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AB142442

Lonidamine, Hexokinase inhibitor

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(1 Publication)

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.

View 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

1 Images
Chemical Structure - Lonidamine, Hexokinase inhibitor (AB142442)
  • Chemical Structure

Lab

Chemical Structure - Lonidamine, Hexokinase inhibitor (AB142442)

2D chemical structure image of ab142442, Lonidamine, Hexokinase inhibitor

Key facts

CAS number

50264-69-2

Purity

>98%

Form

Solid

form

Molecular weight

321.2 Da

Molecular formula

C<sub>1</sub><sub>5</sub>H<sub>1</sub><sub>0</sub>Cl<sub>2</sub>N<sub>2</sub>O<sub>2</sub>

PubChem

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

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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
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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.
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Product protocols

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Publications (1)

Recent publications for all applications. Explore the full list and refine your search

Investigative ophthalmology & visual science 63:7 PubMed35930269

2022

Branched Chain Amino Acids Promote ATP Production Via Translocation of Glucose Transporters.

Applications

Unspecified application

Species

Unspecified reactive species

Sachiko Iwai,Tomoko Hasegawa,Hanako Ohashi Ikeda,Akitaka Tsujikawa
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