Autophagy-IN-2

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Autophagy-IN-2 (Compound 7h) is an autophagic flux inhibitor. Autophagy-IN-2 induces cancer cell apoptosis and can be used for triple-negative breast cancer research.

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Autophagy-IN-2 Chemical Structure

CAS No. : 2755454-90-9

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Description

Autophagy-IN-2 (Compound 7h) is an autophagic flux inhibitor. Autophagy-IN-2 induces cancer cell apoptosis and can be used for triple-negative breast cancer research^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
ASPC1	IC₅₀	26.89 μM Compound: 7h	Antiproliferative activity against human ASPC cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human ASPC cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 35797901]
HCT-116	IC₅₀	35.53 μM Compound: 7h	Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 35797901]
HSC-3	IC₅₀	24.03 μM Compound: 7h	Antiproliferative activity against human HSC-3 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human HSC-3 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 35797901]
LN-229	IC₅₀	61.35 μM Compound: 7h	Antiproliferative activity against human LN-229 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human LN-229 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 35797901]
MDA-MB-231	IC₅₀	8.3 μM Compound: 7h	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 35797901]
MDA-MB-468	IC₅₀	6.03 μM Compound: 7h	Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 35797901]
PANC-1	IC₅₀	19.25 μM Compound: 7h	Antiproliferative activity against human PANC cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human PANC cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 35797901]
PC-3	IC₅₀	17.48 μM Compound: 7h	Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 35797901]
SCC-25	IC₅₀	18.64 μM Compound: 7h	Antiproliferative activity against human SCC-25 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human SCC-25 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 35797901]
SW-620	IC₅₀	25.43 μM Compound: 7h	Antiproliferative activity against human SW-620 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human SW-620 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 35797901]
U-251	IC₅₀	12.92 μM Compound: 7h	Antiproliferative activity against human U-251 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human U-251 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 35797901]
U-87MG ATCC	IC₅₀	15.37 μM Compound: 7h	Antiproliferative activity against human U87 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human U87 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 35797901]

In Vitro

Autophagy-IN-2 (Compound 7h) (0-200 μM, 48 h) shows anti-viability activities against various cancer cells^[1].
Autophagy-IN-2 (0-20 μM, 0-48 h) suppresses autophagic flux and impairs DNA repair through down-regulating chromatin ubiquitination in a p62-dependent manner^[1].
Autophagy-IN-2 (0-20 μM, 48 h) induces cell cycle arrest at S-phase and mitochondria-dependent intrinsic apoptosis^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:	MDA-MB-231, MDA-MB-468, SCC25, HSC-3, HCT116, SW620, PC3, Aspc, PNAC, U87, U251 and LN229
Concentration:	0-200 μM
Incubation Time:	48 h
Result:	Showed anti-viability activities with IC₅₀ values of 8.31 ± 1.05, 6.03 ± 0.82, 18.64 ± 2.92, 24.03 ± 3.75, 35.53 ± 7.52, 25.43 ± 2.42, 17.48 ± 1.27, 26.89 ± 5.23, 19.25 ± 3.96, 15.37 ± 1.78, 12.92 ± 2.38 and 61.35 ± 11.61 μM against MDA-MB-231, MDA-MB-468, SCC25, HSC-3, HCT116, SW620, PC3, Aspc, PNAC, U87, U251 and LN229 cells, respectively.

Western Blot Analysis^[1]

Cell Line:	MDA-MB-231 and MDA-MB-468
Concentration:	5, 10 and 20 μM
Incubation Time:	0, 6, 12, 24, 36 and 48 h
Result:	Significantly induced to LC3B-II in a dose - and time-dependent manner, resulted in a p62 accumulation in TNBC cells, increased γH2AX in a dose and time-dependent manner, activated the phosphorylation of ATM, NBS1 and SMC1, increased p62 in the nucleus and cytoplasm in a dose-dependent manner, and significantly reduced DNA-damage-induced formation of H2A poly-ubiquitin chains. Decreased the cellular levels of Cyclin A, Cyclin B, CDK1 and CDK2, increased P21 and the phosphorylation levels of CHK1 (Serine 345) and CHK2 (Threonine 68), and increased cytochrome c, cleaved caspase-3, cleaved caspase-9 and cleaved PAPR in a dose-dependent manner.

Cell Cycle Analysis^[1]

Cell Line:	MDA-MB-231 and MDA-MB-468
Concentration:	5, 10 and 20 μM
Incubation Time:	48 h
Result:	Induced cell cycle arrest at S-phase.

Apoptosis Analysis^[1]

Cell Line:	MDA-MB-231 and MDA-MB-468
Concentration:	5, 10 and 20 μM
Incubation Time:	48 h
Result:	Dramatically induced cell apoptosis in TNBC cells and obviously increase the proportion of late-phase apoptosis in a dose-dependent manner.

In Vivo

Autophagy-IN-2 (Compound 7h) (5 and 15 mg/kg; i.p.; every 3 days for 3 weeks) suppresses tumor growth in a dose-dependent manner^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Six-week-old female NOD/SCID mice, MDA-MB-231 xenograft^[1]
Dosage:	5 mg/kg, 15 mg/kg
Administration:	Intraperitoneal injection, every 3 days for 3 weeks
Result:	Suppressed human TNBC tumor growth in a dose-dependent manner and resulted in a concentration-dependent upregulation of LC3B-II, p62, γH2AX and PARP.

Molecular Weight

309.37

Formula

C₁₇H₁₉N₅O

CAS No.

2755454-90-9

SMILES

O=C(C1=C(C2=NC3=CC=CC=C3N2)N=CN1)NC4CCCCC4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Yang DL, et al. Discovery of fused benzimidazole-imidazole autophagic flux inhibitors for treatment of triple-negative breast cancer. Eur J Med Chem. 2022 Jun 26;240:114565. [Content Brief]

Autophagy-IN-2 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Autophagy-IN-22755454-90-9AutophagyApoptosistriple-negative breast cancerTNBCMDA-MB-231MDA-MB468Inhibitorinhibitorinhibit

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