| Size | Price | Stock | Qty |
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| 5mg |
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| 50mg |
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SU3327 (SU-3327; Halicin) is a novel and potent JNK inhibitor with IC50 of 0.7 μM. Also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM.
| ln Vitro |
In HeLa cells (EC50=6.23 μM), SU3327 (Compound 9) can prevent TNF-α-stimulated c-Jun phosphorylation[1]. Polymorphonuclear leukocyte (PMN) rolling and attachment to human brain microvascular endothelial cells (hCMEC/D3) is efficiently reduced by SU3327 (25 nM). It also inhibits AP-1 activation and drastically lowers VCAM-1 expression[3].
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| ln Vivo |
In diabetic electrode models, SU3327 (Compound 9; 25 mg/kg; intraperitoneal injection; cosmetic BKS.Cg-+Leprdb/+Leprdb/+Leprdb/OlaHsd db/db electrode) can recuperate the insulin electrodes' processing capacity [1].
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| Animal Protocol |
Animal/Disease Models: Male BKS.Cg-+Leprdb/+Leprdb/OlaHsd db/db mice (11 weeks old) were injected with insulin [1]. ]
Doses: 25 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: Resulted in a statistically significant reduction in blood glucose levels. |
| References |
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| Additional Infomation |
Halicin is a member of the class of thiadiazoles that is 1,3,4-thiadiazol-2-amine which is substituted by a (5-nitro-1,3-thiazol-2-yl)sulfanediyl group at position 5. It is a c-Jun N-terminal kinase inhibitor (IC50 = 0.7uM) and exhibits antibacterial properties. It has a role as a c-Jun N-terminal kinase inhibitor and an antibacterial agent. It is a member of thiadiazoles, a member of 1,3-thiazoles, a primary amino compound, a C-nitro compound and an organic sulfide.
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| Molecular Formula |
C₅H₃N₅O₂S₃
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|---|---|
| Molecular Weight |
261.30
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| Exact Mass |
260.945
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| CAS # |
40045-50-9
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| PubChem CID |
11837140
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.888g/cm3
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| Boiling Point |
549.841ºC at 760 mmHg
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| Melting Point |
160 °C(dec.)
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| Flash Point |
286.334ºC
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| Index of Refraction |
1.793
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| LogP |
2.089
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
15
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| Complexity |
251
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NQQBNZBOOHHVQP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C5H3N5O2S3/c6-3-8-9-5(14-3)15-4-7-1-2(13-4)10(11)12/h1H,(H2,6,8)
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| Chemical Name |
5-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3,4-thiadiazol-2-amine
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| Synonyms |
SU-3327 SU 3327
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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) |
DMSO : ~62.5 mg/mL (~239.19 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.96 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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: ≥ 2.08 mg/mL (7.96 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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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 | 3.8270 mL | 19.1351 mL | 38.2702 mL | |
| 5 mM | 0.7654 mL | 3.8270 mL | 7.6540 mL | |
| 10 mM | 0.3827 mL | 1.9135 mL | 3.8270 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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