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연구용

RGFP966 HDAC3 inhibitor

제품 번호: S7229

RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC.
RGFP966 HDAC inhibitor Chemical Structure

화학 구조

분자량: 362.4

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품질 관리 (Quality Control)

배치: 순도: 99.74%
99.74

함께 자주 사용되는 제품 RGFP966

Tubastatin A

It and Tubastatin A decrease total HDAC activity in HLMVEC and reduce the inflammatory and hyper-permeability response to LPS in mice.

(+)-JQ1

It and JQ1 dramatically reduces tumor volume and growth rate and suppresses tumor growth via induction of apoptosis in the glioma xenograft mouse model.

Trichostatin A (TSA)

It and Trichostatin A increase the expression of AKAP12 at both the mRNA and protein levels.

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
APL cells Function assay ≤2 μM 48 h DMSO RGFP966 did not induce apoptosis in APL cells but did reduce clonogenicity and increased maturation. 26447190
Em-Myc lymphoma cells Function assay ≤1 μM 48 h DMSO Cell proliferated significantly more slowly than vehicle-treated controls in the presence or absence of pro-survival BCL-2 overexpression 26447190
HH and Hut78 cells Proliferation assay 10 μM 0, 24, 48, 72 h DMSO Both cell lines were sensitive to treatment with 10 μM 966. However, Hut78 cells exhibited a greater sensitivity than HH cells. 23894374
HH Function assay 10 μM 24 h DMSO increases the acetylation at H3K9/K14, H3K27, and H4K5 23894374
Hut78 Function assay 10 μM 24 h DMSO increases the acetylation at H3K9/K14, H3K27, and H4K5 23894374
HL60 Antiproliferative assay 48 hrs Antiproliferative activity against human HL60 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 1.64 μM. 29940115
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 1.64 μM. 29940115
HEL Antiproliferative assay 48 hrs Antiproliferative activity against human HEL cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 1.64 μM. 29940115
HL60 Antiproliferative assay 48 hrs Antiproliferative activity against human HL60 cells after 48 hrs by CCK-8 assay, IC50 = 21.71 μM. 29940115
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by CCK-8 assay, IC50 = 21.71 μM. 29940115
HEL Antiproliferative assay 48 hrs Antiproliferative activity against human HEL cells after 48 hrs by CCK-8 assay, IC50 = 21.71 μM. 29940115
Sf9 Function assay 60 mins Inhibition of full length human C-terminal His-tagged HDAC3/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in baculovirus infected Sf9 insect cells using substrate measured after 60 mins by colorimetric method 29541372
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 362.4 화학식

C21H19FN4O

 보관 (수령일로부터)
CAS 번호 1396841-57-8 SDF 다운로드 원액 보관

동의어 N/A Smiles C1=CC=C(C=C1)C=CCN2C=C(C=N2)C=CC(=O)NC3=C(C=C(C=C3)F)N

용해도 (Solubility)

In vitro
배치:

DMSO : 72 mg/mL (198.67 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

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

mg/kg g μL

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 (Mechanism of Action)

Targets/IC50/Ki
HDAC3
(Cell-free assay)
80 nM
시험관 내(In vitro)
RGFP966 is a slow-on/slow-off, competitive tight-binding HDAC inhibitor, with an IC50 of 0.08μM for HDAC3 and no effective inhibition of any other HDAC at concentrations up to 15μM. This compound treatment on two CTCL cell lines for 24 hours prior to western blot analysis resulted in increased acetylation at H3K9/K14, H3K27, and H4K5, but not H3K56ac. It decreases cell growth in CTCL (cutaneous T cell lymphoma) cell lines due to increased apoptosis that is associated with DNA damage and impaired S phase progression. This chemical causes a significant reduction in DNA replication fork velocity within the first hour of drug treatment.
키나아제 분석
Deacetylation assays
Deacetylation assays are based on the homogenous fluorescence release assay. Purified recombinant enzymes are incubated with serial-diluted inhibitors at the concentrations indicated in the figures, with pre-incubation times ranging from 0 to 3 hours, in the standard HDAC buffer. Acetyl-Lys(Ac)-AMC substrate (at 10 μM, corresponding to the Km for both HDAC1 and HDAC3) is added after the pre-incubation period. The reaction is allowed to run for 1 hour. The trypsin peptidase developer, at final concentration of 5mg/ml, is added after 1 hour, and the fluorescence emission is then measured using a Tecan M200 96-well plate reader.
생체 내(In vivo)
RGFP966 treatment (10 mg/kg) enhances long-term memory for object memory. This compound (3 or 10 mg/kg, s.c.) facilitates extinction and prevents reinstatement of cocaine- conditioned place preference.
참조

적용 분야 (Applications)

방법 바이오마커 이미지 PMID
Western blot p-STAT3 / Acetyl-STAT3 / STAT3 / Ac-H3 / Ac-H4 H3K9K14ac / H3 / H3K56ac / H3K27ac / H4K5ac
S7229-WB1
28338101

자주 묻는 질문 (Frequently Asked Questions)

질문 1:
Does this product S7229 specifically inhibit HDAC3? Or does it target other HDACs as well?

답변:
In the paper, it is indicated that "this compound is specific for HDAC3, with an IC50 of 0.08 μM and no effective inhibition of any other HDAC at concentrations up to 15 μM." However, we did not perform experiment to confirm this data. Please refer to the following link for detailed information: http://www.pnas.org/content/110/7/2647.long