208725

Calphostin C, Cladosporium cladosporioides

A cell permeable, highly specific inhibitor of protein kinase C (IC₅₀ = 50 nM) that interacts with the protein′s regulatory domain by competing at the binding site of diacylglycerol and phorbol esters.

• 동의어(들): Calphostin C, Cladosporium cladosporioides, UCN-1028c
• 실험식(Hill 표기법): C₄₄H₃₈O₁₄
• CAS Number: 121263-19-2
• Molecular Weight: 790.76
• MDL number: MFCD00133155
• UNSPSC 코드: 12352200

속성

• Quality Level: 100
• 분석: ≥95% (HPLC)
• 양식: lyophilized solid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: light brown
• solubility: DMSO: 1 mg/mL; ethanol: soluble
• 배송 상태: ambient
• 저장 온도: 2-8°C
• InChI: 1S/C44H38O14/c1-20(56-43(50)22-10-8-7-9-11-22)16-25-31-32-26(17-21(2)57-44(51)58-24-14-12-23(45)13-15-24)42(55-6)40(49)34-28(47)19-30(53-4)36(38(32)34)35-29(52-3)18-27(46)33(37(31)35)39(48)41(25)54-5/h7-15,18-21,45,48-49H,16-17H2,1-6H3
• InChI key: LSUTUUOITDQYNO-UHFFFAOYSA-N

설명

일반 설명

A cell permeable, highly specific inhibitor of protein kinase C (IC₅₀ = 50 nM) that interacts with the protein’s regulatory domain by competing at the binding site of diacylglycerol and phorbol esters. Does not compete with Ca²⁺ or phospholipids. At higher concentrations inhibits myosin light chain kinase (IC₅₀ >5 µM), protein kinase A (IC₅₀ >50 µM), protein kinase G (IC₅₀ >25 µM), and p60^v-src (IC₅₀ >50 µM). Induces apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells. Requires brief exposure to light for activation.

Cell-permeable, highly specific inhibitor of protein kinase C (IC₅₀ = 50 nM) that interacts with the protein′s regulatory domain by competing at the binding site of diacylglycerol and phorbol esters. At higher concentrations inhibits myosin light chain kinase (IC₅₀ >5 µM), protein kinase A (IC₅₀ >50 µM), protein kinase G (IC₅₀ >25 µM), and p60^v-src protein tyrosine kinase (IC₅₀ >50 µM). Does not compete with Ca²⁺ or phospholipids. Also induces apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells. Inhibition of PKC is dependent on exposure to light in cell-free systems. Ordinary fluorescent light is sufficient for full activation.

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
PKC

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 50 nM against protein kinase C

경고

Toxicity: Standard Handling (A)

재구성

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

기타 정보

Jarvis, W.D., et al. 1994. Cancer Res.54, 1707.
Svetlov, S., and Nigami, S. 1993. Biochim. Biophys. Acta 1177, 75.
Gopalakrishna, R., et al. 1992. FEBS Lett. 314, 149.
Shimamato, H., et al. 1992. Br. J. Pharmacol.107, 282.
Bruns, R.F., et al. 1991. Biochem. Biophys. Res. Commun.176, 288.
Tamaoki, T., et al. 1990. Biotechnology8, 732.
Kobayashi, E., et al. 1989. Biochem. Biophys. Res. Commun.159, 548.

법적 정보

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable