2. Apoptosis NF-κB MAPK/ERK Pathway
  3. TNF Receptor NF-κB Apoptosis p38 MAPK
  4. BMS-561392 formate

BMS-561392 formate  (Synonyms: DPC 333 formate)

Cat. No.: HY-19667A Purity: 99.13% ee.: 100.00%
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Handling Instructions Technical Support

BMS-561392 formate (DPC 333 formate) is a selective ADAM17(TACE) inhibitor. BMS-561392 formate inhibits TNF-α secretion by regulating signaling pathways such as p44 MAPK and NF-κB. BMS-561392 formate also affects the survival of central nervous system-related cells including oligodendrocytes and microglia. BMS-561392 formate promotes microglial apoptosis, enlarges the injury area and exacerbates astrogliosis in a mouse spinal cord injury model. BMS-561392 formate can be used in research related to spinal cord injury and inflammatory diseases.

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

BMS-561392 formate

BMS-561392 formate Chemical Structure

CAS No. : 2922280-85-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
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10 mM * 1 mL in DMSO In-stock
Solid
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of BMS-561392 formate:

BMS-561392 formate Related Antibodies

Top Publications Citing Use of Products

View All TNF Receptor Isoform Specific Products:

View All Isoforms
TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

View All NF-κB Isoform Specific Products:

View All Isoforms
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

View All p38 MAPK Isoform Specific Products:

View All Isoforms
p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

BMS-561392 formate (DPC 333 formate) is a selective ADAM17(TACE) inhibitor. BMS-561392 formate inhibits TNF-α secretion by regulating signaling pathways such as p44 MAPK and NF-κB. BMS-561392 formate also affects the survival of central nervous system-related cells including oligodendrocytes and microglia. BMS-561392 formate promotes microglial apoptosis, enlarges the injury area and exacerbates astrogliosis in a mouse spinal cord injury model. BMS-561392 formate can be used in research related to spinal cord injury and inflammatory diseases[1][2].

In Vitro

BMS-561392 formate (10 nM; 1-2.5 h) potently inhibits recombinant human TACE (ADAM17) enzymatic activity by ~80%[1].
BMS-561392 formate (10 μM; 1 h pre-incubation followed by 4 h LPS stimulation) effectively suppresses LPS-induced TNF-α secretion in RAW264.7 macrophage cells[1].
BMS-561392 formate (1-100 μM; 1 h pre-incubation followed by 4 h LPS stimulation) dose-dependently inhibits LPS-induced p-IκB expression, and thus NFκB pathway activation, in RAW264.7 macrophage cells[1].
BMS-561392 formate (1-100 μM; 1 h pre-incubation followed by 1 h LPS stimulation) inhibits LPS-induced p-NFκB expression in RAW264.7 macrophage cells[1].
BMS-561392 formate (0.3-2.7 mM; 48 h) reduces viability of undifferentiated HOG cells in a concentration-dependent manner, with the greatest reduction (89.5-93.5%) observed at 2.7 mM after 48 h incubation[2].
BMS-561392 formate (0.3-2.7 mM; 48 h) modulates viability of BV-2 microglial cells in a concentration-dependent manner after 48 h incubation, with a slight increase at 0.3 mM, 50% reduction at 1.3 mM, and 94% reduction at 2.7 mM[2].
BMS-561392 formate (1.3-2.7 mM) induces apoptosis in BV-2 microglial cells, as shown by increased activated caspase-3-positive cells[2].
BMS-561392 formate (2.7 mM; 3 h) increases membrane TNFR-1 expression in BV-2 microglial cells by >50% after 3 h incubation[2].
BMS-561392 formate (0.3-2.7 mM; 3 h) modulates phosphorylated p44 MAPK levels in BV-2 microglial cells in a concentration-dependent manner after 3 h incubation, increasing levels at 0.3 mM and eliminating detectable levels at 2.7 mM, with no effect on phosphorylated p42 MAPK[2].

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

BMS-561392 formate Related Antibodies

ELISA Assay[1]

Cell Line: RAW264.7 macrophage cells
Concentration: 10 μM (pre-incubation); 1 μg/mL (LPS stimulation)
Incubation Time: 1 h (pre-incubation); 4 h (LPS stimulation)
Result: Reduced LPS-induced TNF-α levels to near-control levels.

Western Blot Analysis[1]

Cell Line: RAW264.7 macrophage cells
Concentration: 1, 10 and 100 μM (pre-incubation); 1 μg/mL (LPS stimulation)
Incubation Time: 1 h (pre-incubation); 4 h (LPS stimulation)
Result: Induced a dose-dependent reduction in LPS-stimulated p-IκB levels.
In Vivo

BMS-561392 formate (2.2 mM; s.c.; daily; 15 days) significantly impairs locomotor recovery, increases lesion size and astrogliosis, reduces microglial/macrophage infiltration, and promotes microglial apoptosis in 10-week-old C57BL/6 mice post SCI[2].

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

Animal Model: C57BL/6 (10-week-old)[2]
Dosage: 2.2 mM
Administration: s.c.; daily; 15 days
Result: Significantly reduced locomotor recovery as measured by BMS score.
Significantly increased lesion size.
Significantly increased astrogliosis in tissue caudal to the lesion site.
Significantly reduced Iba1 expression in tissue rostro-caudal to the lesion epicenter.
Significantly increased the number of apoptotic microglial/macrophage cells in tissue caudal to the lesion site.
Significantly increased pro-apoptotic Bax expression in spinal cord tissue.
Showed a non-significant decrease in anti-apoptotic Bcl-2 expression in spinal cord tissue.
Molecular Weight

522.59

Formula

C28H34N4O6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC=O.N[C@]1(C2=CC=C(C=C2)OCC3=CC(C)=NC4=C3C=CC=C4)C(N(CC1)[C@H](CC(C)C)C(NO)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (239.19 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9135 mL 9.5677 mL 19.1355 mL
5 mM 0.3827 mL 1.9135 mL 3.8271 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 (sealed storage, away from moisture). 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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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.13% ee.: 100.00%

SDS (252 KB)

COA (258 KB) HNMR (300 KB) RP-HPLC (223 KB) NP-HPLC (275 KB) MS (68 KB)

Handling Instructions (2659 KB)
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 (sealed storage, away from moisture). 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 1.9135 mL 9.5677 mL 19.1355 mL 47.8386 mL
5 mM 0.3827 mL 1.9135 mL 3.8271 mL 9.5677 mL
10 mM 0.1914 mL 0.9568 mL 1.9135 mL 4.7839 mL
15 mM 0.1276 mL 0.6378 mL 1.2757 mL 3.1892 mL
20 mM 0.0957 mL 0.4784 mL 0.9568 mL 2.3919 mL
25 mM 0.0765 mL 0.3827 mL 0.7654 mL 1.9135 mL
30 mM 0.0638 mL 0.3189 mL 0.6378 mL 1.5946 mL
40 mM 0.0478 mL 0.2392 mL 0.4784 mL 1.1960 mL
50 mM 0.0383 mL 0.1914 mL 0.3827 mL 0.9568 mL
60 mM 0.0319 mL 0.1595 mL 0.3189 mL 0.7973 mL
80 mM 0.0239 mL 0.1196 mL 0.2392 mL 0.5980 mL
100 mM 0.0191 mL 0.0957 mL 0.1914 mL 0.4784 mL
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BMS-561392 formate 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:

BMS-561392 formate2922280-85-9DPC 333 formateTNF ReceptorNF-κBApoptosisp38 MAPKTumor Necrosis Factor ReceptorTNFRNuclear factor-κBNuclear factor-kappaBADAM17RAW264.7 macrophage cellsTNF-αmicrogliaBV-2 microglial cellscortical neuronsastrocytesoligodendrocytesp44 MAPKmouse spinal cord injury modelInhibitorinhibitorinhibit

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