Welcome to Hodoodo Chemicals

1-Azakenpaullone
featured

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

Hodoodo CAT#: H555366

CAS#: 676596-65-9

Description: 1-Azakenpaullone is an analog of kenpaullone that inhibits glycogen synthase kinase 3β (GSK3β) more potently (IC50 = 18 nM) than CDK1/cyclin B or CDK5/p25 (IC50s = 2.0 and 4.2 µM, respectively).

Chemical Structure

1-Azakenpaullone

CAS# 676596-65-9

Instruction

Theoretical Analysis

Hodoodo Cat#: H555366
Name: 1-Azakenpaullone
CAS#: 676596-65-9
Chemical Formula: C15H10BrN3O
Exact Mass: 327.00
Molecular Weight: 328.169
Elemental Analysis: C, 54.90; H, 3.07; Br, 24.35; N, 12.80; O, 4.88

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 450	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. Hodoodo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: 1-Azakenpaullone

IUPAC/Chemical Name: 9-bromo-7,12-dihydro-pyrido[3',2':2,3]azepino[4,5-b]indol-6(5H)-one

InChi Key: NTSBZVCEIVPKBJ-UHFFFAOYSA-N

InChi Code: InChI=1S/C15H10BrN3O/c16-8-3-4-11-9(6-8)10-7-13(20)18-12-2-1-5-17-15(12)14(10)19-11/h1-6,19H,7H2,(H,18,20)

SMILES Code: O=C(NC1=CC=CN=C12)CC3=C2NC4=C3C=C(Br)C=C4

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: 2934.99.03.00

More Info:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 328.17 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:

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

Mass

Concentration

Volume

M. Wt* g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Concentration 1

Volume 1

Concentration 2

Volume 2

1: Hazlitt RA, Teitz T, Bonga JD, Fang J, Diao S, Iconaru L, Yang L, Goktug AN, Currier DG, Chen T, Rankovic Z, Min J, Zuo J. Development of Second-Generation CDK2 Inhibitors for the Prevention of Cisplatin-Induced Hearing Loss. J Med Chem. 2018 Sep 13;61(17):7700-7709. doi: 10.1021/acs.jmedchem.8b00669. Epub 2018 Aug 24. PubMed PMID: 30091915.

2: Shi L, Tang X, Qian M, Liu Z, Meng F, Fu L, Wang Z, Zhu WG, Huang JD, Zhou Z, Liu B. A SIRT1-centered circuitry regulates breast cancer stemness and metastasis. Oncogene. 2018 Jul 23. doi: 10.1038/s41388-018-0370-5. [Epub ahead of print] PubMed PMID: 30038266.

3: Choi S, Lee K, Jung H, Park N, Kang J, Nam KH, Kim EK, Ju JH, Kang KY. Kruppel-Like Factor 4 Positively Regulates Autoimmune Arthritis in Mouse Models and Rheumatoid Arthritis in Patients via Modulating Cell Survival and Inflammation Factors of Fibroblast-Like Synoviocyte. Front Immunol. 2018 Jun 27;9:1339. doi: 10.3389/fimmu.2018.01339. eCollection 2018. PubMed PMID: 29997611; PubMed Central PMCID: PMC6030377.

4: Joo HC, Choi JW, Moon H, Lee CY, Yoo KJ, Kim SW, Hwang KC. Protective effects of kenpaullone on cardiomyocytes following H(2)O(2)-induced oxidative stress are attributed to inhibition of connexin 43 degradation by SGSM3. Biochem Biophys Res Commun. 2018 May 5;499(2):368-373. doi: 10.1016/j.bbrc.2018.03.166. Epub 2018 Mar 26. PubMed PMID: 29577900.

5: Deng Y, Huang G, Zou L, Nong T, Yang X, Cui J, Wei Y, Yang S, Shi D. Isolation and characterization of buffalo (bubalus bubalis) amniotic mesenchymal stem cells derived from amnion from the first trimester pregnancy. J Vet Med Sci. 2018 Apr 27;80(4):710-719. doi: 10.1292/jvms.17-0556. Epub 2018 Mar 8. PubMed PMID: 29515060; PubMed Central PMCID: PMC5938205.

6: Teitz T, Fang J, Goktug AN, Bonga JD, Diao S, Hazlitt RA, Iconaru L, Morfouace M, Currier D, Zhou Y, Umans RA, Taylor MR, Cheng C, Min J, Freeman B, Peng J, Roussel MF, Kriwacki R, Guy RK, Chen T, Zuo J. CDK2 inhibitors as candidate therapeutics for cisplatin- and noise-induced hearing loss. J Exp Med. 2018 Apr 2;215(4):1187-1203. doi: 10.1084/jem.20172246. Epub 2018 Mar 7. PubMed PMID: 29514916; PubMed Central PMCID: PMC5881471.

7: Anello L, Cavalieri V, Di Bernardo M. Developmental effects of the protein kinase inhibitor kenpaullone on the sea urchin embryo. Comp Biochem Physiol C Toxicol Pharmacol. 2018 Jan;204:36-44. doi: 10.1016/j.cbpc.2017.11.001. Epub 2017 Nov 10. PubMed PMID: 29128602.

8: Lee HW, Arif E, Altintas MM, Quick K, Maheshwari S, Plezia A, Mahmood A, Reiser J, Nihalani D, Gupta V. High-content screening assay-based discovery of paullones as novel podocyte-protective agents. Am J Physiol Renal Physiol. 2018 Feb 1;314(2):F280-F292. doi: 10.1152/ajprenal.00338.2017. Epub 2017 Oct 18. PubMed PMID: 29046299; PubMed Central PMCID: PMC5866451.

9: Hoe SLL, Tan LP, Abdul Aziz N, Liew K, Teow SY, Abdul Razak FR, Chin YM, Mohamed Shahrehan NA, Chu TL, Mohd Kornain NK, Peh SC, Koay CE, Lo KW, Ahmad M, Ng CC, Khoo AS. CD24, CD44 and EpCAM enrich for tumour-initiating cells in a newly established patient-derived xenograft of nasopharyngeal carcinoma. Sci Rep. 2017 Sep 28;7(1):12372. doi: 10.1038/s41598-017-12045-8. PubMed PMID: 28959019; PubMed Central PMCID: PMC5620042.

10: Buchmann B, Döhner K, Schirdewahn T, Sodeik B, Manns MP, Wedemeyer H, Ciesek S, von Hahn T. A screening assay for the identification of host cell requirements and antiviral targets for hepatitis D virus infection. Antiviral Res. 2017 May;141:116-123. doi: 10.1016/j.antiviral.2017.02.008. Epub 2017 Feb 20. PubMed PMID: 28223128.

11: Li R, Liao G, Yin G, Wang B, Yan M, Lin X, Zhang W, Chen X, Du S, Yuan Y. Ionizing Radiation Blocks Hair Cell Regeneration in Zebrafish Lateral Line Neuromasts by Preventing Wnt Signaling. Mol Neurobiol. 2018 Feb;55(2):1639-1651. doi: 10.1007/s12035-017-0430-9. Epub 2017 Feb 13. PubMed PMID: 28194644.

12: Duran J, Oyarce C, Pavez M, Valladares D, Basualto-Alarcon C, Lagos D, Barrientos G, Troncoso MF, Ibarra C, Estrada M. GSK-3β/NFAT Signaling Is Involved in Testosterone-Induced Cardiac Myocyte Hypertrophy. PLoS One. 2016 Dec 15;11(12):e0168255. doi: 10.1371/journal.pone.0168255. eCollection 2016. PubMed PMID: 27977752; PubMed Central PMCID: PMC5158037.

13: Pfisterer U, Ek F, Lang S, Soneji S, Olsson R, Parmar M. Small molecules increase direct neural conversion of human fibroblasts. Sci Rep. 2016 Dec 5;6:38290. doi: 10.1038/srep38290. PubMed PMID: 27917895; PubMed Central PMCID: PMC5137010.

14: Lee SY, Lee S, Choi E, Ham O, Lee CY, Lee J, Seo HH, Cha MJ, Mun B, Lee Y, Yoon C, Hwang KC. Small molecule-mediated up-regulation of microRNA targeting a key cell death modulator BNIP3 improves cardiac function following ischemic injury. Sci Rep. 2016 Mar 24;6:23472. doi: 10.1038/srep23472. Erratum in: Sci Rep. 2018 May 17;8:46973. PubMed PMID: 27008992; PubMed Central PMCID: PMC4806297.

15: Leclère L, Bause M, Sinigaglia C, Steger J, Rentzsch F. Development of the aboral domain in Nematostella requires β-catenin and the opposing activities of Six3/6 and Frizzled5/8. Development. 2016 May 15;143(10):1766-77. doi: 10.1242/dev.120931. Epub 2016 Mar 17. PubMed PMID: 26989171; PubMed Central PMCID: PMC4874479.

16: Chen Y, Sakamuru S, Huang R, Reese DH, Xia M. Identification of compounds that modulate retinol signaling using a cell-based qHTS assay. Toxicol In Vitro. 2016 Apr;32:287-96. doi: 10.1016/j.tiv.2016.01.011. Epub 2016 Jan 25. PubMed PMID: 26820057; PubMed Central PMCID: PMC4779714.

17: Hamilton PW, Sun Y, Henry JJ. Lens regeneration from the cornea requires suppression of Wnt/β-catenin signaling. Exp Eye Res. 2016 Apr;145:206-215. doi: 10.1016/j.exer.2016.01.003. Epub 2016 Jan 8. PubMed PMID: 26778749; PubMed Central PMCID: PMC4842149.

18: Liu ML, Zang T, Zhang CL. Direct Lineage Reprogramming Reveals Disease-Specific Phenotypes of Motor Neurons from Human ALS Patients. Cell Rep. 2016 Jan 5;14(1):115-128. doi: 10.1016/j.celrep.2015.12.018. Epub 2015 Dec 24. PubMed PMID: 26725112; PubMed Central PMCID: PMC4706770.

19: Duan Q, Reid SP, Clark NR, Wang Z, Fernandez NF, Rouillard AD, Readhead B, Tritsch SR, Hodos R, Hafner M, Niepel M, Sorger PK, Dudley JT, Bavari S, Panchal RG, Ma'ayan A. L1000CDS(2): LINCS L1000 characteristic direction signatures search engine. NPJ Syst Biol Appl. 2016;2. pii: 16015. doi: 10.1038/npjsba.2016.15. Epub 2016 Aug 4. PubMed PMID: 28413689; PubMed Central PMCID: PMC5389891.

20: Akiba Y, Mizuta A, Kakihara Y, Nakata J, Nihara J, Saito I, Egusa H, Saeki M. The inhibitors of cyclin-dependent kinases and GSK-3β enhance osteoclastogenesis. Biochem Biophys Rep. 2015 Dec 30;5:253-258. doi: 10.1016/j.bbrep.2015.12.011. eCollection 2016 Mar. PubMed PMID: 28955831; PubMed Central PMCID: PMC5600418.

Your view history

1-Azakenpaullone featured