MW 321.2 Da, Purity >98%. Hexokinase inhibitor (IC50 = 850 μM). Anticancer, antiparasitic and antispermatogenic activity in vivo. Blocks open CFTR Cl- channels in vitro. Orally active.
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- Investigative ophthalmology & visual science 63:72022Branched Chain Amino Acids Promote ATP Production Via Translocation of Glucose Transporters.Applications:Unspecified applicationReactive species:Unspecified reactive speciesSachiko Iwai,Tomoko Hasegawa,Hanako Ohashi Ikeda,Akitaka TsujikawaPubMed 35930269
Key facts
- CAS number
- 50264-69-2
- Purity
- > 98%
- Form
- Solid
- Molecular weight
- 321.2 Da
- Molecular formula
- C15H10Cl2N2O2
- PubChem identifier
- 39562
- Nature
- Synthetic
Target data
Alternative names
Atherosclerosis, susceptibility to, included, BXR, CHNG1, DKFZp686N23123, ER, ER-alpha, ER-beta, ERR a, ERR-alpha, ERR1 protein, ERR1_HUMAN, ER[a], ER[b], ESR, ESR B, ESR BETA, ESR1_HUMAN, ESRA, ESRL 1, ESRR A, ESTR B, Era, Erb, Erb2, Estr, Estra, Estradiol Receptor alpha, Estradiol Receptor beta, Estradiol receptor, Estrogen Receptor 1, Estrogen Receptor 2, Estrogen receptor, Estrogen receptor 1 (alpha), Estrogen receptor 2 (ER beta), Estrogen receptor 2 ER beta, Estrogen receptor alpha, Estrogen receptor beta 4, Estrogen receptor related 1, Estrogen receptor-like 1, Estrogen resistance, included, Estrogen-related receptor alpha, Estrra, GCCR, GCRST, GCR_HUMAN, GR, Glucocorticoid receptor, Grl1, HDL cholesterol, augmented response of, to hormone replacement, included, LGR 3, MGC75129, Myocardial infarction, susceptibility to, included, NR1I2_HUMAN, NR3A1, NR3A2, NR3B1, Nuclear receptor subfamily 1 group I member 2, Nuclear receptor subfamily 3 group A member 1, Nuclear receptor subfamily 3 group A member 2, Nuclear receptor subfamily 3 group B member 1, Nuclear receptor subfamily 3 group C member 1, ONR 1, OTTHUMP00000017718, OTTHUMP00000017719, OTTHUMP00000215173, OTTHUMP00000215174, OTTHUMP00000215175, Orphan nuclear receptor PAR 1, Orphan nuclear receptor PXR, PAR, PAR q, PRR, Pregnane X receptor, RNESTROR, SXR, Seven transmembrane helix receptor, Steroid and xenobiotic receptor, Steroid hormone receptor ERR1, TSH Receptor, TSHR_HUMAN, Thyroid adenoma hyperfunctioning, Thyroid carcinoma with thyrotoxicosis, Thyroid stimulating hormone receptor, isoform 2, Thyroid-stimulating hormone receptor, Thyrotropin receptor, Thyrotropin receptor I, Thyrotropin receptor I, hTSHR I, estrogen receptor related receptor alpha, glucocorticoid nuclear receptor variant 1, hERR1, hTSHR I, nr3c1, nuclear receptor subfamily 3, group C, member 1 (glucocorticoid receptor), pregnane X nuclear receptor variant 2
Recommended products
MW 321.2 Da, Purity >98%. Hexokinase inhibitor (IC50 = 850 μM). Anticancer, antiparasitic and antispermatogenic activity in vivo. Blocks open CFTR Cl- channels in vitro. Orally active.
Key facts
- CAS number
- 50264-69-2
- Purity
- > 98%
- Form
- Solid
- Molecular weight
- 321.2 Da
- Molecular formula
- C15H10Cl2N2O2
- PubChem identifier
- 39562
- Nature
- Synthetic
- Solubility
Soluble in ethanol to 10 mM.
Soluble 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
Storage
- 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 info
- This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
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.
- Associated diseases and disorders
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.
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1 product image
Chemical Structure - Lonidamine, Hexokinase inhibitor (ab142442)
2D chemical structure image of ab142442, Lonidamine, Hexokinase inhibitor
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