WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H414529
CAS#: 803712-67-6 (free base)
Description: Obatoclax, also known as GX 015-070, a synthetic small-molecule inhibitor of the bcl-2 family of proteins with potential pro-apoptotic and antineoplastic activities. Obatoclax binds to members of the Bcl-2 protein family, preventing the binding of these anti-apoptotic proteins to the pro-apoptotic proteins Bax and Bak and so promoting the activation of the apoptotic pathway in Bcl-2-overexpressing cells. The Bcl-2 family of proteins (bcl-2, bcl-xl, bcl-w, and Mcl-1) are overexpressed in a wide variety of cancers, including those of the lymphatic system, breast, lung, prostate, and colon.
Hodoodo Cat#: H414529
Name: Obatoclax free base
CAS#: 803712-67-6 (free base)
Chemical Formula: C20H19N3O
Exact Mass: 317.15
Molecular Weight: 317.390
Elemental Analysis: C, 75.69; H, 6.03; N, 13.24; O, 5.04
Related CAS #: 803712-67-6 (free base); 803712-79-0 (mesylate)
Synonym: Obatoclax Free Base; GX05-070; GX-05-070; GX 05-070; GX15-070; GX 15-070; GX-15-070
IUPAC/Chemical Name: 1H-indole, 2-(2-((3,5-dimethyl-1H-pyrrol-2-yl)methylene)-3-methoxy-2H-pyrrol-5-yl)-
InChi Key: RFTSSZJZXOSICM-GRSHGNNSSA-N
InChi Code: InChI=1S/C20H19N3O/c1-12-8-13(2)21-16(12)10-19-20(24-3)11-18(23-19)17-9-14-6-4-5-7-15(14)22-17/h4-11,21-22H,1-3H3/b19-10-
SMILES Code: COC1=CC(C(N2)=CC3=C2C=CC=C3)=N/C1=C\C4=C(C)C=C(C)N4
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: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
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: |
The following data is based on the product molecular weight 317.39 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: |
1: Zhou C, Li T, Xia M, Wu Z, Zhong X, Li A, Rashid HK, Ma C, Zhou R, Duan H, Zhang X, Peng J, Li L. Bcl-2 Antagonist Obatoclax Reactivates Latent HIV-1 via the NF-κB Pathway and Induces Latent Reservoir Cell Apoptosis in Latently Infected Cells. ACS Infect Dis. 2023 Nov 10;9(11):2105-2118. doi: 10.1021/acsinfecdis.3c00218. Epub 2023 Oct 5. PMID: 37796279.
2: Castillo Bautista CM, Eismann K, Gentzel M, Pelucchi S, Mertens J, Walters HE, Yun MH, Sterneckert J. Obatoclax Rescues FUS-ALS Phenotypes in iPSC-Derived Neurons by Inducing Autophagy. Cells. 2023 Sep 11;12(18):2247. doi: 10.3390/cells12182247. PMID: 37759469; PMCID: PMC10527391.
3: Espona-Fiedler M, Manuel-Manresa P, Benítez-García C, Fontova P, Quesada R, Soto-Cerrato V, Pérez-Tomás R. Antimetastatic Properties of Prodigiosin and the BH3-Mimetic Obatoclax (GX15-070) in Melanoma. Pharmaceutics. 2022 Dec 28;15(1):97. doi: 10.3390/pharmaceutics15010097. PMID: 36678726; PMCID: PMC9862601.
4: Wang X, Li Y, Jia F, Cui X, Pan Z, Wu Y. Boosting nutrient starvation- dominated cancer therapy through curcumin-augmented mitochondrial Ca2+ overload and obatoclax-mediated autophagy inhibition as supported by a novel nano-modulator GO-Alg@CaP/CO. J Nanobiotechnology. 2022 May 12;20(1):225. doi: 10.1186/s12951-022-01439-0. PMID: 35551609; PMCID: PMC9097046.
5: Parkhurst A, Wang SZ, Findlay TR, Malebranche KJ, Odabas A, Alt J, Maxwell MJ, Kaur H, Peer CJ, Figg WD, Warren KE, Slusher BS, Eberhart CG, Raabe EH, Rubens JA. Dual mTORC1/2 inhibition compromises cell defenses against exogenous stress potentiating Obatoclax-induced cytotoxicity in atypical teratoid/rhabdoid tumors. Cell Death Dis. 2022 Apr 28;13(4):410. doi: 10.1038/s41419-022-04868-9. PMID: 35484114; PMCID: PMC9050713.
6: Mao B, Le-Trilling VTK, Wang K, Mennerich D, Hu J, Zhao Z, Zheng J, Deng Y, Katschinski B, Xu S, Zhang G, Cai X, Hu Y, Wang J, Lu M, Huang A, Tang N, Trilling M, Lin Y. Obatoclax inhibits SARS-CoV-2 entry by altered endosomal acidification and impaired cathepsin and furin activity in vitro. Emerg Microbes Infect. 2022 Dec;11(1):483-497. doi: 10.1080/22221751.2022.2026739. PMID: 34989664; PMCID: PMC8843317.
7: Li J, Xu J, Li Z. Obatoclax, the pan-Bcl-2 inhibitor sensitizes hepatocellular carcinoma cells to promote the anti-tumor efficacy in combination with immune checkpoint blockade. Transl Oncol. 2021 Aug;14(8):101116. doi: 10.1016/j.tranon.2021.101116. Epub 2021 May 8. PMID: 33975180; PMCID: PMC8131730.
8: Lima K, Vicari HP, Carlos JAEG, da Silva JCL, Figueiredo-Pontes LL, Rego EM, Machado-Neto JA. Obatoclax reduces cell viability of acute myeloid leukemia cell lines independently of their sensitivity to venetoclax. Hematol Transfus Cell Ther. 2022 Jan-Mar;44(1):124-127. doi: 10.1016/j.htct.2021.01.004. Epub 2021 Mar 13. PMID: 33753045; PMCID: PMC8885367.
9: Varghese FS, van Woudenbergh E, Overheul GJ, Eleveld MJ, Kurver L, van Heerbeek N, van Laarhoven A, Miesen P, den Hartog G, de Jonge MI, van Rij RP. Berberine and Obatoclax Inhibit SARS-Cov-2 Replication in Primary Human Nasal Epithelial Cells In Vitro. Viruses. 2021 Feb 11;13(2):282. doi: 10.3390/v13020282. PMID: 33670363; PMCID: PMC7918080.
10: Yin YP, Shi WH, Deng K, Liu XL, Li H, Lv XT, Lui VWY, Ding C, Hong B, Lin WC. Combinations of proteasome inhibitors with obatoclax are effective for small cell lung cancer. Acta Pharmacol Sin. 2021 Aug;42(8):1298-1310. doi: 10.1038/s41401-020-00544-w. Epub 2020 Nov 2. PMID: 33139838; PMCID: PMC8285499.
11: Song HY, Zhang YM, Lian H, Zhou L. [Effects of obatoclax combined with gemcitabine on breast cancer cells under hypoxia condition]. Zhongguo Ying Yong Sheng Li Xue Za Zhi. 2020 May;36(3):268-272. Chinese. doi: 10.12047/j.cjap.5955.2020.059. PMID: 32981284.
12: Chen S, Ren Y, Duan P. Biomimetic nanoparticle loading obatoclax mesylate for the treatment of non-small-cell lung cancer (NSCLC) through suppressing Bcl-2 signaling. Biomed Pharmacother. 2020 Sep;129:110371. doi: 10.1016/j.biopha.2020.110371. Epub 2020 Jun 18. PMID: 32563984.
13: Opydo-Chanek M, Cichoń I, Rak A, Kołaczkowska E, Mazur L. The pan-Bcl-2 inhibitor obatoclax promotes differentiation and apoptosis of acute myeloid leukemia cells. Invest New Drugs. 2020 Dec;38(6):1664-1676. doi: 10.1007/s10637-020-00931-4. Epub 2020 May 4. PMID: 32367199; PMCID: PMC7575496.
14: Ehrenkaufer G, Li P, Stebbins EE, Kangussu-Marcolino MM, Debnath A, White CV, Moser MS, DeRisi J, Gisselberg J, Yeh E, Wang SC, Company AH, Monti L, Caffrey CR, Huston CD, Wang B, Singh U. Identification of anisomycin, prodigiosin and obatoclax as compounds with broad-spectrum anti-parasitic activity. PLoS Negl Trop Dis. 2020 Mar 20;14(3):e0008150. doi: 10.1371/journal.pntd.0008150. PMID: 32196500; PMCID: PMC7112225.
15: Or CR, Huang CW, Chang CC, Lai YC, Chen YJ, Chang CC. Obatoclax, a Pan-BCL-2 Inhibitor, Downregulates Survivin to Induce Apoptosis in Human Colorectal Carcinoma Cells Via Suppressing WNT/β-catenin Signaling. Int J Mol Sci. 2020 Mar 5;21(5):1773. doi: 10.3390/ijms21051773. PMID: 32150830; PMCID: PMC7084590.
16: Cournoyer S, Addioui A, Belounis A, Beaunoyer M, Nyalendo C, Le Gall R, Teira P, Haddad E, Vassal G, Sartelet H. GX15-070 (Obatoclax), a Bcl-2 family proteins inhibitor engenders apoptosis and pro-survival autophagy and increases Chemosensitivity in neuroblastoma. BMC Cancer. 2019 Oct 29;19(1):1018. doi: 10.1186/s12885-019-6195-y. PMID: 31664947; PMCID: PMC6819521.
17: Andersen PI, Krpina K, Ianevski A, Shtaida N, Jo E, Yang J, Koit S, Tenson T, Hukkanen V, Anthonsen MW, Bjoras M, Evander M, Windisch MP, Zusinaite E, Kainov DE. Novel Antiviral Activities of Obatoclax, Emetine, Niclosamide, Brequinar, and Homoharringtonine. Viruses. 2019 Oct 18;11(10):964. doi: 10.3390/v11100964. PMID: 31635418; PMCID: PMC6832696.
18: Dasmahapatra G, Lembersky D, Son MP, Patel H, Peterson D, Attkisson E, Fisher RI, Friedberg JW, Dent P, Grant S. Retraction: Obatoclax Interacts Synergistically with the Irreversible Proteasome Inhibitor Carfilzomib in GC- and ABC-DLBCL Cells In Vitro and In Vivo. Mol Cancer Ther. 2019 Jun;18(6):1180. doi: 10.1158/1535-7163.MCT-19-0470. PMID: 31160510; PMCID: PMC6613568.
19: Zhou D, Dai L, Liu X, Que F, Xu Y, Luo X, Zhu Y, Liu S, Li Y, Yu L. [Bortezomib and obatoclax for dual blockade of protein degradation pathways show synergistic anti-tumor effect in human acute T lymphoblastic leukemia cells]. Nan Fang Yi Ke Da Xue Xue Bao. 2019 Apr 30;39(4):401-408. Chinese. doi: 10.12122/j.issn.1673-4254.2019.04.04. PMID: 31068282; PMCID: PMC6743991.
20: Steele TM, Talbott GC, Sam A, Tepper CG, Ghosh PM, Vinall RL. Obatoclax, a BH3 Mimetic, Enhances Cisplatin-Induced Apoptosis and Decreases the Clonogenicity of Muscle Invasive Bladder Cancer Cells via Mechanisms That Involve the Inhibition of Pro-Survival Molecules as Well as Cell Cycle Regulators. Int J Mol Sci. 2019 Mar 14;20(6):1285. doi: 10.3390/ijms20061285. PMID: 30875757; PMCID: PMC6470498.
