2. PROTAC Metabolic Enzyme/Protease
  3. PROTACs NAMPT
  4. Nampt degrader-2

Nampt degrader-2 is a fluorescent PROTAC, which efficiently degrades NAMPT with an IC50 of 41.9 nM. Nampt degrader-2 binds to NAMPT and VHL to form a ternary complex and subsequently induced NAMPT degradation via ubiquitin-proteasome system (UPS). Nampt degrader-2 leads to significant reduction of NAD+ and exerts potent antitumor activities.

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Nampt degrader-2 Chemical Structure

Nampt degrader-2 Chemical Structure

CAS No. : 3035008-40-0

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Based on 1 publication(s) in Google Scholar

Nampt degrader-2 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

Nampt degrader-2 is a fluorescent PROTAC, which efficiently degrades NAMPT with an IC50 of 41.9 nM. Nampt degrader-2 binds to NAMPT and VHL to form a ternary complex and subsequently induced NAMPT degradation via ubiquitin-proteasome system (UPS). Nampt degrader-2 leads to significant reduction of NAD+ and exerts potent antitumor activities[1].

IC50 & Target[1]

VHL

 

NAMPT

41.9 nM (IC50)

In Vitro

Nampt degrader-2 (Compound B4; 30 nM; 24 h) is able to degrade NAMPT with a DC50 value of 8.4 nM. Nampt degrader-2 enables the visualization of degradation in A2780 cells[1].
Nampt degrader-2 (Compound B4) shows the best antitumor activity in suppression of the proliferation in A2780 cells (IC50 = 12.1 nM)[1].

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

Nampt degrader-2 Related Antibodies

Western Blot Analysis[1]

Cell Line: A2780 cells
Concentration: 30 nM
Incubation Time: 24 h
Result: Were able to degrade NAMPT in A2780 cells at the concentration of 30 nM.
In Vivo

Nampt degrader-2 (Compound B4; 10-30 mg/kg; i.p; once a day; for 14 consecutive days) shows excellent antitumor effects in a dose-dependent manner. And Nampt degrader-2 significantly decreases the NAMPT levels in the tumors[1].

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

Animal Model: BALB/C nude female mice (4-5 weeks of age, 14-18 g) injected with A2780 cells[1]
Dosage: 10 mg/kg, 30 mg/kg
Administration: i.p; once a day; for 14 consecutive days
Result: Achieved excellent antitumor effects in a dose-dependent manner.
Molecular Weight

1052.33

Formula

C59H73N9O7S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C(C1=CC=C(C=C1)C(NCC2=CN=CC=C2)=O)=NC3=C4C=C(C=C3)NC(CCCCCCCCCCC(N[C@@H](C(C)(C)C)C(N5C[C@H](O)C[C@H]5C(N[C@@H](C)C6=CC=C(C7=C(C)N=CS7)C=C6)=O)=O)=O)=O)N4CCC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (95.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9503 mL 4.7514 mL 9.5027 mL
5 mM 0.1901 mL 0.9503 mL 1.9005 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.9503 mL 4.7514 mL 9.5027 mL 23.7568 mL
5 mM 0.1901 mL 0.9503 mL 1.9005 mL 4.7514 mL
10 mM 0.0950 mL 0.4751 mL 0.9503 mL 2.3757 mL
15 mM 0.0634 mL 0.3168 mL 0.6335 mL 1.5838 mL
20 mM 0.0475 mL 0.2376 mL 0.4751 mL 1.1878 mL
25 mM 0.0380 mL 0.1901 mL 0.3801 mL 0.9503 mL
30 mM 0.0317 mL 0.1584 mL 0.3168 mL 0.7919 mL
40 mM 0.0238 mL 0.1188 mL 0.2376 mL 0.5939 mL
50 mM 0.0190 mL 0.0950 mL 0.1901 mL 0.4751 mL
60 mM 0.0158 mL 0.0792 mL 0.1584 mL 0.3959 mL
80 mM 0.0119 mL 0.0594 mL 0.1188 mL 0.2970 mL
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Nampt degrader-2 Related Classifications

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:

Nampt degrader-23035008-40-0Nampt degrader2Nampt degrader 2PROTACsNAMPTNicotinamide phosphoribosyl transferasePBEFVisfatinpre-B cell-enhancing factorPre-B cell colony enhancing factorPROTAC Nampt degraderVHLubiquitin-proteasome systemantitumor activitiesfluorescentInhibitorinhibitorinhibit

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