1. Apoptosis
  2. Caspase Apoptosis
  3. Ac-ATS010-KE

Ac-ATS010-KE is a selective polypeptide inhibitor of caspase-3. Ac-ATS010-KE protects cells from FasL-induced apoptosis. The unmethylated form of Ac-ATS010-KE exhibits better cell viability than the fully methylated form. Ac-ATS010-KE can be used in research on cancers such as colorectal cancer and the development of caspase-3-targeted molecular probes.

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

Custom Peptide Synthesis

Ac-ATS010-KE

Ac-ATS010-KE Chemical Structure

CAS No. : 2379342-67-1

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Description

Ac-ATS010-KE is a selective polypeptide inhibitor of caspase-3. Ac-ATS010-KE protects cells from FasL-induced apoptosis. The unmethylated form of Ac-ATS010-KE exhibits better cell viability than the fully methylated form. Ac-ATS010-KE can be used in research on cancers such as colorectal cancer and the development of caspase-3-targeted molecular probes[1].

IC50 & Target[1]

Caspase-3

 

In Vitro

Ac-ATS010-KE potently inhibits purified recombinant caspase-3 and exhibits high selectivity over caspase-6, caspase-7, caspase-8, caspase-9, and caspase-10[1].
Ac-ATS010-KE protects Jurkat cells from MegaFasL-induced apoptosis, with non-methylated Ac-ATS010-KE showing superior performance compared to its per-methylated counterpart[1].
Ac-ATS010-KE (25 µM; 1 hour) reduces [18F]MICA-316 uptake in STS-treated caspase-3-positive HeLa cells, demonstrating competitive binding to caspase-3[1].

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

In Vivo

Ac-ATS010-KE-derived radiotracer [18F]MICA-316 (~18.5 MBq; intravenous injection) binds to activated caspase-3 in tumor homogenates in vitro, and exhibits low and non-differential tumor uptake[1].

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

Animal Model: CD1-/- nude (female, 6-8 weeks old, 20-25 g, subcutaneous colorectal cancer xenograft model)[1]
Dosage: 18.5 MBq
Administration: i.v.
Result: Showed tumour uptake of 0.55 %ID/CC at 60 minutes post-injection in conatumumab-treated mice and 0.52 %ID/CC in IgG1 isotype control-treated mice.
Demonstrated no significant difference in high-intensity voxel (P95) intensity between treated and control groups.
Bound active caspase-3 (17 and 19 kDa subunits) in homogenates of conatumumab (HY-P99260)-treated COLO205 tumours.
Animal Model: CD1-/- nude (female, 6-8 weeks old, 20-25 g)[1]
Dosage: 18.5 MBq
Administration: i.v.
Result: Exhibited rapid blood clearance, mixed renal-hepatobiliary excretion, negligible bone uptake, and low non-specific background uptake.
Showed low in vivo serum stability, with < 30% intact tracer remaining for [18F]MICA-314 to -318 at 30 minutes post-injection; [18F]MICA-320 had 58.8% intact tracer remaining at 30 minutes.
Molecular Weight

960.88

Formula

C43H41F5N6O12S

CAS No.
Sequence

Ac-Pal-Asp-{Phe(F5)}-Phe-Asp-KE

Sequence Shortening

Ac-{Pal}-D-{Phe(F5)}-FD-KE

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Purity & Documentation
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    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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Ac-ATS010-KE
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HY-P11865
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