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PK-11007

SKU: orb1225142

Description

A 2-sulfonylpyrimidine compound that is a mild thiol alkylator with anticancer activity toward p53-compromised cells; stabilizes p53 in vitro via selective alkylation of two surface-exposed cysteines without compromising p53 DNA binding activity; also induces cell death independent of p53, but with highly elevated levels of ROS and induction of ER stress.

Images & Validation

Key Properties

CAS Number38275-34-2
MW236.63
Purity>98% (HPLC)
FormulaC6H5ClN2O4S
SMILESO=C(C1=NC(S(=O)(C)=O)=NC=C1Cl)O
TargetMDM2-p53
SolubilityDMSO : 100 mg/mL 422.60 mM

Bioactivity

In Vitro
PK11000 (0-120 μM, 24 h) mildly inhibits mutant p53 cancer cells. PK11000 (0-50 μM, 5 d) shows anti-proliferation effects of breast cell lines. Cell Viability Assay Cell line: WI-38, HUH-6, NUGC-4, SJSA-1, HUH-7, NUGC-3, SW480 and MKN1 cells. Concentration: 0-120 μM. Incubation time: 24 hours. Result: Inhibited NUGC-3 cells mildly. Cell Proliferation Assay Cell line: UACC812, BT474, ZR-75-1, SUM 159, MDA-MD-468, MDA-MD-453, T47D, Hs578T(i8), MCF7, HCC1937, JimT1, BT20, HCC1143, BT549, SKBR3, MCF12A, MCF10A cells. Concentration: 0-50 μM. Incubation time: 5 days. Result: Inhibited breast cell lines with IC50 values ranging from 2.5 to >50 μM.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

PK11007

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Protocol Information

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