2. Autophagy
  3. Autophagy
  4. ELMO2-IN-1

ELMO2-IN-1 is an ELMO2 inhibitor with a human target Kd of 1.0 µM. ELMO2-IN-1 binds to ELMO2, disrupting its function. ELMO2-IN-1 induces autophagy-dependent cell death. ELMO2-IN-1 can be used for the research of non-small cell lung cancer.

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ELMO2-IN-1

ELMO2-IN-1 Chemical Structure

CAS No. : 1216514-48-5

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ELMO2-IN-1 Related Antibodies

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Description

ELMO2-IN-1 is an ELMO2 inhibitor with a human target Kd of 1.0 µM. ELMO2-IN-1 binds to ELMO2, disrupting its function. ELMO2-IN-1 induces autophagy-dependent cell death. ELMO2-IN-1 can be used for the research of non-small cell lung cancer[1].

In Vitro

ELMO2-IN-1 (Compound C52) (200 μM) binds specifically to wild-type ELMO2 with a Kd of 1.05 μM, and the HIS-435 residue is essential for this binding[1].
ELMO2-IN-1 (72 h) selectively suppresses viability of mesenchymal-like NSCLC cell lines including NCI-H1299, A549, NCI-H1703, 95D, and NCI-H1792 in a concentration-dependent manner, has no effect on normal lung cell lines HBE and MRC-5, and its activity depends on ELMO2 binding and ELMO3 expression levels[1].
ELMO2-IN-1 (5-10 μM; 6-24 h) suppresses FAKY397 phosphorylation in a concentration and time-dependent manner, and induces autophagy markers (reduced p62, increased LC3-II/LC3-I ratio) in mesenchymal-like NSCLC cell lines NCI-H1299 and A549[1].
ELMO2-IN-1 induces cell death in mesenchymal-like patient-derived NSCLC organoids with low ELMO3 expression, but not in epithelial-like organoids with high ELMO3 expression[1].
ELMO2-IN-1 (72 h) potently reduces viability of Osimertinib-resistant NSCLC cell lines NCI-H1975-OR (IC50 = 5.88 μM) and HCC827-OR (IC50 = 7.63 μM), and induces autophagy-related changes in these resistant cells[1].

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

ELMO2-IN-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: mesenchymal-like NSCLC cell lines (NCI-H1299, A549)
Concentration: 5 μM; 10 μM
Incubation Time: 6 h; 12 h; 24 h
Result: Suppressed FAK phosphorylation at the Y397 site in a concentration-dependent and time-dependent manner.
Reduced p62 protein expression.
Increased the LC3-II/LC3-I ratio, consistent with induction of autophagy.
In Vivo

ELMO2-IN-1 (Compound C52) (25 mg/kg; i.p.; daily for 30 days) completely inhibits the growth of mesenchymal-like A549 non-small cell lung cancer xenografts in female BALB/c nude mice[1].
ELMO2-IN-1 (25 mg/kg; i.p.; daily for 30 days) does not inhibit the growth of epithelial-like PC-9 non-small cell lung cancer xenografts in female BALB/c nude mice[1].
ELMO2-IN-1 (25 mg/kg; i.p.; daily for 30 days) completely inhibits the growth of Osimertinib (HY-15772)-resistant NCI-H1975-OR non-small cell lung cancer xenografts in female BALB/c nude mice, with no activity against parental NCI-H1975 tumors[1].
ELMO2-IN-1 (25 mg/kg; i.p.; daily for 30 days) does not inhibit the growth of A549 non-small cell lung cancer xenografts expressing ELMO2H435A mutant[1].
ELMO2-IN-1 (2.5-25 mg/kg; i.p.; daily) induces a dose-dependent antitumor response in mesenchymal-like A549 non-small cell lung cancer xenografts in female BALB/c nude mice[1].

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

Animal Model: BALB/c nude (female, 6-8 weeks old, subcutaneous xenograft of mesenchymal-like A549 cells)[1]
Dosage: 25 mg/kg
Administration: i.p.; daily for 30 days
Result: Achieved near-complete suppression of tumor growth.
By day 40, mean tumor volume remained near baseline, while vehicle-treated mice had a mean tumor volume of ~1600 mm3 (P<0.0001).
Animal Model: BALB/c nude (female, 6-8 weeks old, subcutaneous xenograft of epithelial-like PC-9 cells)[1]
Dosage: 25 mg/kg
Administration: i.p.; daily for 30 days
Result: Showed no significant effect on tumor growth.
By day 40, mean tumor volume in treated and vehicle-treated mice was nearly identical (P=0.9973).
Animal Model: BALB/c nude (female, 6-8 weeks old, subcutaneous xenograft of osimertinib-resistant NCI-H1975-OR cells)[1]
Dosage: 25 mg/kg
Administration: i.p.; daily for 30 days
Result: Completely suppressed tumor growth.
By day 40, mean tumor volume remained near baseline, while vehicle-treated mice had a mean tumor volume of ~1200 mm3 (P<0.0001).
Showed no effect on tumor growth in parental NCI-H1975 xenografts (P>0.9999).
Animal Model: BALB/c nude (female, 6-8 weeks old, subcutaneous xenograft of A549 cells expressing ELMO2-H435A mutant)[1]
Dosage: 25 mg/kg
Administration: i.p.; daily for 30 days
Result: Failed to suppress growth of tumors expressing the ELMO2-H435A mutant, confirming on-target activity via binding to ELMO2's HIS-435 residue.
Animal Model: BALB/c nude (female, 6-8 weeks old, subcutaneous xenograft of A549 cells)[1]
Dosage: 2.5 mg/kg; 10 mg/kg; 25 mg/kg
Administration: i.p.; daily
Result: Exhibited a dose-dependent antitumor response in A549 xenografts.
Molecular Weight

464.56

Formula

C29H28N4O2
CAS No.
SMILES

CC(NC(CN1C2=C(C3=C1C(N(C=N3)CC4=CC=CC=C4)=O)C=CC=C2)=O)CCC5=CC=CC=C5
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Storage

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Purity & Documentation
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ELMO2-IN-1 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:

ELMO2-IN-11216514-48-5AutophagyFAKA549NCI-H179295DNCI-H1703NCI-H1299mesenchymal-like non-small cell lung cancerELMO2EGFR inhibitor-resistant non-small cell lung cancerautophagy-dependent cell deathInhibitorinhibitorinhibit

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