NVP 231
Modify Date: 2024-01-09 16:34:42
NVP 231 structure
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Common Name | NVP 231 | ||
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| CAS Number | 362003-83-6 | Molecular Weight | 431.550 | |
| Density | 1.4±0.1 g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C25H25N3O2S | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | N/A | |
Use of NVP 231NVP-231 is a potent, specific, and reversible CerK inhibitor(IC50=12±2 nM) that competitively inhibits binding of ceramide to CerK.IC50 Value: 12±2 nM [1]Target: CERKin vitro: NVP-231 showed an IC50 value of 12 ± 2 nM and 90% inhibition at 100 nM in the radioassay. NVP-231 did not compete with ATP but rather with ceramide, displaying an inhibition constant (Ki) of 7.4 nM. Furthermore, inhibition by NVP-231 was instantaneous and fully reversible, implying that this compound does not covalently modify CerK. At 10 nM, NVP-231 inhibited C1P formation by >50%; at 100 nM, NVP-231 achieved complete inhibition. Thus the potency and efficacy of NVP-231 observed in cell culture are consistent with those found in vitro. It is noteworthy that, NVP-231 did not inhibit GlcCer and SM formation; rather, it increased these metabolites in correlation with compound concentration, demonstrating that NVP-231 does not act as a general inhibitor of ceramide metabolism [1]. The EC(50) of NVP-231 in this assay is in the low nanomolar range, consistent with the IC(50) determined in activity assays in vitro using purified CerK [2]. |
| Name | N-(2-benzamido-1,3-benzothiazol-6-yl)adamantane-1-carboxamide |
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| Synonym | More Synonyms |
| Description | NVP-231 is a potent, specific, and reversible CerK inhibitor(IC50=12±2 nM) that competitively inhibits binding of ceramide to CerK.IC50 Value: 12±2 nM [1]Target: CERKin vitro: NVP-231 showed an IC50 value of 12 ± 2 nM and 90% inhibition at 100 nM in the radioassay. NVP-231 did not compete with ATP but rather with ceramide, displaying an inhibition constant (Ki) of 7.4 nM. Furthermore, inhibition by NVP-231 was instantaneous and fully reversible, implying that this compound does not covalently modify CerK. At 10 nM, NVP-231 inhibited C1P formation by >50%; at 100 nM, NVP-231 achieved complete inhibition. Thus the potency and efficacy of NVP-231 observed in cell culture are consistent with those found in vitro. It is noteworthy that, NVP-231 did not inhibit GlcCer and SM formation; rather, it increased these metabolites in correlation with compound concentration, demonstrating that NVP-231 does not act as a general inhibitor of ceramide metabolism [1]. The EC(50) of NVP-231 in this assay is in the low nanomolar range, consistent with the IC(50) determined in activity assays in vitro using purified CerK [2]. |
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| Related Catalog | |
| References |
| Density | 1.4±0.1 g/cm3 |
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| Molecular Formula | C25H25N3O2S |
| Molecular Weight | 431.550 |
| Exact Mass | 431.166748 |
| PSA | 99.33000 |
| LogP | 5.34 |
| Index of Refraction | 1.743 |
| RIDADR | NONH for all modes of transport |
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~%
NVP 231 CAS#:362003-83-6 |
| Literature: US2009/170914 A1, ; Page/Page column 18 ; |
| Precursor 2 | |
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| DownStream 0 | |
| Tricyclo[3.3.1.1]decane-1-carboxamide, N-[2-(benzoylamino)-6-benzothiazolyl]- |
| nvp-231 |
| (3s,5s,7s)-N-[2-(Benzoylamino)-1,3-benzothiazol-6-yl]-1-adamantanecarboxamide |
| N-[2-(Benzoylamino)-1,3-benzothiazol-6-yl]-1-adamantanecarboxamide |
| NVP 231 |