Page last updated: 2024-11-13

ap20187

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

AP20187: a nontoxic, cell-permeable analog, a wholly synthesized, cell-permeable dimeric FK506 derivative [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

AP20187 : A tertiary amino compound that is 2-(aminomethyl)-N,N-dimethylpropane-1,3-diamine in which the primary ammino groups have each been acylated by condensation with the carboxy group of 2-{3-[(1R)-3-(3,4-dimethoxyphenyl)-1-hydroxypropyl]phenoxy}acetic acid, the hydroxy groups of which have been esterified by condensation with the carboxy group of L-pipecolic acid, the nitrogen of which has been acylated by condensation with (2S)-2-(3,4,5-trimethoxyphenyl)butyric acid. It is a synthetic, cell-permeable ligand that can be used to induce homodimerization of fusion proteins containing the DmrB domain. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID78357784
CHEBI ID136847
SCHEMBL ID15806778
MeSH IDM0435891

Synonyms (21)

Synonym
ap20187
ap 20187
CHEBI:136847
195514-80-8
b/b homodimerizer
(1r)-3-(3,4-dimethoxyphenyl)-1-{3-[2-({3-[2-(3-{(1r)-3-(3,4-dimethoxyphenyl)-1-[({(2s)-1-[(2s)-2-(3,4,5-trimethoxyphenyl)butanoyl]piperidin-2-yl}carbonyl)oxy]propyl}phenoxy)acetamido]-2-[(dimethylamino)methyl]propyl}amino)-2-oxoethoxy]phenyl}propyl (2s)-1
CS-1953
HY-13992
SCHEMBL15806778
AC-33599
AKOS030526693
EX-A3907
(S,2S,2'S)-(1R,1'R)-(((((2-((DIMETHYLAMINO)METHYL)PROPANE-1,3-DIYL)BIS(AZANEDIYL))BIS(2-OXOETHANE-2,1-DIYL))BIS(OXY))BIS(3,1-PHENYLENE))BIS(3-(3,4-DIMETHOXYPHENYL)PROPANE-1,1-DIYL) BIS(1-((S)-2-(3,4,5-TRIMETHOXYPHENYL)BUTANOYL)PIPERIDINE-2-CARBOXYLATE)
A936437
{2-[(dimethylamino)methyl]-1,3-propanediyl}bis[imino(2-oxo-2,1-ethanediyl)oxy-3,1-phenylene(1r)-3-(3,4-dimethoxyphenyl)-1,1-propanediyl] (2s,2's)bis{1-[(2s)-2-(3,4,5-trimethoxyphenyl)butanoyl]-2-piper idinecarboxylate}
F84990
MS-32182
[(1r)-3-(3,4-dimethoxyphenyl)-1-[3-[2-[[2-[[[2-[3-[(1r)-3-(3,4-dimethoxyphenyl)-1-[(2s)-1-[(2s)-2-(3,4,5-trimethoxyphenyl)butanoyl]piperidine-2-carbonyl]oxypropyl]phenoxy]acetyl]amino]methyl]-3-(dimethylamino)propyl]amino]-2-oxoethoxy]phenyl]propyl] (2s)-
VHA51480
2,2'-[[2-[(dimethylamino)methyl]-1,3-propanediyl]bis[imino(2-oxo-2,1-ethanediyl)oxy-3,1-phenylene[(1r)-3-(3,4-dimethoxyphenyl)propylidene]]] bis[1-[(2s)-1-oxo-2-(3,4,5-trimethoxyphenyl)butyl]-2-piperidinecarboxylate]
DTXSID101098203

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Transplantation of hPSC-derived cell populations into preclinical models has generated teratomas (tumors arising from undifferentiated hPSCs), unwanted tissues, and other types of adverse events."( Improving the safety of human pluripotent stem cell therapies using genome-edited orthogonal safeguards.
Cromer, MK; Fowler, JL; Lesch, BJ; Loh, KM; Martin, RM; Nishimura, T; Ponce, E; Porteus, MH; Uchida, N, 2020
)
0.56

Dosage Studied

ExcerptRelevanceReference
" In vivo LFv2IRE transduction of insulin target tissues followed by AP20187 dosing may represent a therapeutic strategy to be tested in animal models of insulin resistance due to insulin receptor deficiency or of type I diabetes."( Pharmacological regulation of the insulin receptor signaling pathway mimics insulin action in cells transduced with viral vectors.
Auricchio, A; Beguinot, F; Cotugno, G; Formisano, P; Linher, K; Pollock, R, 2004
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
ligandAny molecule or ion capable of binding to a central metal atom to form coordination complexes.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (4)

ClassDescription
N-acylpiperidine
carboxylic esterAn ester of a carboxylic acid, R(1)C(=O)OR(2), where R(1) = H or organyl and R(2) = organyl.
aromatic etherAny ether in which the oxygen is attached to at least one aryl substituent.
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Research

Studies (82)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's37 (45.12)29.6817
2010's38 (46.34)24.3611
2020's7 (8.54)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 32.39

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index32.39 (24.57)
Research Supply Index4.42 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index42.91 (26.88)
Search Engine Supply Index2.04 (0.95)

This Compound (32.39)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other82 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]