1. GPCR/G Protein MAPK/ERK Pathway Apoptosis
  2. Ras Apoptosis
  3. Diazepinomicin

Diazepinomicin  (Synonyms: ECO-4601; TLN-4601; BU 4664L)

Cat. No.: HY-N6674
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Diazepinomicin (TLN-4601) is a secondary metabolite produced by Micromonospora sp. Diazepinomicin (TLN-4601) inhibits the EGF-induced Ras-ERK MAPK signaling pathway and induces apoptosis. An anti-tumor agent for K-Ras mutant models.

For research use only. We do not sell to patients.

Diazepinomicin Chemical Structure

Diazepinomicin Chemical Structure

CAS No. : 733035-26-2

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Description

Diazepinomicin (TLN-4601) is a secondary metabolite produced by Micromonospora sp. Diazepinomicin (TLN-4601) inhibits the EGF-induced Ras-ERK MAPK signaling pathway and induces apoptosis. An anti-tumor agent for K-Ras mutant models[1].

IC50 & Target

Diazepinomicin (TLN-4601) inhibits the EGF-induced Ras-ERK MAPK signaling pathway post Ras prenylation and prior to MEK activation[1].

Cellular Effect
Cell Line Type Value Description References
HUVEC IC50
0.43 μg/mL
Compound: 1, BU-4664L
Antiinvasive activity against HUVEC assessed as inhibition of cell migration after 6 hrs by Matrigel assay
Antiinvasive activity against HUVEC assessed as inhibition of cell migration after 6 hrs by Matrigel assay
[PMID: 20056543]
HUVEC IC50
0.72 μg/mL
Compound: 1, BU-4664L
Antiangiogenic activity against HUVEC cells assessed as inhibition of vascular formation after 6 hrs by wound healing assay
Antiangiogenic activity against HUVEC cells assessed as inhibition of vascular formation after 6 hrs by wound healing assay
[PMID: 20056543]
NCI-H460 GI50
13.6 μM
Compound: 1; BU-4664L
Antiproliferative activity against human NCI-H460 cells assessed as cell growth inhibition by MTT assay
Antiproliferative activity against human NCI-H460 cells assessed as cell growth inhibition by MTT assay
[PMID: 34838651]
PC-3 GI50
1.95 μM
Compound: 1; BU-4664L
Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition by MTT assay
Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition by MTT assay
[PMID: 34838651]
Renca IC50
0.78 μg/mL
Compound: 1, BU-4664L
Antiinvasive activity against mouse Renca by Matrigel assay
Antiinvasive activity against mouse Renca by Matrigel assay
[PMID: 20056543]
Clinical Trial
Molecular Weight

462.58

Formula

C28H34N2O4

CAS No.
Appearance

Solid

Color

Off-white to gray

SMILES

O=C1C2=CC=CC(O)=C2NC3=C(O)C=C(O)C=C3N1C/C=C(C)/CC/C=C(C)/CC/C=C(C)\C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Purity & Documentation
References
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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.

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Diazepinomicin
Cat. No.:
HY-N6674
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