Description
Key facts
CAS number:50264-69-2,
Purity:>98%,
Form:SolidSee storage information,
Molecular weight:321.2 Da,
Molecular formula:C15H10Cl2N2O2,
PubChem:39562,
Nature:Synthetic,
Solubility:Soluble in ethanol to 10 mMSoluble in DMSO to 100 mM,
Biochemical name:Lonidamine,
Biological description:Hexokinase inhibitor (IC50 = 850 μM). Anticancer, antiparasitic and antispermatogenic activity in vivo. Blocks open CFTR Cl- channels in vitro. Orally active.,
Canonical smiles:C1=CC=C2C(=C1)C(=NN2CC3=C(C=C(C=C3)Cl)Cl)C(=O)O,
InChi:InChI=1S/C15H10Cl2N2O2/c16-10-6-5-9(12(17)7-10)8-19-13-4-2-1-3-11(13)14(18-19)15(20)21/h1-7H,8H2,(H,20,21),
InChiKey:WDRYRZXSPDWGEB-UHFFFAOYSA-N,
IUPAC Name:1-[(2,4-dichlorophenyl)methyl]indazole-3-carboxylic acid
Properties and Storage Information:
Shipped at conditions-Ambient - Can Ship with Ice, Appropriate short-term storage conditions-Ambient, Appropriate long-term storage conditions-Ambient, Storage information-The product can be stored for up to 12 months
Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
Glucocorticoid Receptor also known as NR3C1 and Estrogen Receptor alpha also referred as ERα or ESR1 along with TSH Receptor (TSH-R) PXR (Pregnane X Receptor) and Estrogen Related Receptor alpha (ERRα or ESRRA) are part of a family of nuclear receptors. These receptors function as transcription factors that modulate gene expression upon binding with their respective ligands. Glucocorticoid Receptor for instance is around 94 kDa and is widely expressed in various tissues including the liver and immune cells. Estrogen Receptor alpha with a mass of about 66 kDa is mainly found in reproductive tissues. TSH-R is expressed predominantly in thyroid cells.
Biological function summary
These receptors play critical roles in regulating diverse physiological processes. Glucocorticoid Receptor mediates metabolic and immune system functions activating or repressing target genes. Estrogen Receptor alpha controls reproductive and sexual development while ERRα relates to energy metabolism. TSH-R is vital in thyroid hormone synthesis. PXR is involved in detoxification processes. None of these receptors works in isolation; they often form complexes with co-activators or co-repressors to synergistically drive their biological roles.
Pathways
The pathways these receptors integrate into are intricate and highly regulated. Glucocorticoid Receptor is central to the hypothalamic-pituitary-adrenal (HPA) axis which influences stress responses and metabolic homeostasis. It interacts closely with the NF-κB pathway impacting immune responses. Estrogen Receptor alpha can activate the MAPK/ERK pathway influencing cell proliferation and apoptosis. TSH-R is critical in the cAMP signaling pathway impacting thyroid function and hormone production.
Abnormalities in these receptors' functions link to various health issues. Glucocorticoid Receptor malfunctions can contribute to disorders like Cushing's syndrome or Addison's disease due to its regulatory role in metabolism and stress adaptation. Estrogen Receptor alpha is heavily implicated in breast cancer development and progression due to its regulation of cell proliferation. Aberrations in TSH-R can lead to thyroid disorders such as Graves' disease. These pathways frequently interact with other proteins such as Aromatase in cancer or CRH in adrenal disorders illustrating the complexity of their roles in health and disease.
