Name: IPA-3
Brand: Selleck Chemicals
SKU: S7093
Rating: 5 (49 reviews)

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품질 관리

배치: S709301 DMSO]70 mg/mL]false]Ethanol]7 mg/mL]false]Water]Insoluble]false 순도: 99.66%

최고 수준의 품질로 Nature Medicine에 인용됨
COA
NMR
SDS
데이터시트

99.66

관련 타겟	Akt Wnt/beta-catenin PKC HSP ROCK Microtubule Associated Integrin Bcr-Abl Actin FAK
기타 PAK 억제제	FRAX597 PF-3758309 FRAX486 FRAX1036 LCH-7749944 NVS-PAK1-1 Hydrastine GNE 2861 G-5555

세포 배양, 처리 및 작업 농도

세포주	분석 유형	활성 설명
human NALM-6 cell	Growth inhibition assay	Inhibition of human NALM-6 cell growth in a cell viability assay, IC50=0.97694 μM
human SW1710 cell	Growth inhibition assay	Inhibition of human SW1710 cell growth in a cell viability assay, IC50=1.17833 μM
human YT cell	Growth inhibition assay	Inhibition of human YT cell growth in a cell viability assay, IC50=1.39036 μM
human BL-70 cell	Growth inhibition assay	Inhibition of human BL-70 cell growth in a cell viability assay, IC50=2.03796 μM
human SIG-M5 cell	Growth inhibition assay	Inhibition of human SIG-M5 cell growth in a cell viability assay, IC50=2.10219 μM
human MCF7 cell	Growth inhibition assay	Inhibition of human MCF7 cell growth in a cell viability assay, IC50=2.1807 μM
human GB-1 cell	Growth inhibition assay	Inhibition of human GB-1 cell growth in a cell viability assay, IC50=2.63494 μM
human KU812 cell	Growth inhibition assay	Inhibition of human KU812 cell growth in a cell viability assay, IC50=2.7595 μM
human QIMR-WIL cell	Growth inhibition assay	Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50=2.90891 μM
human BL-41 cell	Growth inhibition assay	Inhibition of human BL-41 cell growth in a cell viability assay, IC50=3.09844 μM
human CMK cell	Growth inhibition assay	Inhibition of human CMK cell growth in a cell viability assay, IC50=3.14599 μM
human U-698-M cell	Growth inhibition assay	Inhibition of human U-698-M cell growth in a cell viability assay, IC50=3.23856 μM
human Daoy cell	Growth inhibition assay	Inhibition of human Daoy cell growth in a cell viability assay, IC50=3.24662 μM
human 786-0 cell	Growth inhibition assay	Inhibition of human 786-0 cell growth in a cell viability assay, IC50=3.31805 μM
human REH cell	Growth inhibition assay	Inhibition of human REH cell growth in a cell viability assay, IC50=3.36655 μM
human MHH-PREB-1 cell	Growth inhibition assay	Inhibition of human MHH-PREB-1 cell growth in a cell viability assay, IC50=3.46687 μM
human KE-37 cell growth	Growth inhibition assay	Inhibition of human KE-37 cell growth in a cell viability assay, IC50=3.50231 μM
human CAL-51 cell	Growth inhibition assay	Inhibition of human CAL-51 cell growth in a cell viability assay, IC50=3.54519 μM
human CA46 cell	Growth inhibition assay	Inhibition of human CA46 cell growth in a cell viability assay, IC50=3.6618 μM
human HEL cell	Growth inhibition assay	Inhibition of human HEL cell growth in a cell viability assay, IC50=3.72768 μM
human NB6 cell	Growth inhibition assay	Inhibition of human NB6 cell growth in a cell viability assay, IC50=3.83751 μM
human 8305C cell	Growth inhibition assay	Inhibition of human 8305C cell growth in a cell viability assay, IC50=4.16758 μM
human EW-13 cell	Growth inhibition assay	Inhibition of human EW-13 cell growth in a cell viability assay, IC50=4.20148 μM
human NB13 cell	Growth inhibition assay	Inhibition of human NB13 cell growth in a cell viability assay, IC50=4.2256 μM
human EB2 cell	Growth inhibition assay	Inhibition of human EB2 cell growth in a cell viability assay, IC50=4.49142 μM
human HOS cell	Growth inhibition assay	Inhibition of human HOS cell growth in a cell viability assay
human HLE cell	Growth inhibition assay	Inhibition of human HLE cell growth in a cell viability assay, IC50=4.52149 μM
human ST486 cell	Growth inhibition assay	Inhibition of human ST486 cell growth in a cell viability assay, IC50=4.8654 μM
human NCI-H2009 cell	Growth inhibition assay	Inhibition of human NCI-H2009 cell growth in a cell viability assay, IC50=5.04354 μM
human NH-12 cell	Growth inhibition assay	Inhibition of human NH-12 cell growth in a cell viability assay, IC50=5.1176 μM
human BFTC-905 cell	Growth inhibition assay	Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=5.14768 μM
human RKO cell	Growth inhibition assay	Inhibition of human RKO cell growth in a cell viability assay, IC50=5.28471 μM
human PF-382	Growth inhibition assay	Inhibition of human PF-382 cell growth in a cell viability assay, IC50=5.35226 μM
human SR cell	Growth inhibition assay	Inhibition of human SR cell growth in a cell viability assay, IC50=5.37256 μM
human WSU-NHL cell	Growth inhibition assay	Inhibition of human WSU-NHL cell growth in a cell viability assay, IC50=5.52067 μM
human CAL-12T cell	Growth inhibition assay	Inhibition of human CAL-12T cell growth in a cell viability assay, IC50=5.6414 μM
human Daudi cell	Growth inhibition assay	Inhibition of human Daudi cell growth in a cell viability assay, IC50=5.68477 μM
human MC-CAR cell	Growth inhibition assay	Inhibition of human MC-CAR cell growth in a cell viability assay, IC50=5.70644 μM
human RPMI-8402 cell	Growth inhibition assay	Inhibition of human RPMI-8402 cell growth in a cell viability assay, IC50=5.76876 μM
human CCRF-CEM cell	Growth inhibition assay	Inhibition of human CCRF-CEM cell growth in a cell viability assay, IC50=5.97667 μM
human CHP-126 cell	Growth inhibition assay	Inhibition of human CHP-126 cell growth in a cell viability assay, IC50=6.74268 μM
human NB69 cell	Growth inhibition assay	Inhibition of human NB69 cell growth in a cell viability assay, IC50=6.76352 μM
human KS-1 cell	Growth inhibition assay	Inhibition of human KS-1 cell growth in a cell viability assay, IC50=6.88549 μM
human J82 cell	Growth inhibition assay	Inhibition of human J82 cell growth in a cell viability assay, IC50=7.04965 μM
human SW872 cell	Growth inhibition assay	Inhibition of human SW872 cell growth in a cell viability assay, IC50=7.83558 μM
human HC-1 cell	Growth inhibition assay	Inhibition of human HC-1 cell growth in a cell viability assay, IC50=8.06805 μM
human DU-145 cell	Growth inhibition assay	Inhibition of human DU-145 cell growth in a cell viability assay, IC50=8.21464 μM
human HL-60 cell	Growth inhibition assay	Inhibition of human HL-60 cell growth in a cell viability assay, IC50=8.84605 μM
human MV-4-11 cell	Growth inhibition assay	Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=9.1649 μM
human SK-N-DZ cell	Growth inhibition assay	Inhibition of human SK-N-DZ cell growth in a cell viability assay, IC50=9.20423 μM
human HT-1197 cell	Growth inhibition assay	Inhibition of human HT-1197 cell growth in a cell viability assay, IC50=10.3073 μM
human NOS-1 cell	Growth inhibition assay	Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=11.7152 μM
human HT-1080 cell	Growth inhibition assay	Inhibition of human HT-1080 cell growth in a cell viability assay, IC50=18.6283 μM
human SK-LU-1 cell	Growth inhibition assay	Inhibition of human SK-LU-1 cell growth in a cell viability assay, IC50=18.8731 μM
human SW48 cell	Growth inhibition assay	Inhibition of human SW48 cell growth in a cell viability assay, IC50=21.8897 μM
human A2780 cell	Growth inhibition assay	Inhibition of human A2780 cell growth in a cell viability assay, IC50=28.371 μM
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화학 정보, 보관 및 안정성

분자량	350.45	화학식	C₂₀H₁₄O₂S₂	보관 (수령일로부터)	3년-20°C분말
CAS 번호	42521-82-4	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	N/A			Smiles	C1=CC=C2C(=C1)C=CC(=C2SSC3=C(C=CC4=CC=CC=C43)O)O

용해도

In vitro
배치:

DMSO : 70 mg/mL (199.74 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 7 mg/mL

Water : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	2.500mg/ml (7.13mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH₂O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘

특징	IPA-3 binds covalently to the Pak1 regulatory domain and prevents binding to the upstream activator Cdc42.
Targets/IC₅₀/Ki	PAK1 (Cell-free assay) 2.5 μM
시험관 내(In vitro)	IPA-3은 p21-활성화 키나제 1(Pak1)의 비-ATP 경쟁적 알로스테릭 억제제입니다. PIR3.5는 이 화합물의 대조 화합물입니다. 이는 Thr423에서 Cdc42-자극 Pak1 자가인산화를 방지합니다. 이 화합물은 스핑고신 의존성 Pak1 자가인산화도 방지합니다. Pak1의 노출된 시스테인 잔류물을 표적으로 삼지 않습니다. 이 억제제의 이황화 결합은 Pak1 억제에 중요하며, 환원제 디티오트레이톨(DTT)에 의한 시험관 내 환원은 이 화학 물질에 의한 Pak1 억제를 무효화합니다. 다양한 활성제에 의한 Pak1 활성화를 억제하지만, 사전 활성화된 Pak1은 억제하지 않습니다. 이 화합물은 생쥐 배아 섬유아세포에서 PDGF-자극 Pak 활성화를 억제합니다. 부분적으로 Pak1 조절 도메인에 공유 결합하여 Pak1 활성화를 억제합니다. 이 화학 물질은 시간 및 온도 의존적으로 Pak1에 공유 결합합니다. Pak1 활성제 Cdc42의 결합을 방지합니다. 이 억제제는 Pak1 자가조절 도메인에 직접 결합합니다. 세포에서 PMA 유도 막 잔물결을 가역적으로 억제합니다.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/18420139/ [2] https://pubmed.ncbi.nlm.nih.gov/19723886/

적용 분야

방법	바이오마커	PMID
Growth inhibition assay	Cell viability	30971268
Western blot	p-PAK1 / PAK1 / p-PAK2 / PAK2 / p-Raf1 / Raf1 / p-MEK1 / MEK1 / p-ERK / ERK	30971268
Immunofluorescence	BiP NF-κB Paxillin	24844382

기술 지원

취급 설명서

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자주 묻는 질문

질문 1:
If this compound is cell membrane permeable, would it be suitable for PAK1 inhibition on a pancreatic beta cell line?

답변:
Based on the reference, this compound is able to penetrate the cell membrane, and it is likely to inhibit PAK1 on a pancreatic beta cell line although there is no reference confirming it: Figure 3: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3963893/; http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4353635/

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

IPA-3 PAK 억제제

화학 구조

분자량: 350.45