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MedKoo Cat#: 563380 | Name: MKT-077
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Description:

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

MKT-077 is an inhibitor of mitochondrial hsp70 family member mortalin (mot-2), causing the selective death of cancer cells.

Chemical Structure

MKT-077
MKT-077
CAS#147366-41-4

Theoretical Analysis

MedKoo Cat#: 563380

Name: MKT-077

CAS#: 147366-41-4

Chemical Formula: C21H22ClN3OS2

Exact Mass:

Molecular Weight: 432.00

Elemental Analysis: C, 58.39; H, 5.13; Cl, 8.21; N, 9.73; O, 3.70; S, 14.84

Price and Availability

Size Price Availability Quantity
5mg USD 250.00 2 Weeks
10mg USD 420.00 2 Weeks
25mg USD 750.00 2 Weeks
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Related CAS #
No Data
Synonym
MKT-077; MKT 077; MKT077; FJ-776; FJ 776; FJ776;
IUPAC/Chemical Name
(2Z,5E)-3-ethyl-2-[(1-ethylpyridin-1-ium-2-yl)methylidene]-5-(3-methyl-1,3-benzothiazol-2-ylidene)-1,3-thiazolidin-4-one chloride
InChi Key
VSKYOTRJSLYFHX-UXJRWBAGSA-M
InChi Code
InChI=1S/C21H22N3OS2.ClH/c1-4-23-13-9-8-10-15(23)14-18-24(5-2)20(25)19(27-18)21-22(3)16-11-6-7-12-17(16)26-21;/h6-14H,4-5H2,1-3H3;1H/q+1;/p-1/b21-19+;
SMILES Code
O=C1N(CC)/C(S/C1=C2SC3=CC=CC=C3N/2C)=C/C4=CC=CC=[N+]4CC.[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
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
Product Data
Product Data
Instruction
View handling instruction
Biological target:
MKT-077 is a rhodacyanine dye and also a heat shock protein 70 (Hsp70) inhibitor.
In vitro activity:
MKT-077 binds to an hsp70 family member, mortalin (mot-2), and abrogates its interactions with the tumor suppressor protein, p53. In cancer cells, but not in normal cells, MKT-077 induced release of wild-type p53 from cytoplasmically sequestered p53-mot-2 complexes and rescued its transcriptional activation function. Thus, MKT-077 may be particularly useful for therapy of cancers with wild-type p53. Reference: Cancer Res. 2000 Dec 15;60(24):6818-21. https://pubmed.ncbi.nlm.nih.gov/11156371/
In vivo activity:
This study determined whether MKT-077 could suppress TT xenografts in immune-compromised nude mice. Systemic administration of MKT-077 significantly delayed the growth of TT xenografts in mice throughout the treatment (Fig. 5A). At the end of the drug treatment, this study found that tumor weights were about two-times less in MKT-077-treated group than in control group (Fig. 5B). Reference: Endocrinol Metab (Seoul). 2015 Dec;30(4):593-603. https://pubmed.ncbi.nlm.nih.gov/26485469/
Solvent mg/mL mM comments
Solubility
DMSO 23.3 53.98
Ethanol 6.0 13.89
PBS (pH 7.2) 2.0 4.63
Water 53.8 124.54
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 432.00 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:
1. Wadhwa R, Colgin L, Yaguchi T, Taira K, Reddel RR, Kaul SC. Rhodacyanine dye MKT-077 inhibits in vitro telomerase assay but has no detectable effects on telomerase activity in vivo. Cancer Res. 2002 Aug 1;62(15):4434-8. PMID: 12154051. 2. Wadhwa R, Sugihara T, Yoshida A, Nomura H, Reddel RR, Simpson R, Maruta H, Kaul SC. Selective toxicity of MKT-077 to cancer cells is mediated by its binding to the hsp70 family protein mot-2 and reactivation of p53 function. Cancer Res. 2000 Dec 15;60(24):6818-21. PMID: 11156371. 3. Starenki D, Park JI. Selective Mitochondrial Uptake of MKT-077 Can Suppress Medullary Thyroid Carcinoma Cell Survival In Vitro and In Vivo. Endocrinol Metab (Seoul). 2015 Dec;30(4):593-603. doi: 10.3803/EnM.2015.30.4.593. Epub 2015 Oct 20. PMID: 26485469; PMCID: PMC4722416. 4. Guo W, Yan L, Yang L, Liu X, E Q, Gao P, Ye X, Liu W, Zuo J. Targeting GRP75 improves HSP90 inhibitor efficacy by enhancing p53-mediated apoptosis in hepatocellular carcinoma. PLoS One. 2014 Jan 17;9(1):e85766. doi: 10.1371/journal.pone.0085766. PMID: 24465691; PMCID: PMC3894982.
In vitro protocol:
1. Wadhwa R, Colgin L, Yaguchi T, Taira K, Reddel RR, Kaul SC. Rhodacyanine dye MKT-077 inhibits in vitro telomerase assay but has no detectable effects on telomerase activity in vivo. Cancer Res. 2002 Aug 1;62(15):4434-8. PMID: 12154051. 2. Wadhwa R, Sugihara T, Yoshida A, Nomura H, Reddel RR, Simpson R, Maruta H, Kaul SC. Selective toxicity of MKT-077 to cancer cells is mediated by its binding to the hsp70 family protein mot-2 and reactivation of p53 function. Cancer Res. 2000 Dec 15;60(24):6818-21. PMID: 11156371
In vivo protocol:
1. Starenki D, Park JI. Selective Mitochondrial Uptake of MKT-077 Can Suppress Medullary Thyroid Carcinoma Cell Survival In Vitro and In Vivo. Endocrinol Metab (Seoul). 2015 Dec;30(4):593-603. doi: 10.3803/EnM.2015.30.4.593. Epub 2015 Oct 20. PMID: 26485469; PMCID: PMC4722416. 2. Guo W, Yan L, Yang L, Liu X, E Q, Gao P, Ye X, Liu W, Zuo J. Targeting GRP75 improves HSP90 inhibitor efficacy by enhancing p53-mediated apoptosis in hepatocellular carcinoma. PLoS One. 2014 Jan 17;9(1):e85766. doi: 10.1371/journal.pone.0085766. PMID: 24465691; PMCID: PMC3894982.
1: Abunimer AN, Mohammed H, Cook KL, Soto-Pantoja DR, Campos MM, Abu-Asab MS. Mitochondrial autophagosomes as a mechanism of drug resistance in breast carcinoma. Ultrastruct Pathol. 2018 Mar-Apr;42(2):170-180. doi: 10.1080/01913123.2017.1419328. Epub 2018 Feb 8. PubMed PMID: 29419344. 2: Ben-Hamo O, Rosner A, Rabinowitz C, Oren M, Rinkevich B. Coupling astogenic aging in the colonial tunicate Botryllus schlosseri with the stress protein mortalin. Dev Biol. 2018 Jan 1;433(1):33-46. doi: 10.1016/j.ydbio.2017.10.023. Epub 2017 Nov 8. PubMed PMID: 29128264. 3: Gao Z, Niu X, Zhang Q, Chen H, Gao A, Qi S, Xiang R, Belting M, Zhang S. Mitochondria chaperone GRP75 moonlighting as a cell cycle controller to derail endocytosis provides an opportunity for nanomicrosphere intracellular delivery. Oncotarget. 2017 Apr 19;8(35):58536-58552. doi: 10.18632/oncotarget.17234. eCollection 2017 Aug 29. PubMed PMID: 28938577; PubMed Central PMCID: PMC5601673. 4: Liu T, Krysiak K, Shirai CL, Kim S, Shao J, Ndonwi M, Walter MJ. Knockdown of HSPA9 induces TP53-dependent apoptosis in human hematopoietic progenitor cells. PLoS One. 2017 Feb 8;12(2):e0170470. doi: 10.1371/journal.pone.0170470. eCollection 2017. PubMed PMID: 28178280; PubMed Central PMCID: PMC5298293. 5: Yun CO, Bhargava P, Na Y, Lee JS, Ryu J, Kaul SC, Wadhwa R. Relevance of mortalin to cancer cell stemness and cancer therapy. Sci Rep. 2017 Feb 6;7:42016. doi: 10.1038/srep42016. PubMed PMID: 28165047; PubMed Central PMCID: PMC5292728. 6: Starenki D, Park JI. Selective Mitochondrial Uptake of MKT-077 Can Suppress Medullary Thyroid Carcinoma Cell Survival In Vitro and In Vivo. Endocrinol Metab (Seoul). 2015 Dec;30(4):593-603. doi: 10.3803/EnM.2015.30.4.593. Epub 2015 Oct 20. PubMed PMID: 26485469; PubMed Central PMCID: PMC4722416. 7: Amick J, Schlanger SE, Wachnowsky C, Moseng MA, Emerson CC, Dare M, Luo WI, Ithychanda SS, Nix JC, Cowan JA, Page RC, Misra S. Crystal structure of the nucleotide-binding domain of mortalin, the mitochondrial Hsp70 chaperone. Protein Sci. 2014 Jun;23(6):833-42. doi: 10.1002/pro.2466. Epub 2014 Apr 17. PubMed PMID: 24687350; PubMed Central PMCID: PMC4093958. 8: Guo W, Yan L, Yang L, Liu X, E Q, Gao P, Ye X, Liu W, Zuo J. Targeting GRP75 improves HSP90 inhibitor efficacy by enhancing p53-mediated apoptosis in hepatocellular carcinoma. PLoS One. 2014 Jan 17;9(1):e85766. doi: 10.1371/journal.pone.0085766. eCollection 2014. PubMed PMID: 24465691; PubMed Central PMCID: PMC3894982. 9: Li X, Srinivasan SR, Connarn J, Ahmad A, Young ZT, Kabza AM, Zuiderweg ER, Sun D, Gestwicki JE. Analogs of the Allosteric Heat Shock Protein 70 (Hsp70) Inhibitor, MKT-077, as Anti-Cancer Agents. ACS Med Chem Lett. 2013 Nov 14;4(11). doi: 10.1021/ml400204n. PubMed PMID: 24312699; PubMed Central PMCID: PMC3845967. 10: Tai-Nagara I, Matsuoka S, Ariga H, Suda T. Mortalin and DJ-1 coordinately regulate hematopoietic stem cell function through the control of oxidative stress. Blood. 2014 Jan 2;123(1):41-50. doi: 10.1182/blood-2013-06-508333. Epub 2013 Nov 15. PubMed PMID: 24243970. 11: Budina-Kolomets A, Balaburski GM, Bondar A, Beeharry N, Yen T, Murphy ME. Comparison of the activity of three different HSP70 inhibitors on apoptosis, cell cycle arrest, autophagy inhibition, and HSP90 inhibition. Cancer Biol Ther. 2014 Feb;15(2):194-9. doi: 10.4161/cbt.26720. Epub 2013 Nov 1. PubMed PMID: 24100579; PubMed Central PMCID: PMC3928135. 12: Miyata Y, Li X, Lee HF, Jinwal UK, Srinivasan SR, Seguin SP, Young ZT, Brodsky JL, Dickey CA, Sun D, Gestwicki JE. Synthesis and initial evaluation of YM-08, a blood-brain barrier permeable derivative of the heat shock protein 70 (Hsp70) inhibitor MKT-077, which reduces tau levels. ACS Chem Neurosci. 2013 Jun 19;4(6):930-9. doi: 10.1021/cn300210g. Epub 2013 Mar 20. PubMed PMID: 23472668; PubMed Central PMCID: PMC3689201. 13: Wang AM, Miyata Y, Klinedinst S, Peng HM, Chua JP, Komiyama T, Li X, Morishima Y, Merry DE, Pratt WB, Osawa Y, Collins CA, Gestwicki JE, Lieberman AP. Activation of Hsp70 reduces neurotoxicity by promoting polyglutamine protein degradation. Nat Chem Biol. 2013 Feb;9(2):112-8. doi: 10.1038/nchembio.1140. Epub 2012 Dec 9. PubMed PMID: 23222885; PubMed Central PMCID: PMC3552084. 14: Chunta JL, Vistisen KS, Yazdi Z, Braun RD. Uptake rate of cationic mitochondrial inhibitor MKT-077 determines cellular oxygen consumption change in carcinoma cells. PLoS One. 2012;7(5):e37471. doi: 10.1371/journal.pone.0037471. Epub 2012 May 17. PubMed PMID: 22616013; PubMed Central PMCID: PMC3355126. 15: Koren J 3rd, Miyata Y, Kiray J, O'Leary JC 3rd, Nguyen L, Guo J, Blair LJ, Li X, Jinwal UK, Cheng JQ, Gestwicki JE, Dickey CA. Rhodacyanine derivative selectively targets cancer cells and overcomes tamoxifen resistance. PLoS One. 2012;7(4):e35566. doi: 10.1371/journal.pone.0035566. Epub 2012 Apr 26. Erratum in: PLoS One. 2012;7(7). doi:.1371/annotation/7493e5d2-4c1a-43eb-a83f-16814861ff13. Li, Xiokai [corrected to Li, Xiaokai]. PubMed PMID: 22563386; PubMed Central PMCID: PMC3338522. 16: Grover A, Priyandoko D, Gao R, Shandilya A, Widodo N, Bisaria VS, Kaul SC, Wadhwa R, Sundar D. Withanone binds to mortalin and abrogates mortalin-p53 complex: computational and experimental evidence. Int J Biochem Cell Biol. 2012 Mar;44(3):496-504. doi: 10.1016/j.biocel.2011.11.021. Epub 2011 Dec 2. PubMed PMID: 22155302. 17: Rousaki A, Miyata Y, Jinwal UK, Dickey CA, Gestwicki JE, Zuiderweg ER. Allosteric drugs: the interaction of antitumor compound MKT-077 with human Hsp70 chaperones. J Mol Biol. 2011 Aug 19;411(3):614-32. doi: 10.1016/j.jmb.2011.06.003. Epub 2011 Jun 25. PubMed PMID: 21708173; PubMed Central PMCID: PMC3146629. 18: Chiasserini D, Tozzi A, de Iure A, Tantucci M, Susta F, Orvietani PL, Koya K, Binaglia L, Calabresi P. Mortalin inhibition in experimental Parkinson's disease. Mov Disord. 2011 Aug 1;26(9):1639-47. doi: 10.1002/mds.23647. Epub 2011 May 3. PubMed PMID: 21542017. 19: Pilzer D, Saar M, Koya K, Fishelson Z. Mortalin inhibitors sensitize K562 leukemia cells to complement-dependent cytotoxicity. Int J Cancer. 2010 Mar 15;126(6):1428-35. doi: 10.1002/ijc.24888. PubMed PMID: 19739077. 20: Walker CW, Böttger SA. A naturally occurring cancer with molecular connectivity to human diseases. Cell Cycle. 2008 Aug;7(15):2286-9. Epub 2008 May 29. Review. PubMed PMID: 18677101.

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