2. Anti-infection TGF-beta/Smad Epigenetics Apoptosis
  3. Antibiotic PKC Apoptosis
  4. Calphostin C

Calphostin C  (Synonyms: カルホスチンC; UCN-1028C)

製品番号: HY-105416 純度: 99.9%
COA 取扱説明書 Technical Support

Calphostin C is a highly selective PKC inhibitor (IC50=0.05 μM) and tumor apoptosis inducer. Calphostin C competitively binds to PKC and inhibits PKC-mediated phosphorylation signal transduction. Calphostin C restores Na+/K+ ATPase activity in the sciatic nerve of diabetic mice and improves neuropathy. Calphostin C can be used in the study of anti-tumor and diabetic complications.

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Calphostin C

Calphostin C 構造式

CAS 番号 : 121263-19-2

容量 価格（税別） 在庫状況 数量
100 μg $400 在庫あり

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Based on 2 publication(s) in Google Scholar

Calphostin C 関連抗体

Top Publications Citing Use of Products

Antibiotic アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

PKC アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

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製品説明

Calphostin C is a highly selective PKC inhibitor (IC50=0.05 μM) and tumor apoptosis inducer. Calphostin C competitively binds to PKC and inhibits PKC-mediated phosphorylation signal transduction. Calphostin C restores Na+/K+ ATPase activity in the sciatic nerve of diabetic mice and improves neuropathy. Calphostin C can be used in the study of anti-tumor and diabetic complications[1][2][3].

IC50 & Target

protein kinase C[1]
Cellular Effect
Cell Line Type Value Description References
A549 IC50
3.2 μM
Compound: cal C
Inhibition of Wnt2/beta-casein signaling in human A549 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay
Inhibition of Wnt2/beta-casein signaling in human A549 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay
[PMID: 20729080]
A549 IC50
3.2 μM
Compound: Cal C
Cytotoxicity against human A549 cells expressing Wnt2 after 24 to 72 hrs by MTS assay
Cytotoxicity against human A549 cells expressing Wnt2 after 24 to 72 hrs by MTS assay
[PMID: 21855350]
HCT-116 IC50
2.86 μM
Compound: 83; PKF115-584
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTS assay
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTS assay
[PMID: 33445154]
体外実験

Calphostin C blocks the binding of [3H]PDBu to PKC and inhibits its activation process with IC50=0.03 μM[1].
Calphostin C (5 μM; 10 min-6 h) induces apoptosis in NALM-6 leukemia cells[2].
Calphostin C (2 μM; 24 h) is metabolized to inactive Calphostin B by esterases, and Calphostin B is not toxic to NALM-6 cells[2].

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

Calphostin C 関連抗体

Apoptosis Analysis[2]

Cell Line: NALM-6 (human B-cell leukemia)
Concentration: 5 μM
Incubation Time: 6 h
Result: Rapidly accumulated in NALM-6 cells, reaching a peak intracellular concentration of 212 pmol/10^6 cells (tmax=84.4 min) and inducing apoptosis via calcium mobilization.

Apoptosis Analysis[2]

Cell Line: NALM-6 (human B-cell leukemia)
Concentration: 2 μM
Incubation Time: 24 h
Result: Induced 100% cell death in NALM-6 cells, as confirmed by calcein/ethidium homodimer staining. Showed 90% of cells undergoing apoptosis, characterized by phosphatidylserine externalization (MC540-positive) and membrane permeability (PI-positive) in flow cytometry assay.

Cell Cytotoxicity Assay[2]

Cell Line: NALM-6 (human B-cell leukemia)
Concentration: 2-4 μM
Incubation Time: 24 h
Result: Showed no cytotoxicity in NALM-6 cells, with <5% cell death observed at 4 μM. Confirmed no induction of phosphatidylserine externalization or membrane permeability.
体内実験

Calphostin C (40 mg/kg; i.p.; single dose) has a maximum plasma concentration of 2.9 μM and an elimination half-life of 91.3 minutes in CD-1 mice, and showed no toxicity[2].
Calphostin C (1 μg/kg and 10 μg/kg; i.p.; single dose) restores the sciatic nerve Na+/K+ ATPase activity to normal levels in a streptozotocin (STZ)-induced diabetic mouse model[3].
Calphostin C (50 μg/mL; continuous administration by mini-osmotic pump; 0.5 μL per day; 2 weeks) restores the sciatic nerve Na+/K+ ATPase activity to normal levels in diabetic mice without affecting blood glucose levels[3].

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

790.76

分子式

C44H38O14
CAS 番号
Appearance

Solid

Color

Brown to reddish brown

SMILES

O=C(O[C@@H](CC1=C(C(C2=C(C=C(C(C3=C4C5=C(O)C=C3OC)=C2C1=C4C(C[C@@H](C)OC(C6=CC=CC=C6)=O)=C(OC)C5=O)OC)O)=O)OC)C)OC7=CC=C(C=C7)O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 1 mg/mL (1.26 mM; Need ultrasonic and warming; 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 1.2646 mL 6.3230 mL 12.6461 mL
5 mM --- --- ---
10 mM --- --- ---
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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純度とドキュメンテーション

純度: 99.9%

COA (258 KB)

取扱説明書 (2659 KB)
参考文献

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 1.2646 mL 6.3230 mL 12.6461 mL 31.6152 mL
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Calphostin C Related Classifications

  • Molarity Calculator

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The molarity calculator equation

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

質量   濃度   体積   分子量 *
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The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
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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:

Calphostin C121263-19-2UCN-1028CAntibioticPKCApoptosisProtein kinase Cprotein kinase Cantibioticapoptosiscytotoxic activityantitumorInhibitorinhibitorinhibit

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Calphostin C
製品番号:
HY-105416
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