WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H122949
CAS#: 2648855-18-7
Description: RK-701 is a structurally distinct potent inhibitor of G9a/GLP (IC50 = 27/53 nM). RK-701 exhibited remarkable selectivity against other related methyltransferases, dose-dependent attenuation of cellular H3K9me2 levels, and tumor growth inhibition in MOLT-4 cells in vitro. Moreover, RK-701 showed inhibition of tumor initiation and growth in a carcinogen-induced hepatocellular carcinoma (HCC) in vivo mouse model without overt acute toxicity
Hodoodo Cat#: H122949
Name: RK-701
CAS#: 2648855-18-7
Chemical Formula: C26H30N4O3
Exact Mass: 446.23
Molecular Weight: 446.550
Elemental Analysis: C, 69.93; H, 6.77; N, 12.55; O, 10.75
This product is not in stock, which may be available by custom synthesis.
For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge).
Quote less than 1g will not be provided. To request quote, please email to sales @hodoodo.com or click below button.
Note: Price will be listed if it is available in the future.
Synonym: RK-701; RK 701; RK701
IUPAC/Chemical Name: (S)-N-(1-((4-cyanophenyl)amino)-4-cyclopropyl-1-oxobutan-2-yl)-3,6,6-trimethyl-4-oxo-4,5,6,7-tetrahydro-1H-indole-2-carboxamide
InChi Key: OWORSODZTADOQX-IBGZPJMESA-N
InChi Code: InChI=1S/C26H30N4O3/c1-15-22-20(12-26(2,3)13-21(22)31)29-23(15)25(33)30-19(11-8-16-4-5-16)24(32)28-18-9-6-17(14-27)7-10-18/h6-7,9-10,16,19,29H,4-5,8,11-13H2,1-3H3,(H,28,32)(H,30,33)/t19-/m0/s1
SMILES Code: CC1=C(NC(CC(C2)(C)C)=C1C2=O)C(N[C@H](C(NC3=CC=C(C#N)C=C3)=O)CCC4CC4)=O
Appearance: To be determined
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: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
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:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 446.55 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 |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Nishigaya Y, Takase S, Sumiya T, Kikuzato K, Sato T, Niwa H, Sato S, Nakata
A, Sonoda T, Hashimoto N, Namie R, Honma T, Umehara T, Shirouzu M, Koyama H,
Yoshida M, Ito A, Shirai F. Discovery of Novel Substrate-Competitive Lysine
Methyltransferase G9a Inhibitors as Anticancer Agents. J Med Chem. 2023 Mar 7.
doi: 10.1021/acs.jmedchem.2c02059. Epub ahead of print. PMID: 36882960.
2: Takase S, Hiroyama T, Shirai F, Maemoto Y, Nakata A, Arata M, Matsuoka S,
Sonoda T, Niwa H, Sato S, Umehara T, Shirouzu M, Nishigaya Y, Sumiya T,
Hashimoto N, Namie R, Usui M, Ohishi T, Ohba SI, Kawada M, Hayashi Y, Harada H,
Yamaguchi T, Shinkai Y, Nakamura Y, Yoshida M, Ito A. A specific G9a inhibitor
unveils BGLT3 lncRNA as a universal mediator of chemically induced fetal globin
gene expression. Nat Commun. 2023 Jan 12;14(1):23. doi:
10.1038/s41467-022-35404-0. PMID: 36635268; PMCID: PMC9837035.