| 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 |
Purity: ≥98%
| Targets |
recombinant sACt ( IC50 = 3-10 μM )
Soluble adenylate cyclase (sAC, ADCY10) is the primary target of KH7. KH7 is a specific inhibitor of sAC with IC50 values of 3-10 µM against recombinant sACt proteins (human and others) in cells. sAC is a ubiquitously expressed enzyme that produces the second messenger cAMP independently of G protein-coupled receptors. Unlike transmembrane adenylyl cyclases, sAC is not regulated by G proteins but rather by bicarbonate and calcium. By inhibiting sAC, KH7 can block cAMP production in various cellular contexts, making it a valuable tool for studying sAC-dependent signaling pathways. |
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| ln Vitro |
KH7 (10 μM) inhibits this increase in cAMP caused by capture energy. In beer, KH7 significantly reduces basal cAMP accumulation, regardless of incubation medium, at higher concentrations (50 μM), 5 to 10 times higher than its IC50 and still selective against tmAC and sAC [1]. KH7 inhibits the synthesis of CaSF [2]. Myocytes exhibit a 20% negative inotropic effect (NIE) when KH7 is present, suggesting a role for sAC in the development of basal myocardial contractility [2].
KH7 is a specific inhibitor of soluble adenylate cyclase (sAC) with IC50 values of 3-10 µM against recombinant sACt proteins (human and others) in cells. It is also an inhibitor of cAMP. The compound exhibits IC50 values of 3–10 µM against both recombinant purified human sAC protein and heterologously expressed sAC in cellular assays. By inhibiting sAC, KH7 blocks the production of cAMP, a key second messenger involved in various cellular processes including metabolism, gene expression, and cell proliferation. The compound's specificity for sAC over other adenylyl cyclases makes it a valuable tool for dissecting sAC-dependent signaling pathways. |
| ln Vivo |
No specific in vivo activity data is publicly available for KH7. As an sAC inhibitor, KH7 would be expected to modulate cAMP-dependent processes in vivo. sAC is involved in various physiological processes including sperm maturation, insulin secretion, and regulation of mitochondrial function. By inhibiting sAC, KH7 could affect these processes in animal models. However, specific in vivo studies using KH7 have not been detailed in the available literature.
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| Enzyme Assay |
No specific non-cell assay protocol is available for KH7. For sAC inhibitors, standard cell-free assays use recombinant sAC protein and measure cAMP production from ATP. The compound is incubated with the enzyme and substrate, and cAMP production is measured by ELISA, radioimmunoassay, or mass spectrometry. These assays provide quantitative data on the compound's potency (IC50) against purified sAC protein. The selectivity of KH7 for sAC over other adenylyl cyclases can be assessed using related enzymes.
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| Cell Assay |
No specific cell-based assay protocol is available for KH7. For sAC inhibitors, standard cellular assays use cells expressing recombinant sAC or cells with endogenous sAC activity. Cells are treated with KH7, and intracellular cAMP levels are measured by ELISA or using cAMP biosensors. The compound's ability to inhibit sAC-mediated cAMP production in cells is assessed to determine cellular potency. Selectivity for sAC over transmembrane adenylyl cyclases can be assessed using cells that express both types of enzymes.
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| Animal Protocol |
No specific animal protocol is available for KH7. For studying sAC function in vivo, KH7 could be administered to animal models to investigate the role of sAC in various physiological and pathological processes. Potential applications include studying sAC in sperm maturation, insulin secretion, mitochondrial function, and other sAC-dependent processes. However, specific protocols for KH7 administration in vivo have not been detailed in the available literature.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data is publicly available for KH7. The compound has a molecular weight of 360.23 and formula C15H10BrN3OS. As a small molecule with moderate lipophilicity, it would be expected to have reasonable cell permeability. The compound is soluble in DMSO. Comprehensive pharmacokinetic studies would be required for any therapeutic application. For research use, the compound is typically dissolved in DMSO for in vitro studies.
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| Toxicity/Toxicokinetics |
No detailed toxicology data is publicly available for KH7. As a research compound, standard preclinical toxicology would be required for therapeutic development. The compound's selectivity for sAC may contribute to a manageable safety profile, though potential effects on other adenylyl cyclases or off-target proteins would need to be assessed. The compound is for research use only and not for therapeutic applications.
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| References |
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| Additional Infomation |
KH7 has the molecular formula C15H10BrN3OS and molecular weight 360.23. The chemical name is (E)-2-(1H-Benzo[d]imidazol-2-ylthio)-N'-(5-bromo-2-hydroxybenzylidene)acetohydrazide. It is a specific inhibitor of soluble adenylate cyclase (sAC) with IC50 values of 3-10 µM. It is also an inhibitor of cAMP. The compound is soluble in DMSO. No clinical trial status has been identified; it remains a research tool for studying sAC function and cAMP signaling.
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| Molecular Formula |
C17H15BRN4O2S
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|---|---|
| Molecular Weight |
419.297
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| Exact Mass |
418.009
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| Elemental Analysis |
C, 48.70; H, 3.61; Br, 19.06; N, 13.36; O, 7.63; S, 7.65
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| CAS # |
330676-02-3
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| PubChem CID |
135496218
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| Appearance |
White to light yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Index of Refraction |
1.716
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| LogP |
6.01
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
25
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| Complexity |
495
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C(N/N=C/C1=C(O)C=CC(Br)=C1)=O)SC1NC2=C(C=CC=C2)N=1
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| InChi Key |
WILMXUAKQKGGCC-DJKKODMXSA-N
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| InChi Code |
InChI=1S/C17H15BrN4O2S/c1-10(25-17-20-13-4-2-3-5-14(13)21-17)16(24)22-19-9-11-8-12(18)6-7-15(11)23/h2-10,23H,1H3,(H,20,21)(H,22,24)/b19-9+
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| Chemical Name |
2-(1H-benzimidazol-2-ylsulfanyl)-N-[(E)-(5-bromo-2-hydroxyphenyl)methylideneamino]propanamide
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| Synonyms |
KH-7; KH7; KH 7
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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, avoid exposure to moisture. |
| 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: ~250 mg/mL (~596.2 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.96 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.96 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.96 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3849 mL | 11.9246 mL | 23.8493 mL | |
| 5 mM | 0.4770 mL | 2.3849 mL | 4.7699 mL | |
| 10 mM | 0.2385 mL | 1.1925 mL | 2.3849 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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