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AG-205, Pgrmc1 Inhibitor


Small molecule AG-205 inhibits Pgrmc1 (Progesterone Receptor Membrane Component 1), a heme-1 domain protein that promotes tumorigenesis.

IDNUMBER ST050150 Order online

Formula: C22H23ClN6CS

MW: 454.98

IUPACNAME: [5-({[1-(4-chlorophenyl)-1H-tetraazol-5-yl]sulfanyl}acetyl)-2,8-

dimethyl-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole]

Smiles: n1(c(nnn1)SCC(N1C2C(CN(CC2)C)c2c1ccc(C)c2)=O)c1ccc(cc1)Cl

Reference:

Ahmed IS., et.al. Progesterone Receptor Membrane Component 1 (Pgrmc1): A Heme-1 Domain Protein That Promotes Tumorigenesis and Is Inhibited by a Small Molecule. J Pharmacol Exp Ther. May 2010 333, p564-573

Abstract

Tumorigenesis requires the concerted action of multiple pathways, including pathways that stimulate proliferation and increase metabolism. Progesterone receptor membrane component 1 (Pgrmc1) is related to cytochrome b5, binds to heme, and is associated with DNA damage resistance and apoptotic suppression. Pgrmc1 is induced by carcinogens, including dioxin, and is up-regulated in multiple types of cancer. In the present study, we found that Pgrmc1 increased in vivo tumor growth, anchorage-independent growth, and migration. Pgrmc1 also promoted proliferation in the absence of serum in A549 non-small cell lung cancer cells but enhanced proliferation regardless of serum concentration in MDA-MB-468 breast cancer cells. Pgrmc1 promotes cholesterol synthesis and binds to Insig (insulin-induced gene), Scap (sterol regulatory element binding protein cleavage activating protein), and P450 proteins, but Pgrmc1 did not affect cholesterol synthesis in lung cancer cells. Pgrmc1 is also associated with progesterone signaling and plasminogen activator inhibitor (PAI1) RNA binding protein, but neither progesterone activity nor PAI1 transcript levels were altered in Pgrmc1-knockdown lung cancer cells. Pgrmc1 homologues bind to aryl ligands identified in an in silico screen, and we have found that a Pgrmc1 ligand induced cell death in a Pgrmc1-specific manner in multiple breast and lung tumor cell lines. Our data support a role for Pgrmc1 in promoting cancer-associated phenotypes and provide a therapeutic approach for targeting Pgrmc1 with a small molecule in lung and breast cancer.

 

ST050150, Ag-205, was acquired from TimTec. Please view structurally similar molecules available for purchase.

Download AG-205 analog structures

Progesterone Receptor Membrane Component  1, ST050150, Analogs:

ST006253
C16H14ClN5OS
359.84
ST019077
C15H12ClN5OS
345.81
ST041902
C22H23ClN6O
422.92

ST048271
C28H28N4OS
468.62
ST058667
C15H11Cl2N5OS
380.26
ST060724
C16H15N5OS
325.39

ST064839
C13H16ClN5OS
325.82
ST065184
C13H17N5OS
291.38
ST065371
C15H18ClN5OS
351.86

ST065559
C10H11N5OS
249.30
ST065560
C15H19N5OS
317.41
ST091913
C25H26N6OS
458.59

ST4050448
C16H14ClN5OS
359.84
ST4064857
C16H11ClF3N5OS
413.81
ST4066640
C18H18ClN5OS
387.89

ST4074479
C23H26N6O2S
450.56
ST4074690
C25H30N6OS
462.62
ST4075725
C23H18ClN5OS2
480.01

ST4077097
C15H11Cl2N5OS
380.26
ST4091372
C17H16ClN5OS
373.87
ST4134537
C24H25N5OS
431.56

ST4134557
C32H32N6OS
548.71
ST50053630
C15H12ClN5OS
345.81
 ST50133623
C16H15N5OS
325.39

ST50134402
C17H17N5OS
339.42
ST50600017
C15H11Cl2N5OS
380.26

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