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AB141840

Paxilline, Ca2+-activated K+channel blocker

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(1 Publication)

MW 435.6 Da, Purity >98%. Potent high-conductance Ca2+-activated K+channel blocker (Ki = 2 nM, α-subunit BKCa)Inhibits sarco/endoplasmic reticulum Ca2+-ATPase (IC50 = 5 - 50 μM). Shows anticonvulsant effects *in vivo.*.

View Alternative Names

DNA replication inhibitor, GEMI_HUMAN, GMNN, Geminin, Geminin DNA replication inhibitor, OTTHUMP00000039393, RP3 369A17.3

1 Images
Chemical Structure - Paxilline, Ca2+-activated K+channel blocker (AB141840)
  • Chemical Structure

Lab

Chemical Structure - Paxilline, Ca2+-activated K+channel blocker (AB141840)

2D chemical structure image of ab141840, Paxilline, Ca2+-activated K+channel blocker

Key facts

CAS number

57186-25-1

Purity

>98%

Form

Solid

form

Source

Penicillium paxilli

Molecular weight

435.6 Da

Molecular formula

C<sub>2</sub><sub>7</sub>H<sub>3</sub><sub>3</sub>NO<sub>4</sub>

PubChem

105008

Nature

Native

Solubility

Soluble in DMSO to 100 mM

Soluble in ethanol to 10 mM

Biochemical name

Paxilline

Biological description

Potent high-conductance Ca2+-activated K+channel blocker (Ki = 2 nM, α-subunit BKCa)Inhibits sarco/endoplasmic reticulum Ca2+-ATPase (IC50 = 5 - 50 μM). Shows anticonvulsant effects *in vivo.*

Canonical smiles

CC12CCC3C(=CC(=O)C(O3)C(C)(C)O)C1(CCC4C2(C5=C(C4)C6=CC=CC=C6N5)C)O

Isomeric smiles

C[C@]12CC[C@H]3C(=CC(=O)[C@H](O3)C(C)(C)O)[C@@]1(CC[C@@H]4[C@@]2(C5=C(C4)C6=CC=CC=C6N5)C)O

InChi

InChI=1S/C27H33NO4/c1-24(2,30)23-20(29)14-18-21(32-23)10-11-25(3)26(4)15(9-12-27(18,25)31)13-17-16-7-5-6-8-19(16)28-22(17)26/h5-8,14-15,21,23,28,30-31H,9-13H2,1-4H3/t15-,21-,23-,25+,26+,27+/m0/s1

InChiKey

ACNHBCIZLNNLRS-UBGQALKQSA-N

IUPAC Name

(1S,2R,5S,7R,11S,14S)-11-hydroxy-7-(2-hydroxypropan-2-yl)-1,2-dimethyl-6-oxa-23-azahexacyclo[12.10.0.02,11.05,10.016,24.017,22]tetracosa-9,16(24),17,19,21-pentaen-8-one

Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C
Storage information
Store under desiccating conditions|The product can be stored for up to 12 months

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

Geminin also referred to as GMNN is a protein that regulates DNA replication. It has approximately 25 kDa mass. Geminin inhibits DNA replication by preventing the loading of the mini-chromosome maintenance complex onto DNA during the cell cycle. This function ensures that DNA replication takes place only once per cell cycle. Geminin expresses mainly in tissues with high proliferative activity such as the developing nervous system and hematopoietic cells. Its interaction with other proteins plays a significant role in controlling cell cycle progression.
Biological function summary

In a cellular context Geminin forms part of a complex with the nuclear protein Cdt1. This complex is essential in the regulation of the cell cycle's S phase. Geminin's function restricts DNA replication by binding to Cdt1 and stopping its activity which is necessary during the G1/S phase transition. By doing so it preserves the integrity of genetic information and prevents re-replication. Geminin's inhibition remains strict until it is degraded during mitosis allowing Cdt1 to resume its function in the following cell cycle.

Pathways

The regulation of Geminin is important to maintaining proper DNA replication and cell cycle integrity. Geminin plays a role in the cell cycle control pathway particularly during the G1 to S phase transition. Additionally it interfaces with other proteins like Paxillin which is involved in cell adhesion and movement. Although not directly linked in a pathway Paxillin's role in regulating cellular dynamics can influence cell cycle processes in which Geminin is involved. Geminin also serves as a K blocker relevant in maintaining genetic stability.

Aberrations in Geminin activity can lead to severe conditions such as cancer. Its overexpression or misregulation has a link to various tumor types due to its effect on uncontrolled cell proliferation. Geminin's interaction with proteins like Paxillin and Cyclin-dependent kinases also relates to cancer progression as these interactions may involve changes in cellular adhesion and cycle checkpoints. Therefore understanding Geminin's role offers valuable insight for potential therapeutic targets in oncology.

Product protocols

Publications (1)

Recent publications for all applications. Explore the full list and refine your search

Acta biochimica et biophysica Sinica 54:1-11 PubMed36514218

2022

Deletion of large-conductance calcium-activated potassium channels promotes vascular remodelling through the CTRP7-mediated PI3K/Akt signaling pathway.

Applications

Unspecified application

Species

Unspecified reactive species

Jing Bi,Yanru Duan,Meili Wang,Chunyu He,Xiaoyue Li,Xi Zhang,Yan Tao,Yunhui Du,Huirong Liu
View all publications

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