effect to CCR7 antibodies in that it prevents JAK3 phosphorylation that is induced by CCL19. ZM39923 also considerably inhibits the migration and invasion of PCI-37B cells and blocks the rate of wound closure induced by CCL19 [3].
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| References |
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| Additional Infomation |
1-(2-naphthalenyl)-3-[(phenylmethyl)-propan-2-ylamino]-1-propanone is a member of naphthalenes.
ZM-39923 is a small molecule that inhibits Janus kinase and human tissue transglutaminase (TGM2). |
| Molecular Formula |
C23H25NO
|
|---|---|
| Molecular Weight |
331.45
|
| Exact Mass |
331.194
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| CAS # |
273727-89-2
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| Related CAS # |
ZM39923 hydrochloride;1021868-92-7
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| PubChem CID |
3797
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| Appearance |
Typically exists as solid at room temperature
|
| LogP |
5.323
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| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
25
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| Complexity |
412
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(C1=CC=C2C=CC=CC2=C1)CCN(C(C)C)CC3=CC=CC=C3
|
| InChi Key |
JSASWRWALCMOQP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H25NO/c1-18(2)24(17-19-8-4-3-5-9-19)15-14-23(25)22-13-12-20-10-6-7-11-21(20)16-22/h3-13,16,18H,14-15,17H2,1-2H3
|
| Chemical Name |
3-[benzyl(propan-2-yl)amino]-1-naphthalen-2-ylpropan-1-one
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| Synonyms |
ZM 39923 JAK3 inhibitor IV ZM-39923
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0170 mL | 15.0852 mL | 30.1705 mL | |
| 5 mM | 0.6034 mL | 3.0170 mL | 6.0341 mL | |
| 10 mM | 0.3017 mL | 1.5085 mL | 3.0170 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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