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MedKoo Cat#: 329451 | Name: Apoptozole
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Description:

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

Apoptozole, also known as Apoptosis Activator VII, is a selective inhibitor of heat shock protein 70 (Hsp70; 65% inhibition at 200 µM) that acts by blocking its ATPase activity. Apoptozole enhances immune responses to administered antigens. Treatment of mice with Apoptozole elicits production of antibodies with a high IgG2c/IgG1 ratio and stimulates the release of Th1 and Th2-type cytokines, suggesting that Apoptozole activates the Th1 and Th2 immune responses. The ATPase activities of Hsp70 and Hsc70 are known to be responsible for regulation of various biological processes.

Chemical Structure

Apoptozole
Apoptozole
CAS#1054543-47-3

Theoretical Analysis

MedKoo Cat#: 329451

Name: Apoptozole

CAS#: 1054543-47-3

Chemical Formula: C33H25F6N3O3

Exact Mass: 625.1800

Molecular Weight: 625.57

Elemental Analysis: C, 63.36; H, 4.03; F, 18.22; N, 6.72; O, 7.67

Price and Availability

Size Price Availability Quantity
25mg USD 250.00 2 Weeks
50mg USD 450.00 2 Weeks
100mg USD 750.00 2 Weeks
200mg USD 1,150.00 2 Weeks
500mg USD 1,950.00 2 Weeks
1g USD 2,650.00 2 Weeks
2g USD 3,850.00 2 Weeks
5g USD 5,450.00 2 Weeks
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Synonym
Apoptozole; Apoptosis Activator VII.
IUPAC/Chemical Name
4-((2-(3,5-bis(trifluoromethyl)phenyl)-4,5-bis(4-methoxyphenyl)-1H-imidazol-1-yl)methyl)benzamide
InChi Key
ZIMMTPFXOMAJTQ-UHFFFAOYSA-N
InChi Code
InChI=1S/C33H25F6N3O3/c1-44-26-11-7-20(8-12-26)28-29(21-9-13-27(45-2)14-10-21)42(18-19-3-5-22(6-4-19)30(40)43)31(41-28)23-15-24(32(34,35)36)17-25(16-23)33(37,38)39/h3-17H,18H2,1-2H3,(H2,40,43)
SMILES Code
COC(C=C1)=CC=C1C2=C(C3=CC=C(OC)C=C3)N(CC4=CC=C(C(N)=O)C=C4)C(C5=CC(C(F)(F)F)=CC(C(F)(F)F)=C5)=N2
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
Solvent mg/mL mM
Solubility
Soluble in DMSO 0.0 100.00
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 625.57 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
1: Liu H, Zhang J, Xu X, Lu S, Yang D, Xie C, Jia M, Zhang W, Jin L, Wang X, Shen X, Li F, Wang W, Bao X, Li S, Zhu M, Wang W, Wang Y, Huang Z, Teng H. SARM1 promotes neuroinflammation and inhibits neural regeneration after spinal cord injury through NF-κB signaling. Theranostics. 2021 Feb 20;11(9):4187-4206. doi: 10.7150/thno.49054. PMID: 33754056; PMCID: PMC7977471. 2: Evans LE, Cheeseman MD, Yahya N, Jones K. Investigating Apoptozole as a Chemical Probe for HSP70 Inhibition. PLoS One. 2015 Oct 12;10(10):e0140006. doi: 10.1371/journal.pone.0140006. PMID: 26458144; PMCID: PMC4601772. 3: Yang J, Xu Y, Yan Y, Li W, Zhao L, Dai Q, Li Y, Li S, Zhong J, Cao R, Zhong W. Small Molecule Inhibitor of ATPase Activity of HSP70 as a Broad-Spectrum Inhibitor against Flavivirus Infections. ACS Infect Dis. 2020 May 8;6(5):832-843. doi: 10.1021/acsinfecdis.9b00376. Epub 2020 Feb 3. PMID: 31967789. 4: Li H, Lee CH, Shin I. A triple-targeting delivery system carrying two anticancer agents. Org Biomol Chem. 2021 Sep 29;19(37):8009-8013. doi: 10.1039/d1ob01089a. PMID: 34236071. 5: Park SH, Park S, Shin I. Synthesis of an Hsp70 inhibitor and its assessment of lysosomal membrane permeabilization. STAR Protoc. 2021 Feb 18;2(1):100349. doi: 10.1016/j.xpro.2021.100349. PMID: 33665629; PMCID: PMC7903460. 6: Luo LL, Li YF, Shan HM, Wang LP, Yuan F, Ma YY, Li WL, He TT, Wang YY, Qu MJ, Liang HB, Zhang ZJ, Yang GY, Tang YH, Wang YT. L-glutamine protects mouse brain from ischemic injury via up-regulating heat shock protein 70. CNS Neurosci Ther. 2019 Sep;25(9):1030-1041. doi: 10.1111/cns.13184. Epub 2019 Jun 20. PMID: 31218845; PMCID: PMC6698979. 7: Gu J, Ye Y, Zheng ZW, Luo W, Gong YJ, Feng QL, Li S, Huang LH. Cytoplasmic Hsp70s promote EcR transport into the nucleus by responding to various stimuli. Insect Biochem Mol Biol. 2023 Jun;157:103964. doi: 10.1016/j.ibmb.2023.103964. Epub 2023 May 23. PMID: 37230333. 8: Tan C, Liu X, Peng W, Wang H, Zhou W, Jiang J, Wei X, Mo L, Chen Y, Chen L. Seizure-induced impairment in neuronal ketogenesis: Role of zinc-α2-glycoprotein in mitochondria. J Cell Mol Med. 2020 Jun;24(12):6833-6845. doi: 10.1111/jcmm.15337. Epub 2020 Apr 27. PMID: 32340079; PMCID: PMC7299723. 9: Liu P, Zhang M, Liu T, Mo R, Wang H, Zhang G, Wu Y. Avenanthramide Improves Colonic Damage Induced by Food Allergies in Mice through Altering Gut Microbiota and Regulating Hsp70-NF-κB Signaling. Nutrients. 2023 Feb 16;15(4):992. doi: 10.3390/nu15040992. PMID: 36839351; PMCID: PMC9962348. 10: Park SH, Ko W, Park SH, Lee HS, Shin I. Evaluation of the Interaction between Bax and Hsp70 in Cells by Using a FRET System Consisting of a Fluorescent Amino Acid and YFP as a FRET Pair. Chembiochem. 2020 Jan 15;21(1-2):59-63. doi: 10.1002/cbic.201900293. Epub 2019 Sep 26. PMID: 31206981. 11: Park SH, Baek KH, Shin I, Shin I. Subcellular Hsp70 Inhibitors Promote Cancer Cell Death via Different Mechanisms. Cell Chem Biol. 2018 Oct 18;25(10):1242-1254.e8. doi: 10.1016/j.chembiol.2018.06.010. Epub 2018 Jul 26. PMID: 30057298. 12: Park SH, Kim WJ, Li H, Seo W, Park SH, Kim H, Shin SC, Zuiderweg ERP, Kim EE, Sim T, Kim NK, Shin I. Anti-leukemia activity of a Hsp70 inhibitor and its hybrid molecules. Sci Rep. 2017 Jun 14;7(1):3537. doi: 10.1038/s41598-017-03814-6. PMID: 28615625; PMCID: PMC5471252. 13: Park SH, Kim S, Lee HS, Shin I. Real-Time Spatial and Temporal Analysis of the Translocation of the Apoptosis-Inducing Factor in Cells. ACS Chem Biol. 2021 Nov 19;16(11):2462-2471. doi: 10.1021/acschembio.1c00565. Epub 2021 Oct 25. PMID: 34694772. 14: Cho HJ, Kim GH, Park SH, Hyun JY, Kim NK, Shin I. Probing the effect of an inhibitor of an ATPase domain of Hsc70 on clathrin-mediated endocytosis. Mol Biosyst. 2015 Oct;11(10):2763-9. doi: 10.1039/c4mb00695j. PMID: 25728281. 15: Ko SK, Kim J, Na DC, Park S, Park SH, Hyun JY, Baek KH, Kim ND, Kim NK, Park YN, Song K, Shin I. A small molecule inhibitor of ATPase activity of HSP70 induces apoptosis and has antitumor activities. Chem Biol. 2015 Mar 19;22(3):391-403. doi: 10.1016/j.chembiol.2015.02.004. Epub 2015 Mar 12. PMID: 25772468. 16: Roundhill E, Turnbull D, Burchill S. Localization of MRP-1 to the outer mitochondrial membrane by the chaperone protein HSP90β. FASEB J. 2016 May;30(5):1712-23. doi: 10.1096/fj.15-283408. Epub 2015 Dec 31. PMID: 26722004. 17: Liu P, Liu T, Zhang M, Mo R, Zhou W, Li D, Wu Y. Effects of Avenanthramide on the Small Intestinal Damage through Hsp70-NF-κB Signaling in an Ovalbumin- Induced Food Allergy Model. Int J Mol Sci. 2022 Dec 3;23(23):15229. doi: 10.3390/ijms232315229. PMID: 36499554; PMCID: PMC9739943. 18: Baek KH, Zhang H, Lee BR, Kwon YG, Ha SJ, Shin I. A small molecule inhibitor for ATPase activity of Hsp70 and Hsc70 enhances the immune response to protein antigens. Sci Rep. 2015 Dec 3;5:17642. doi: 10.1038/srep17642. PMID: 26631605; PMCID: PMC4668564. 19: Chen Y, Murillo-Solano C, Kirkpatrick MG, Antoshchenko T, Park HW, Pizarro JC. Repurposing drugs to target the malaria parasite unfolding protein response. Sci Rep. 2018 Jul 9;8(1):10333. doi: 10.1038/s41598-018-28608-2. PMID: 29985421; PMCID: PMC6037779. 20: Chang PK, Chien KY, Chen JC. Dopamine transporter is downregulated and its association with chaperone protein Hsc70 is enhanced by activation of dopamine D3 receptor. Brain Res Bull. 2020 Dec;165:263-271. doi: 10.1016/j.brainresbull.2020.10.005. Epub 2020 Oct 10. PMID: 33049353.

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