All Photos(1)

SML2247

Sigma-Aldrich

1G244

≥98% (HPLC)

Synonym(s):
PTX 1210, 2-[(2S)-2-Amino-4-[4-[bis(4-fluorophenyl)methyl]-1-piperazinyl]-1,4-dioxobutyl]-2,3-dihydro-1H-isoindole, (2S)- 2-Amino-4-[4-[bis(4-fluorophenyl)methyl]-1-piperazinyl]-1-(1,3-dihydro-2H-isoindol-2-yl)-1,4-butanedione
Empirical Formula (Hill Notation):
C29H30F2N4O2
CAS Number:
Molecular Weight:
504.57
MDL number:
NACRES:
NA.77

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

O=C(C[C@@H](C(N1CC(C=CC=C2)=C2C1)=O)N)N3CCN(C(C4=CC=C(F)C=C4)C5=CC=C(F)C=C5)CC3

Biochem/physiol Actions

1G244 is known to exhibit in vitro anti-myeloma actions. It might be involved in inducing pyroptotic cell death without ASC (apoptosis-associated speck-like protein containing a CARD) or interleukin (IL)-1 cleavage in human macrophage-like cells.
1G244 is a cell penetrant, highly potent and specific inhibitor of dipeptidyl peptidase 8 (DPP8) and DPP9. 1G244 is a slow-tight binding competitive inhibitor of DPP8, but it is a competitive and reversible inhibitor of DPP9.

Storage Class Code

13 - Non Combustible Solids

WGK Germany

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificate of Analysis

Certificate of Origin

Franklin L Zhong et al.
The Journal of biological chemistry, 293(49), 18864-18878 (2018-10-07)
The inflammasome is a critical molecular complex that activates interleukin-1 driven inflammation in response to pathogen- and danger-associated signals. Germline mutations in the inflammasome sensor NLRP1 cause Mendelian systemic autoimmunity and skin cancer susceptibility, but its endogenous regulation remains less...
Tsutomu Sato et al.
Scientific reports, 9(1), 18094-18094 (2019-12-04)
Dipeptidyl peptidases (DPPs) are proteolytic enzymes that are ideal therapeutic targets in human diseases. Indeed, DPP4 inhibitors are widely used in clinical practice as anti-diabetic agents. In this paper, we show that DPP4 inhibitors also induced cell death in multiple...
Jelka Gabrilovac et al.
Immunobiology, 222(2), 327-342 (2016-09-30)
Dipeptidyl peptidase 9 (DPP9) is a relatively new member of the DPPIV family of prolyl dipeptidases which is ubiquitously expressed. Its role in regulation of immune responses and proliferation of epithelial carcinoma cells was reported. There is no data on...
Veerle Matheeussen et al.
Basic research in cardiology, 108(3), 350-350 (2013-04-24)
Atherosclerosis is a chronic inflammatory disorder of the arterial wall leading to coronary artery disease, stroke, and peripheral arterial disease. Along with the discovery of dipeptidyl peptidase 4 (DPP4) as a therapeutic target in type 2 diabetes, a role for...
Ruijun Han et al.
Scientific reports, 5, 12348-12348 (2015-08-06)
Adipocytes are the primary cells in adipose tissue, and adipocyte dysfunction causes lipodystrophy, obesity and diabetes. The dipeptidyl peptidase (DPP) 4 family includes four enzymes, DPP4, DPP8, DPP9 and fibroblast activation protein (FAP). DPP4 family inhibitors have been used for...

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