APTSTAT3-9R

APTSTAT3-9R, a specific STAT3-binding peptide, inhibits STAT3 activation and downstream signaling by specifically blocking STAT3 phosphorylation. APTSTAT3-9R exerts antiproliferative effects and antitumor activity.

Product information

Molecular Weight: 4947.51

Formula: C223H330N80O51

Synonym:

s8197

Chemical Name: H-DL-His-Gly-DL-Phe-DL-Gln-DL-Trp-DL-Pro-Gly-DL-Ser-DL-Trp-DL-xiThr-DL-Trp-DL-Glu-DL-Asn-Gly-DL-Lys-DL-Trp-DL-xiThr-DL-Trp-DL-Lys-Gly-DL-Ala-DL-Tyr-DL-Gln-DL-Phe-DL-Leu-DL-Lys-Gly-Gly-Gly-Gly-DL-Ser-DL-Arg-DL-Arg-DL-Arg-DL-Arg-DL-Arg-DL-Arg-DL-Arg-DL-Arg-DL-Arg-OH

Smiles: CC(C)CC(NC(=O)C(CC1=CC=CC=C1)NC(=O)C(CCC(N)=O)NC(=O)C(CC1=CC=C(O)C=C1)NC(=O)C(C)NC(=O)CNC(=O)C(CCCCN)NC(=O)C(CC1=CNC2=CC=CC=C12)NC(=O)C(NC(=O)C(CC1=CNC2=CC=CC=C12)NC(=O)C(CCCCN)NC(=O)CNC(=O)C(CC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(CC1=CNC2=CC=CC=C12)NC(=O)C(NC(=O)C(CC1=CNC2=CC=CC=C12)NC(=O)C(CO)NC(=O)CNC(=O)C1CCCN1C(=O)C(CC1=CNC2=CC=CC=C12)NC(=O)C(CCC(N)=O)NC(=O)C(CC1=CC=CC=C1)NC(=O)CNC(=O)C(N)CC1=CNC=N1)C(C)O)C(C)O)C(=O)NC(CCCCN)C(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)NC(CO)C(=O)NC(CCCNC(N)=N)C(=O)NC(CCCNC(N)=N)C(=O)NC(CCCNC(N)=N)C(=O)NC(CCCNC(N)=N)C(=O)NC(CCCNC(N)=N)C(=O)NC(CCCNC(N)=N)C(=O)NC(CCCNC(N)=N)C(=O)NC(CCCNC(N)=N)C(=O)NC(CCCNC(N)=N)C(O)=O

InChiKey: DSGGVPGAEGYDOM-UHFFFAOYSA-N

InChi: InChI=1S/C223H330N80O51/c1-116(2)88-156(200(339)278-141(52-22-25-75-224)185(324)268-107-174(314)265-105-172(312)264-106-173(313)266-108-176(316)276-166(113-304)208(347)287-150(61-34-84-256-221(243)244)195(334)285-148(59-32-82-254-219(239)240)193(332)283-146(57-30-80-252-217(235)236)191(330)281-144(55-28-78-250-215(231)232)189(328)280-145(56-29-79-251-216(233)234)190(329)282-147(58-31-81-253-218(237)238)192(331)284-149(60-33-83-255-220(241)242)194(333)286-151(62-35-85-257-222(245)246)196(335)291-155(214(353)354)63-36-86-258-223(247)248)293-203(342)159(90-121-40-10-7-11-41-121)294-197(336)152(69-72-169(228)309)289-202(341)158(91-122-65-67-129(308)68-66-122)292-183(322)117(3)273-175(315)109-269-186(325)142(53-23-26-76-225)279-204(343)160(92-123-99-259-136-47-17-12-42-130(123)136)298-211(350)181(118(4)306)301-206(345)162(94-125-101-261-138-49-19-14-44-132(125)138)295-188(327)143(54-24-27-77-226)274-177(317)111-270-187(326)164(98-171(230)311)297-198(337)154(71-74-180(320)321)290-205(344)161(93-124-100-260-137-48-18-13-43-131(124)137)299-212(351)182(119(5)307)302-207(346)163(95-126-102-262-139-50-20-15-45-133(126)139)296-209(348)167(114-305)277-179(319)112-271-210(349)168-64-37-87-303(168)213(352)165(96-127-103-263-140-51-21-16-46-134(127)140)300-199(338)153(70-73-170(229)310)288-201(340)157(89-120-38-8-6-9-39-120)275-178(318)110-267-184(323)135(227)97-128-104-249-115-272-128/h6-21,38-51,65-68,99-104,115-119,135,141-168,181-182,259-263,304-308H,22-37,52-64,69-98,105-114,224-227H2,1-5H3,(H2,228,309)(H2,229,310)(H2,230,311)(H,249,272)(H,264,312)(H,265,314)(H,266,313)(H,267,323)(H,268,324)(H,269,325)(H,270,326)(H,271,349)(H,273,315)(H,274,317)(H,275,318)(H,276,316)(H,277,319)(H,278,339)(H,279,343)(H,280,328)(H,281,330)(H,282,329)(H,283,332)(H,284,331)(H,285,334)(H,286,333)(H,287,347)(H,288,340)(H,289,341)(H,290,344)(H,291,335)(H,292,322)(H,293,342)(H,294,336)(H,295,327)(H,296,348)(H,297,337)(H,298,350)(H,299,351)(H,300,338)(H,301,345)(H,302,346)(H,320,321)(H,353,354)(H4,231,232,250)(H4,233,234,251)(H4,235,236,252)(H4,237,238,253)(H4,239,240,254)(H4,241,242,255)(H4,243,244,256)(H4,245,246,257)(H4,247,248,258)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: To be determined

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

APTSTAT3-9R (7.5, 15, and 30 μmol/L; 6 hours) significantly reduces STAT3–DNA-binding activity in a dose-dependent manner in human lung carcinoma cells (A549). APTSTAT3-9R (30 μM; for 2 weeks) suppresses cell viability and proliferation of cancer cells and significantly suppresses colony formation. APTSTAT3-9R has IC50s of 10 to 20 μM in A549, B16F1 and HepG2 cells. APTSTAT3-9R (7.5, 15, and 30 μmol/L; 6 hours) effectively inhibits phosphorylation of STAT3 but does not affect the level of AKT phosphorylation, indicating specificity of the aptide.

In Vivo:

APTSTAT3-9R (8 mg/kg in 50 μL; intratumorally injected every other day for a total of four injections) suppresses tumor growth in 6-week-old female BALB/c nude mice with A549 cells.

References:

1. Daejin Kim, et al. A Specific STAT3-binding Peptide Exerts Antiproliferative Effects and Antitumor Activity by Inhibiting STAT3 Phosphorylation and Signaling. Cancer Res. 2014 Apr 15;74(8):2144-51.

Products are for research use only. Not for human use.