WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406532
CAS#: 521937-07-5
Description: CID-755673 is a selective protein kinase D (PKD) inhibitor. CID-755673 was identified from the National Institutes of Health small molecule repository library of 196,173 compounds. In cell-based assays, CID755673 blocked phorbol ester-induced endogenous PKD1 activation in LNCaP cells in a concentration-dependent manner. CID755673 inhibited prostate cancer cell proliferation, cell migration, and invasion. In summary, our findings indicate that CID755673 is a potent and selective PKD1 inhibitor with valuable pharmacological and cell biological potential.
MedKoo Cat#: 406532
Name: CID-755673
CAS#: 521937-07-5
Chemical Formula: C12H11NO3
Exact Mass: 217.07389
Molecular Weight: 217.22
Elemental Analysis: C, 66.35; H, 5.10; N, 6.45; O, 22.10
Synonym: CID755673; CID 755673; CID-755673.
IUPAC/Chemical Name: 7-hydroxy-2,3,4,5-tetrahydro-1H-benzofuro[2,3-c]azepin-1-one
InChi Key: AACFPJSJOWQNBN-UHFFFAOYSA-N
InChi Code: InChI=1S/C12H11NO3/c14-7-3-4-10-9(6-7)8-2-1-5-13-12(15)11(8)16-10/h3-4,6,14H,1-2,5H2,(H,13,15)
SMILES Code: O=C1NCCCC2=C1OC3=CC=C(O)C=C32
Appearance: brown 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 217.22 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: Talman V, Gateva G, Ahti M, Ekokoski E, Lappalainen P, Tuominen RK. Evidence for a role of MRCK in mediating HeLa cell elongation induced by the C1 domain ligand HMI-1a3. Eur J Pharm Sci. 2014 May 13;55:46-57. doi: 10.1016/j.ejps.2014.01.002. Epub 2014 Jan 29. PubMed PMID: 24486483.
2: Scheiter M, Bulitta B, van Ham M, Klawonn F, König S, Jänsch L. Protein Kinase Inhibitors CK59 and CID755673 Alter Primary Human NK Cell Effector Functions. Front Immunol. 2013 Mar 18;4:66. doi: 10.3389/fimmu.2013.00066. eCollection 2013. PubMed PMID: 23508354; PubMed Central PMCID: PMC3600540.
3: Mansky KC, Jensen ED, Davidova J, Yamamoto M, Gopalakrishnan R. Protein kinase D promotes in vitro osteoclast differentiation and fusion. J Biol Chem. 2013 Apr 5;288(14):9826-34. doi: 10.1074/jbc.M112.444133. Epub 2013 Feb 21. PubMed PMID: 23430742; PubMed Central PMCID: PMC3617283.
4: Uesugi A, Kataoka A, Tozaki-Saitoh H, Koga Y, Tsuda M, Robaye B, Boeynaems JM, Inoue K. Involvement of protein kinase D in uridine diphosphate-induced microglial macropinocytosis and phagocytosis. Glia. 2012 Jul;60(7):1094-105. doi: 10.1002/glia.22337. Epub 2012 Apr 4. PubMed PMID: 22488958.
5: Yuan J, Liu Y, Tan T, Guha S, Gukovsky I, Gukovskaya A, Pandol SJ. Protein kinase d regulates cell death pathways in experimental pancreatitis. Front Physiol. 2012 Mar 27;3:60. doi: 10.3389/fphys.2012.00060. eCollection 2012. PubMed PMID: 22470346; PubMed Central PMCID: PMC3313474.
6: George KM, Frantz MC, Bravo-Altamirano K, Lavalle CR, Tandon M, Leimgruber S, Sharlow ER, Lazo JS, Wang QJ, Wipf P. Design, Synthesis, and Biological Evaluation of PKD Inhibitors. Pharmaceutics. 2011;3(2):186-228. doi: 10.3390/pharmaceutics3020186. PubMed PMID: 22267986; PubMed Central PMCID: PMC3261798.
7: Bravo-Altamirano K, George KM, Frantz MC, Lavalle CR, Tandon M, Leimgruber S, Sharlow ER, Lazo JS, Wang QJ, Wipf P. Synthesis and Structure-Activity Relationships of Benzothienothiazepinone Inhibitors of Protein Kinase D. ACS Med Chem Lett. 2011 Feb 14;2(2):154-159. PubMed PMID: 21617763; PubMed Central PMCID: PMC3100199.
8: Pilankatta R, Lewis D, Inesi G. Involvement of protein kinase D in expression and trafficking of ATP7B (copper ATPase). J Biol Chem. 2011 Mar 4;286(9):7389-96. doi: 10.1074/jbc.M110.171454. Epub 2010 Dec 27. PubMed PMID: 21189263; PubMed Central PMCID: PMC3044995.
9: Lavalle CR, Bravo-Altamirano K, Giridhar KV, Chen J, Sharlow E, Lazo JS, Wipf P, Wang QJ. Novel protein kinase D inhibitors cause potent arrest in prostate cancer cell growth and motility. BMC Chem Biol. 2010 May 5;10:5. doi: 10.1186/1472-6769-10-5. PubMed PMID: 20444281; PubMed Central PMCID: PMC2873968.
10: Torres-Marquez E, Sinnett-Smith J, Guha S, Kui R, Waldron RT, Rey O, Rozengurt E. CID755673 enhances mitogenic signaling by phorbol esters, bombesin and EGF through a protein kinase D-independent pathway. Biochem Biophys Res Commun. 2010 Jan 1;391(1):63-8. doi: 10.1016/j.bbrc.2009.11.002. Epub 2009 Nov 5. PubMed PMID: 19896460; PubMed Central PMCID: PMC2812606.
