Small molecule AG-205 inhibits Pgrmc1 (Progesterone Receptor Membrane Component 1), a heme-1 domain protein that promotes tumorigenesis.
IDNUMBER ST050150
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
Contact us to order. Prices are 0.1mg/$58.00, 0.5mg/$79.00, 1mg/$90.00 plus shipping.
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 |
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ST048271 C28H28N4OS 468.62 |
ST058667 C15H11Cl2N5OS 380.26 |
ST060724 C16H15N5OS 325.39 |
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ST064839 C13H16ClN5OS 325.82 |
ST065184 C13H17N5OS 291.38 |
ST065371 C15H18ClN5OS 351.86 |
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ST065559 C10H11N5OS 249.30 |
ST065560 C15H19N5OS 317.41 |
ST091913 C25H26N6OS 458.59 |
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ST4050448 C16H14ClN5OS 359.84 |
ST4064857 C16H11ClF3N5OS 413.81 |
ST4066640 C18H18ClN5OS 387.89 |
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ST4074479 C23H26N6O2S 450.56 |
ST4074690 C25H30N6OS 462.62 |
ST4075725 C23H18ClN5OS2 480.01 |
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ST4077097 C15H11Cl2N5OS 380.26 |
ST4091372 C17H16ClN5OS 373.87 |
ST4134537 C24H25N5OS 431.56 |
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ST4134557 C32H32N6OS 548.71 |
ST50053630 C15H12ClN5OS 345.81 |
ST50133623 C16H15N5OS 325.39 |
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ST50134402 C17H17N5OS 339.42 |
ST50600017 C15H11Cl2N5OS 380.26 |
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