| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
NF-κB; MMP-9; p38 MAP kinase
SM-7368 targets the NF-κB signaling pathway, specifically inhibiting TNF-α-stimulated NF-κB activation. The compound acts downstream of MAPK p38 activation, indicating that it targets a component of the signaling cascade between p38 and NF-κB. SM-7368 inhibits TNF-α-induced MMP-9 upregulation, which is mediated through NF-κB-dependent transcription. The compound shows selectivity for NF-κB over AP-1, as it does not inhibit AP-1 activity. By blocking NF-κB activation, SM-7368 reduces the expression of NF-κB target genes involved in inflammation, invasion, and metastasis. |
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| ln Vitro |
In the human colon derived crypt like HT-29 and Caco-2 epithelial cell lines, SM-7368 (5 μM) targets downstream of MAPK p38 activation[1].
SM-7368 inhibits TNF--α-induced MMP-9 upregulation in a concentration-dependent manner, reaching its peak activity at 10 μM. MMP-9 mRNA transcript accumulation and protein expression are suppressed by SM-7368 in response to TNFα. TNF-α induced NF-κB activity is severely inhibited by SM-7368, but AP-1 activity is not affected. The TNF-induced invasion of the human fibrosarcoma cell line HT1080 is severely inhibited by SM-7368[2].
TNF-α (20 ng/mL)-induced MMP-9 upregulation is significantly inhibited by SM-7368 (10-25 μM） This upregulation is almost entirely eliminated by 10 μM of SM-7368[2].
In vitro studies demonstrate that SM-7368 inhibits TNF-α-induced MMP-9 protein expression with maximal effect at 10 μM by blocking NF-κB activity in HT1080 human fibrosarcoma cells. The compound strongly inhibits TNF-α-induced NF-κB activity but does not affect AP-1 activity, indicating selectivity for the NF-κB pathway. SM-7368 targets downstream of MAPK p38 activation, suggesting that it inhibits a component of the signaling cascade that leads to NF-κB activation. The compound's ability to inhibit MMP-9 upregulation is relevant for studying tumor invasion and metastasis. |
| ln Vivo |
In vivo data for SM-7368 is limited in the available literature. Based on its mechanism as an NF-κB inhibitor that targets TNF-α-mediated signaling, the compound is expected to demonstrate activity in animal models of tumor invasion, metastasis, and inflammation. By inhibiting NF-κB activation and MMP-9 upregulation, SM-7368 may reduce tumor cell invasion and metastatic spread. The compound can be used for research on chemotherapies targeting TNF-α-mediated tumor invasion and metastasis. Further in vivo studies are warranted to fully characterize the compound's efficacy in various cancer models.
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| Enzyme Assay |
The in vitro enzyme/receptor binding assay for SM-7368 involves measuring NF-κB activation using reporter gene assays or electrophoretic mobility shift assays (EMSA). Cells (e.g., HT1080) are stimulated with TNF-α (10 ng/mL) in the presence of varying concentrations of SM-7368 (0.1-100 μM) for 1-6 hours. NF-κB DNA binding activity is assessed by EMSA using radiolabeled NF-κB consensus oligonucleotides. NF-κB-dependent transcriptional activity is measured using luciferase reporter constructs. MMP-9 protein expression is measured by Western blot or gelatin zymography. AP-1 activity is measured as a control for selectivity. IC50 values are determined from dose-response curves using non-linear regression analysis.
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| Cell Assay |
In vitro cellular assays for SM-7368 typically use HT1080 human fibrosarcoma cells or other cancer cell lines. Cells are cultured in appropriate media and treated with the compound at concentrations of 0.1-100 μM for 1-24 hours, followed by TNF-α stimulation (10 ng/mL). MMP-9 expression is measured by Western blot, gelatin zymography, or ELISA. NF-κB activation is assessed by measuring phosphorylated IκB-α, nuclear translocation of p65, or NF-κB DNA binding activity. Cell viability is assessed using MTT or CCK-8 assays. Cell invasion is evaluated using Transwell invasion assays. Cell migration is assessed using wound healing assays.
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| Animal Protocol |
In vivo animal studies for SM-7368 would typically involve mouse models of tumor invasion and metastasis. Mice bearing tumors are treated with the compound via oral gavage, intraperitoneal injection, or tail vein injection at doses of 1-50 mg/kg daily or on a scheduled basis for 2-4 weeks. Tumor volume is measured regularly. Metastasis is assessed by examining lung or other organs for metastatic nodules. MMP-9 expression in tumor tissues is measured by immunohistochemistry or Western blot. NF-κB activation in tumor tissues is assessed by immunohistochemistry for p65 nuclear localization. Survival analysis is performed.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of SM-7368 are not extensively reported. The compound has a molecular weight of 328.68 and is cell-permeable. It is soluble in DMSO and other organic solvents. The compound should be stored at -20°C for long-term preservation. Based on its physicochemical properties, the compound is expected to have reasonable membrane permeability and tissue penetration. Further studies on oral bioavailability, plasma half-life, clearance, volume of distribution, and protein binding are needed to fully characterize its PK profile. The compound's cell-permeability makes it suitable for both in vitro and in vivo studies.
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| Toxicity/Toxicokinetics |
Toxicological data for SM-7368 is not extensively reported. As an NF-κB inhibitor, the compound may affect immune function and inflammatory responses. The compound is for research use only and not for human therapeutic applications. Standard safety precautions should be followed when handling. For detailed toxicity information, including acute toxicity, genotoxicity, and organ-specific toxicity, specialized toxicological studies would need to be performed in appropriate animal models.
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| References |
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| Additional Infomation |
SM-7368 (NF-κB Activation Inhibitor III) is a research-grade compound with CAS number 380623-76-7. Its molecular weight is 328.68. The compound is a cell-permeable inhibitor of TNF-α-induced MMP-9 upregulation and NF-κB activation. It targets downstream of MAPK p38 activation. The compound can be used for research on chemotherapies targeting TNF-α-mediated tumor invasion and metastasis. The mechanism of action involves inhibition of NF-κB signaling, leading to reduced MMP-9 expression and decreased tumor cell invasion. This compound has not advanced to clinical trials and is not FDA-approved. It is strictly for research purposes only.
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| Molecular Formula |
C10H5CLN4O5S
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|---|---|
| Molecular Weight |
328.68
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| Exact Mass |
327.967
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| Elemental Analysis |
C, 36.54; H, 1.53; Cl, 10.79; N, 17.05; O, 24.34; S, 9.75
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| CAS # |
380623-76-7
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| Related CAS # |
380623-76-7
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| PubChem CID |
11537217
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4.295
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
21
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| Complexity |
442
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=[N+](C1=CN=C(NC(C2C=CC([N+]([O-])=O)=C(Cl)C=2)=O)S1)[O-]
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| InChi Key |
XCHLNGBTHLJLFG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H5ClN4O5S/c11-6-3-5(1-2-7(6)14(17)18)9(16)13-10-12-4-8(21-10)15(19)20/h1-4H,(H,12,13,16)
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| Chemical Name |
3-chloro-4-nitro-N-(5-nitro-1,3-thiazol-2-yl)benzamide
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| Synonyms |
Activation Inhibitor III; SM-7368; SM7368; SM 7368;NF-kappaB
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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: 66~83.33 mg/mL (200.8~253.52 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.33 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 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0425 mL | 15.2124 mL | 30.4247 mL | |
| 5 mM | 0.6085 mL | 3.0425 mL | 6.0849 mL | |
| 10 mM | 0.3042 mL | 1.5212 mL | 3.0425 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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