Cortistatin A

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

Hodoodo CAT#: H562116

CAS#: 882976-95-6

Description: Cortistatin A is a potent and selective inhibitor of mediator-associated kinase CDK8 and its paralogue CDK19.


Chemical Structure

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Cortistatin A
CAS# 882976-95-6

Theoretical Analysis

Hodoodo Cat#: H562116
Name: Cortistatin A
CAS#: 882976-95-6
Chemical Formula: C30H36N2O3
Exact Mass: 472.27
Molecular Weight: 472.620
Elemental Analysis: C, 76.24; H, 7.68; N, 5.93; O, 10.16

Price and Availability

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.

Request quote for custom synthesis

Synonym: Cortistatin A; Cortistatin-A;

IUPAC/Chemical Name: (1R,2R,3S,5R)-3-(Dimethylamino)-17beta-(isoquinolin-7-yl)-5,8alpha-epoxy-9,19-cyclo-9,10-secoandrosta-9(11),10-diene-1,2-diol

InChi Key: KSGZCKSNTAJOJS-DZBMUNJRSA-N

InChi Code: InChI=1S/C30H36N2O3/c1-28-10-8-21-15-23-26(33)27(34)24(32(2)3)16-29(23)11-12-30(21,35-29)25(28)7-6-22(28)19-5-4-18-9-13-31-17-20(18)14-19/h4-5,8-9,13-15,17,22,24-27,33-34H,6-7,10-12,16H2,1-3H3/t22-,24+,25-,26-,27-,28-,29-,30-/m1/s1

SMILES Code: C[C@@]12[C@@H](C3=CC4=C(C=C3)C=CN=C4)CC[C@@]1([H])[C@@]56CC[C@@]7(O6)C[C@H](N(C)C)[C@@H](O)[C@H](O)C7=CC5=CC2

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: >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

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 472.62 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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Nitulescu II, Meyer SC, Wen QJ, Crispino JD, Lemieux ME, Levine RL, Pelish HE, Shair MD. Mediator Kinase Phosphorylation of STAT1 S727 Promotes Growth of Neoplasms With JAK-STAT Activation. EBioMedicine. 2017 Dec;26:112-125. doi: 10.1016/j.ebiom.2017.11.013. Epub 2017 Nov 21. PubMed PMID: 29239838.

2: Kessing CF, Nixon CC, Li C, Tsai P, Takata H, Mousseau G, Ho PT, Honeycutt JB, Fallahi M, Trautmann L, Garcia JV, Valente ST. In Vivo Suppression of HIV Rebound by Didehydro-Cortistatin A, a "Block-and-Lock" Strategy for HIV-1 Treatment. Cell Rep. 2017 Oct 17;21(3):600-611. doi: 10.1016/j.celrep.2017.09.080. PubMed PMID: 29045830; PubMed Central PMCID: PMC5653276.

3: Audetat KA, Galbraith MD, Odell AT, Lee T, Pandey A, Espinosa JM, Dowell RD, Taatjes DJ. A Kinase-Independent Role for Cyclin-Dependent Kinase 19 in p53 Response. Mol Cell Biol. 2017 Jun 15;37(13). pii: e00626-16. doi: 10.1128/MCB.00626-16. Print 2017 Jul 1. PubMed PMID: 28416637; PubMed Central PMCID: PMC5472832.

4: Ibáñez-Costa A, Luque RM, Castaño JP. Cortistatin: A new link between the growth hormone/prolactin axis, stress, and metabolism. Growth Horm IGF Res. 2017 Apr;33:23-27. doi: 10.1016/j.ghir.2017.01.004. Epub 2017 Jan 22. Review. PubMed PMID: 28157571.

5: Poss ZC, Ebmeier CC, Odell AT, Tangpeerachaikul A, Lee T, Pelish HE, Shair MD, Dowell RD, Old WM, Taatjes DJ. Identification of Mediator Kinase Substrates in Human Cells using Cortistatin A and Quantitative Phosphoproteomics. Cell Rep. 2016 Apr 12;15(2):436-50. doi: 10.1016/j.celrep.2016.03.030. Epub 2016 Mar 31. PubMed PMID: 27050516; PubMed Central PMCID: PMC4833653.

6: Boyer TG. Transcriptional kinases: Less is more (or less). Nat Chem Biol. 2016 Jan;12(1):4-5. doi: 10.1038/nchembio.1985. PubMed PMID: 26678610.

7: Mousseau G, Valente ST. Didehydro-Cortistatin A: a new player in HIV-therapy? Expert Rev Anti Infect Ther. 2016;14(2):145-8. doi: 10.1586/14787210.2016.1122525. Epub 2015 Dec 11. PubMed PMID: 26581953; PubMed Central PMCID: PMC4793404.

8: Tweaking Transcription to Stop AML Cell Growth. Cancer Discov. 2015 Dec;5(12):OF1. doi: 10.1158/2159-8290.CD-NB2015-149. Epub 2015 Oct 30. PubMed PMID: 26519460.

9: Pelish HE, Liau BB, Nitulescu II, Tangpeerachaikul A, Poss ZC, Da Silva DH, Caruso BT, Arefolov A, Fadeyi O, Christie AL, Du K, Banka D, Schneider EV, Jestel A, Zou G, Si C, Ebmeier CC, Bronson RT, Krivtsov AV, Myers AG, Kohl NE, Kung AL, Armstrong SA, Lemieux ME, Taatjes DJ, Shair MD. Mediator kinase inhibition further activates super-enhancer-associated genes in AML. Nature. 2015 Oct 8;526(7572):273-276. doi: 10.1038/nature14904. Epub 2015 Sep 28. PubMed PMID: 26416749; PubMed Central PMCID: PMC4641525.

10: Kuang L, Liu LL, Chiu P. Formal total synthesis of (+)-cortistatins A and J. Chemistry. 2015 Oct 5;21(41):14287-91. doi: 10.1002/chem.201502890. Epub 2015 Aug 27. PubMed PMID: 26310712.

11: Mousseau G, Kessing CF, Fromentin R, Trautmann L, Chomont N, Valente ST. The Tat Inhibitor Didehydro-Cortistatin A Prevents HIV-1 Reactivation from Latency. MBio. 2015 Jul 7;6(4):e00465. doi: 10.1128/mBio.00465-15. PubMed PMID: 26152583; PubMed Central PMCID: PMC4495168.

12: Mediouni S, Jablonski J, Paris JJ, Clementz MA, Thenin-Houssier S, McLaughlin JP, Valente ST. Didehydro-cortistatin A inhibits HIV-1 Tat mediated neuroinflammation and prevents potentiation of cocaine reward in Tat transgenic mice. Curr HIV Res. 2015;13(1):64-79. PubMed PMID: 25613133; PubMed Central PMCID: PMC4416414.

13: Kotoku N, Mizushima K, Tamura S, Kobayashi M. Synthetic studies of cortistatin A analogue from the CD-ring fragment of vitamin D₂. Chem Pharm Bull (Tokyo). 2013;61(10):1024-9. PubMed PMID: 24088693.

14: Kotoku N. Creation of readily accessible analogue of cortistatin A as an antitumor drug lead. Yakugaku Zasshi. 2013;133(8):867-72. Review. Japanese. PubMed PMID: 23903226.

15: Wang Z, Dai M, Park PK, Danishefsky SJ. Synthetic studies toward (+)-cortistatin A. Tetrahedron. 2011 Dec 30;67(52):10249-10260. Epub 2011 Oct 29. PubMed PMID: 22879684; PubMed Central PMCID: PMC3413295.

16: Kotoku N, Sumii Y, Hayashi T, Tamura S, Kawachi T, Shiomura S, Arai M, Kobayashi M. Creation of readily accessible and orally active analogue of cortistatin a. ACS Med Chem Lett. 2012 Jul 10;3(8):673-7. doi: 10.1021/ml300143d. eCollection 2012 Aug 9. PubMed PMID: 24900528; PubMed Central PMCID: PMC4025756.

17: Mousseau G, Clementz MA, Bakeman WN, Nagarsheth N, Cameron M, Shi J, Baran P, Fromentin R, Chomont N, Valente ST. An analog of the natural steroidal alkaloid cortistatin A potently suppresses Tat-dependent HIV transcription. Cell Host Microbe. 2012 Jul 19;12(1):97-108. doi: 10.1016/j.chom.2012.05.016. PubMed PMID: 22817991; PubMed Central PMCID: PMC3403716.

18: Kotoku N, Sumii Y, Kobayashi M. Stereoselective synthesis of core structure of cortistatin A. Org Lett. 2011 Jul 1;13(13):3514-7. doi: 10.1021/ol201327u. Epub 2011 Jun 9. PubMed PMID: 21651309.

19: Shi J, Manolikakes G, Yeh CH, Guerrero CA, Shenvi RA, Shigehisa H, Baran PS. Scalable synthesis of cortistatin A and related structures. J Am Chem Soc. 2011 May 25;133(20):8014-27. doi: 10.1021/ja202103e. Epub 2011 May 3. PubMed PMID: 21539314; PubMed Central PMCID: PMC3119343.

20: Yamashita S, Iso K, Kitajima K, Himuro M, Hirama M. Total synthesis of cortistatins A and J. J Org Chem. 2011 Apr 15;76(8):2408-25. doi: 10.1021/jo2002616. Epub 2011 Mar 15. PubMed PMID: 21405132.