KL001
- Product Name
- KL001
- CAS No.
- 309928-48-1
- Chemical Name
- KL001
- Synonyms
- KL001(KL-001;N-(3-(9H-Carbazol-9-yl)-2-hydroxypropyl)-N-(furan-2-ylmethyl)methanesulfonamide;N-[3-(9H-Carbazol-9-yl)-2-hydroxypropyl]-N-(2-furanylmethyl)-methanesulfonamide;Methanesulfonamide, N-[3-(9H-carbazol-9-yl)-2-hydroxypropyl]-N-(2-furanylmethyl)-;Inhibitor,inhibit,stabilizer,KL001,circadian,cryptochrome,ubiquitin,period,gluconeogenesis,CRY
- CBNumber
- CB32695946
- Molecular Formula
- C21H22N2O4S
- Formula Weight
- 398.48
- MOL File
- 309928-48-1.mol
KL001 Property
- storage temp.
- 2-8°C
- solubility
- DMSO: soluble20mg/mL, clear
- form
- powder
- color
- white to beige
- Stability:
- Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
N-Bromosuccinimide Price
- Product number
- SML1032
- Product name
- KL001
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $104
- Updated
- 2024/03/01
- Product number
- SML1032
- Product name
- KL001
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $404
- Updated
- 2024/03/01
- Product number
- 13878
- Product name
- KL001
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $68
- Updated
- 2024/03/01
- Product number
- 13878
- Product name
- KL001
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $121
- Updated
- 2024/03/01
- Product number
- 13878
- Product name
- KL001
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $235
- Updated
- 2024/03/01
KL001 Chemical Properties,Usage,Production
Description
KL-001 (309928-48-1) is a novel tool that specifically interacts with cryptochrome (CRY) preventing its ubiquitin-dependent degradation resulting in lengthening of the circadian period. KL-001-mediated CRY stabilization inhibits glucagon-induced gluconeogenesis in primary hepatocytes.1?Binds to the FAD-binding pocket of CRY2 as determined by co-crystal structure.2?KL-001 induces an increase in period along with simultaneous reduction in amplitude of circadian reporter expression3 in mammalian cells.
Uses
KL001 is a small molecule that specifically interacts with cryptochrome (CRY). KL001 prevented ubiquitin-dependent degrdation of CRY, resulting in lengthening of the circadian period. KL001-mediated CRY stabilization inhibited glucagon-induced gluconeogenesis in primary hepatocytes making it a tool to study the regulation of CRY-dependent physiology and aid development of clock-based therapeutics of diabetes.
Biochem/physiol Actions
KL001 stabilizes cryptochrome (CRY), preventing ubiquitin-dependent degradation. CRY proteins are part of a feedback loop, acting as transcription repressors to inhibit CLOCK-BMAL1 components of the circadian clock. KL001 stabilization of CRY proteins results in lengthening of the circadian period, and also inhibited glucagon-induced gluconeogenesis in primary hepatocytes. Other compounds affecting circadian rhythms include Casein kinase I (CKI) inhibitors such as longdaysin (Sigma Prod. No. SML0127) and synthetic ligands for the nuclear receptors REV-ERB such as SR8278 (Sigma Prod. No. S9576), but KL001 appears to be the first small molecule that specifically acts on CRY proteins.
storage
Store at +4°C
References
1) Hirota et al. (2012), Identification of small molecule activators of cryptochrome; Science, 337 1094 2) Nangle et al. (2013), Crystal structure of mammalian cryptochrome in complex with a small molecule competitor of its ubiquitin ligase; Cell Res., 23 1417 3) St. John et al. (2014), Spatiotemporal separation of PER and CRY posttranslational regulation in the mammalian circadian clock; Proc. Natl. Acad. Sci. USA, 11 2040