MedKoo Cat#: 407963 | Name: KRH102053

Description:

WARNING: This product is for research use only, not for human or veterinary use.

KRH102053 is a HIF-1alpha inhibitor. KRH102053 decreased the protein level of HIF-1alpha and the mRNA levels of HIF-regulated downstream target genes, such as vascular endothelial growth factor, aldolase A, enolase 1 and monocarboxylate transporter 4. Consistent with these results, KRH102053 also inhibited the rates of HIF-related migration and invasion of HOS cells as well as the degree of tube formation in human umbilical vein endothelium cells.

Chemical Structure

KRH102053
KRH102053
CAS#1353254-53-1

Theoretical Analysis

MedKoo Cat#: 407963

Name: KRH102053

CAS#: 1353254-53-1

Chemical Formula: C25H34N2O5S

Exact Mass: 474.2188

Molecular Weight: 474.62

Elemental Analysis: C, 63.27; H, 7.22; N, 5.90; O, 16.85; S, 6.75

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
KRH10205; KRH 102053; KRH-102053;
IUPAC/Chemical Name
4-methoxy-6-((4-methoxybenzyl)amino)-2,2-dimethylchroman-3-yl methioninate
InChi Key
YRALDHSTDKVSML-UHFFFAOYSA-N
InChi Code
InChI=1S/C25H34N2O5S/c1-25(2)23(31-24(28)20(26)12-13-33-5)22(30-4)19-14-17(8-11-21(19)32-25)27-15-16-6-9-18(29-3)10-7-16/h6-11,14,20,22-23,27H,12-13,15,26H2,1-5H3
SMILES Code
O=C(OC1C(C)(C)OC2=C(C=C(NCC3=CC=C(OC)C=C3)C=C2)C1OC)C(N)CCSC
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Hypoxia-inducible factor (HIF) is a transcription factor induced by hypoxia and degraded by ubiquitin-dependent proteasomes in normoxic conditions. Under hypoxic conditions, hydroxylation of HIF-1alpha subunit by prolyl hydroxylase (PHD) is suppressed, thus leading to increased levels of HIF. Although PHD2 plays a key role in regulating the levels of HIF, chemical activators of PHD2 are relatively unknown.

Preparing Stock Solutions

The following data is based on the product molecular weight 474.62 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Nepal M, Gong YD, Park YR, Soh Y. An activator of PHD2, KRH102140, decreases angiogenesis via inhibition of HIF-1α. Cell Biochem Funct. 2011 Mar;29(2):126-34. doi: 10.1002/cbf.1732. Epub 2011 Feb 1. PubMed PMID: 21287578. 2: Choi HJ, Song BJ, Gong YD, Gwak WJ, Soh Y. Rapid degradation of hypoxia-inducible factor-1alpha by KRH102053, a new activator of prolyl hydroxylase 2. Br J Pharmacol. 2008 May;154(1):114-25. doi: 10.1038/bjp.2008.70. Epub 2008 Mar 10. PubMed PMID: 18332861; PubMed Central PMCID: PMC2438970.