(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione

Product Name: (S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione
CAS No.: 847928-32-9
Chemical Name: (S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione
Synonyms: 1G244;1G-244,1G244;(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione;2-Amino-4-[4-[bis(4-fluorophenyl)methyl]-1-piperazinyl]-1-(1,3-dihydro-2H-isoindol-2-yl)-1,4-butaned;(2S)-2-amino-4-[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl]-1-(1,3-dihydroisoindol-2-yl)butane-1,4-dione;1,4-Butanedione, 2-amino-4-[4-[bis(4-fluorophenyl)methyl]-1-piperazinyl]-1-(1,3-dihydro-2H-isoindol-2-yl)-, (2S)-
CBNumber: CB23367548
Molecular Formula: C29H30F2N4O2
Formula Weight: 504.57
MOL File: 847928-32-9.mol

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(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione Property

Boiling point:: 674.3±55.0 °C(Predicted)
Density: 1.304±0.06 g/cm3(Predicted)
storage temp.: 2-8°C(protect from light)
solubility: Soluble in DMSO (>20 mg/ml)
pka: 7.25±0.33(Predicted)
form: solid
color: Off-white
Stability:: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0064911
Product name: 1G244
Purity: 98.55%
Packaging: 5mg
Price: $85
Updated: 2021/12/16

ChemScene

Product number: CS-0064911
Product name: 1G244
Purity: 98.55%
Packaging: 10mg
Price: $150
Updated: 2021/12/16

ChemScene

Product number: CS-0064911
Product name: 1G244
Purity: 98.55%
Packaging: 25mg
Price: $320
Updated: 2021/12/16

AK Scientific

Product number: Y0432
Product name: 1G244
Packaging: 10mg
Price: $389
Updated: 2021/12/16

Alichem

Product number: 847928329
Product name: (S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione
Packaging: 100mg
Price: $1163.25
Updated: 2021/12/16

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(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione Chemical Properties,Usage,Production

Description

1G244 (847928-32-9) is a potent and selective inhibitor of the prolyl dipeptidases DPP8 (IC50 = 14 nM) and DPP9 (IC50 = 53 nM).1,2? It does not inhibit DPP2, DPP4 or fibroblast activation protein (FAP) at 100 μM.1,2 1G244 is a slow binding competitive inhibitor of DPP8 but a competitive and reversible inhibitor of DPP9.2? Inhibition of DPP8/9 by 1G244 has been shown to cause pro-caspase-1-dependent pyroptosis in macrophages and monocytes.3 1G244 also induced cell death in DPP8/9 knockout cells at higher concentration indicating there may be some off-target effects.3 1G244 blocks adipogenesis in preadipocyte 3T3-L1 and 3T3-F422A cells.4? DPP8/9 inhibition attenuates PPARg2 induction during preadipocyte differentiation.4 Because of its inhibitory effects on pro-inflammatory macrophages, 1G244 inhibition of DPP8/9 has been examined as a potential therapy for reducing atherosclerosis and/or in the prevention of plaque rupture.5,6 Cell permeable.

Uses

1G244 is a potent DPP8/9 inhibitor with IC50s of 12 nM and 84 nM, respectively. 1G244 does not inhibit DPPIV and DPPII. 1G244 induces apoptosis in multiple myeloma cells and has anti-myeloma effects[1][2].

in vivo

1G244 (30 mg/kg; subcutaneous injection; once-a-week; for 3 weeks; NOG female mice) treatment apparently suppresses the subcutaneous growth of MM.1 S cells in murine xenograft model^[1].

Animal Model:	NOD/Shi-scid IL-2Rγnull (NOG) female mice (6-7 weeks; 19-21?g) injected with MM.1?S cells^[1]
Dosage:	30 mg/kg
Administration:	Subcutaneous injection; once-a-week; for 3 weeks
Result:	Apparently suppressed the subcutaneous growth of MM.1?S cells in murine xenograft model.

IC 50

DPP-4

References

[1] WEIR-TORN JIAANG. Novel Isoindoline Compounds for Potent and Selective Inhibition of Prolyl Dipeptidase DPP8.[J]. ChemInform, 2005, 36 25. DOI:10.1002/chin.200525117
[2] JIA-JING WU . Biochemistry, pharmacokinetics, and toxicology of a potent and selective DPP8/9 inhibitor[J]. Biochemical pharmacology, 2009, 78 2: Pages 203-210. DOI:10.1016/j.bcp.2009.03.032
[3] MARIAN C OKONDO. DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis[J]. Nature chemical biology, 2016, 13 1: 46-53. DOI:10.1038/nchembio.2229
[4] RUIJUN HAN. Inhibition of dipeptidyl peptidase 8/9 impairs preadipocyte differentiation.[J]. Scientific Reports, 2015: 12348. DOI:10.1038/srep12348
[5] VEERLE MATHEEUSSEN. Dipeptidyl peptidases in atherosclerosis: expression and role in macrophage differentiation, activation and apoptosis.[J]. Basic Research in Cardiology, 2013, 108 3: 350. DOI:10.1007/s00395-013-0350-4
[6] YANNICK WAUMANS. The Dipeptidyl Peptidases 4, 8, and 9 in Mouse Monocytes and Macrophages: DPP8/9 Inhibition Attenuates M1 Macrophage Activation in Mice.[J]. Inflammation, 2016, 39 1: 413-424. DOI:10.1007/s10753-015-0263-5

(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione Preparation Products And Raw materials

Raw materials

Preparation Products

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(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione Suppliers

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847928-32-9, (S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dioneRelated Search:

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(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione

1G244

(2S)-2-amino-4-[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl]-1-(1,3-dihydroisoindol-2-yl)butane-1,4-dione

1,4-Butanedione, 2-amino-4-[4-[bis(4-fluorophenyl)methyl]-1-piperazinyl]-1-(1,3-dihydro-2H-isoindol-2-yl)-, (2S)-

2-Amino-4-[4-[bis(4-fluorophenyl)methyl]-1-piperazinyl]-1-(1,3-dihydro-2H-isoindol-2-yl)-1,4-butaned

1G-244,1G244

847928-32-9

C29H30F2N4O2