1. Anti-infection Apoptosis
  2. Antibiotic Bcl-2 Family Apoptosis
  3. KRN5500

KRN5500 (NSC 650426), a Spicamycin (HY-127130) derivative and a nucleoside-like antibiotic with anti-tumor activity. KRN5500 also induces apoptosis via the down-regulation of Bcl-2 expression. KRN5500 shows a significant efficacy in the human tumor xenograft model in mice.

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KRN5500 Chemical Structure

KRN5500 Chemical Structure

CAS No. : 151276-95-8

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Description

KRN5500 (NSC 650426), a Spicamycin (HY-127130) derivative and a nucleoside-like antibiotic with anti-tumor activity. KRN5500 also induces apoptosis via the down-regulation of Bcl-2 expression. KRN5500 shows a significant efficacy in the human tumor xenograft model in mice[1][2].

IC50 & Target[1]

Bcl-2

 

In Vitro

KRN5500 (10-160 ng/mL; 0-5 d) potently inhibits cell proliferation and viability of NB4, NKM-1, and HL-60 cells. KRN5500 (40 ng/mL, 160 ng/mL; 48 h) induces apoptosis in NB4, HL-60 and NKM-1 cells. KRN5500 (40 ng/mL, 80 ng/mL; 36 h) down-regulates the Bcl-2 expression in NB4 cells[1].

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

Cell Viability Assay[1]

Cell Line: NB4, HL-60, NKM-1, NOP-1 and Daudi cells
Concentration: 10 ng/mL, 20 ng/mL, 40 ng/mL, 80 ng/mL, 160 ng/mL
Incubation Time: 0, 1, 2, 3, 4, and 5 days or 72 h
Result: Completely inhibited cell proliferation and viability of NB4 and NKM-1 at about 80 ng/mL, of HL-60 at 160 ng/mL.
Inhibited cells viability of IC50s of 51.6 ng/mL, 89.7 ng/mL, 66.5 ng/mL, 277.0 ng/mL, 242.1 ng/mL, respectively.

Western Blot Analysis[1]

Cell Line: NB4 cells
Concentration: 40 ng/mL, 80 ng/mL
Incubation Time: 36 h
Result: Reduced the Bcl-2 expression without affecting Bcl-xL and Bax expression.
In Vivo

KRN5500 (4 mg/kg; i.p.; once daily for 5 d) shows anti-tumor activity against some murine tumors and human tumor xenografts with a decreasing tumor weight[2].

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

Animal Model: Mouse model with murine tumors and human tumor xenografts[2]
Dosage: 4 mg/kg
Administration: Intraperitoneal injection; once daily for 5 days
Result: Prolonged the survival of P388 leukemia- and B16 melanoma-bearing mice but lacked marginally effective on colon adenocarcinoma.
Decreased tumor weight in 10 human stomach, 14 colon and 2 esophageal cancers.
Clinical Trial
Molecular Weight

589.68

Formula

C28H43N7O7

CAS No.
SMILES

O[C@@H]1[C@H](O)[C@@H](NC(CNC(/C=C/C=C/CCCCCCCCC)=O)=O)[C@]([H])([C@@H](O)CO)O[C@@H]1NC2=NC=NC3=C2NC=N3

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
References
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KRN5500 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.

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Product Name:
KRN5500
Cat. No.:
HY-13659
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