WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407209
CAS#: 1610536-69-0 (HCl)
Description: MELK-T1 is a potent and selective inhibitor of protein kinase MELK. MELK-T1 decreases DNA-damage tolerance in proliferating cancer cells. MELK-T1 triggered a rapid and proteasome-dependent degradation of the MELK protein. Treatment of MCF-7 breast adenocarcinoma cells with MELK-T1 induced the accumulation of stalled replication forks and double-strand breaks that culminated in a replicative senescence phenotype. MELK-T1 induced a strong phosphorylation of p53, a prolonged upregulation of p21 and a downregulation of FOXM1 target genes.
MedKoo Cat#: 407209
Name: MELK-T1 HCl
CAS#: 1610536-69-0 (HCl)
Chemical Formula: C21H23ClN4O2
Exact Mass:
Molecular Weight: 398.89
Elemental Analysis: C, 63.23; H, 5.81; Cl, 8.89; N, 14.05; O, 8.02
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Related CAS #: 1610536-69-0 (HCl) 1610586-62-3 (free base)
Synonym: MELK-T1; MELK-T 1; MELK-T-1; MELK-T1 HCl salt.
IUPAC/Chemical Name: 2-methoxy-4-(1H-pyrazol-4-yl)-N-(2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yl)benzamide hydrochloride
InChi Key: OXRWZUUCCUDKJJ-UHFFFAOYSA-N
InChi Code: InChI=1S/C21H22N4O2.ClH/c1-27-20-11-15(17-12-23-24-13-17)3-5-19(20)21(26)25-18-4-2-14-6-8-22-9-7-16(14)10-18;/h2-5,10-13,22H,6-9H2,1H3,(H,23,24)(H,25,26);1H
SMILES Code: O=C(NC1=CC=C2CCNCCC2=C1)C3=CC=C(C4=CNN=C4)C=C3OC.[H]Cl
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, not in water
Shelf Life: >2 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
The following data is based on the product molecular weight 398.89 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.
| 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: Beke L, Kig C, Linders JT, Boens S, Boeckx A, Van Heerde E, Parade M, De Bondt A, Van Den Wyngaert I, Bashir T, Ogata S, Meerpoel L, Van Eynde A, Johnson CN, Beullens M, Brehmer D, Bollen M. MELK-T1, a small-molecule inhibitor of protein kinase MELK, decreases DNA-damage tolerance in proliferating cancer cells. Biosci Rep. 2015 Oct 2. pii: BSR20150194. [Epub ahead of print] PubMed PMID: 26431963.
Related CAS#
1610536-69-0 (HCl salt); 1610586-62-3 (free base)
Maternal Embryonic Leucine Zipper Kinase (MELK), a Ser/Thr protein kinase, has oncogenic properties and is overexpressed in many cancer cells. The oncogenic function of MELK is attributed to its capacity to disable critical cell-cycle checkpoints and reduce replication stress. MELK is a key stimulator of proliferation by its ability to increase the threshold for DNA-damage tolerance.
