1. Apoptosis
  2. Apoptosis Caspase
  3. d-(KLAKLAK)2, Proapoptotic Peptide acetate

d-(KLAKLAK)2, Proapoptotic Peptide acetate is a pro-Apoptotic peptide whose core mechanism of action is to disrupt organelle membranes, especially mitochondrial membranes, thereby inducing apoptosis. d-(KLAKLAK)2, Proapoptotic Peptide acetate activates the activity of caspase 3/7 in cancer cells. Although d-(KLAKLAK)2 Proapoptotic Peptide acetate exhibits very low toxicity to eukaryotic cells extracellularly, it cannot effectively penetrate cell membranes to enter the cytoplasm on its own. d-(KLAKLAK)2, Proapoptotic Peptide acetate must be conjugated with a carrier capable of "homing" and "internalization" to exert its anti-cancer effects.

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d-(KLAKLAK)2, Proapoptotic Peptide acetate

d-(KLAKLAK)2, Proapoptotic Peptide acetate Chemical Structure

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Description

d-(KLAKLAK)2, Proapoptotic Peptide acetate is a pro-Apoptotic peptide whose core mechanism of action is to disrupt organelle membranes, especially mitochondrial membranes, thereby inducing apoptosis. d-(KLAKLAK)2, Proapoptotic Peptide acetate activates the activity of caspase 3/7 in cancer cells. Although d-(KLAKLAK)2 Proapoptotic Peptide acetate exhibits very low toxicity to eukaryotic cells extracellularly, it cannot effectively penetrate cell membranes to enter the cytoplasm on its own. d-(KLAKLAK)2, Proapoptotic Peptide acetate must be conjugated with a carrier capable of "homing" and "internalization" to exert its anti-cancer effects[1][2].

IC50 & Target [1]

Caspase-3

 

Caspase-7

 

In Vitro

d-(KLAKLAK)2 (0.44 μM) acetate induces mitochondrial swelling in a cell-free system with an ED50 of 0.44 μM[1].
d-(KLAKLAK)2 (0.4 μM) acetate induces mitochondrial membrane potential loss in a cell-free system with an ED50 of 0.4 μM[1].
Cationic liposome-delivered d-(KLAKLAK)2 (co-loaded with G3139) (0.1875-1.5 μM; 24 h) acetate reduces viability of B16(F10) mouse melanoma cells by ~20% at 0.1875 μM and ~40% at 0.375 μM[1].
d-(KLAKLAK)2, Proapoptotic Peptide (24 hours) acetate does not inhibit proliferation of highly metastatic PC-3M-1E8 prostate cancer cells, MKN-45sci gastric cancer cells, or NIH/3T3 fibroblast cells[2].
d-(KLAKLAK)2, Proapoptotic Peptide acetate does not induce apoptosis in highly metastatic PC-3M-1E8 prostate cancer cells or MKN-45sci gastric cancer cells, as it cannot enter the tumor cells[2].

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

In Vivo

Cationic liposomes co-loaded with d-(KLAKLAK)2, Proapoptotic Peptide acetate and G3139 (1.52 μg; intratumoral; twice daily, total 2 doses) deliver a 60% tumor growth inhibition in B16(F10) melanoma-bearing mice via enhanced apoptotic activity[1].

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

Molecular Weight

1523.01 (free base)

Formula

C72H139N21O14xC2H4O2

Appearance

Solid

Sequence

{d-(Lys-Leu-Ala-Lys-Leu-Ala-Lys-Lys-Leu-Ala-Lys-Leu-Ala-Lys)}-NH2

Sequence Shortening

{d-(KLAKLAKKLAKLAK)}-NH2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

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

Solvent & Solubility
In Vitro: 

DMSO : 1 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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Purity & Documentation
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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:
d-(KLAKLAK)2, Proapoptotic Peptide acetate
Cat. No.:
HY-P10370B
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