Apoptozole | Apoptosis Activator VII | CAS#1054543-47-3

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

MedKoo CAT#: 329451

CAS#: 1054543-47-3

Description: 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

CAS# 1054543-47-3

Instruction

Theoretical Analysis

MedKoo Cat#: 329451
Name: Apoptozole
CAS#: 1054543-47-3
Chemical Formula: C33H25F6N3O3
Exact Mass: 625.18
Molecular Weight: 625.571
Elemental Analysis: C, 63.36; H, 4.03; F, 18.22; N, 6.72; O, 7.67

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 150
25mg	USD 250
50mg	USD 450
100mg	USD 750
200mg	USD 1150
500mg	USD 1950
1g	USD 2650
2g	USD 3850
5g	USD 5450
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. MedKoo 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: 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:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	Soluble in DMSO	0.0	100.00

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.

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: 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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