연구용
제품 번호S2767
| 세포주 | 분석 유형 | 농도 | 배양 시간 | 제형 | 활성 설명 | PMID |
|---|---|---|---|---|---|---|
| K562 | Function Assay | 10mM | 1h | decreases the expression of LC3-II and the formation of autophagosomes | 21864037 | |
| Jurkat | Function Assay | 10mM | 1h | decreases the expression of LC3-II and the formation of autophagosomes | 21864037 | |
| HeLa | Cytotoxicity Assay | 2mM | 24h | inhibites the cytotoxicity of silibinin to HeLa cells. | 21875385 | |
| PC12/TetOn | Function Assay | 0.1/1mM | 18h | leads to α-syn(WT) accumulation, toxicity, and oligomer formation | 21906659 | |
| RMPI8226 | Function Assay | 5mM | 1h | suppresses the level of autophagy under nutrient depletion | 21915620 | |
| MCF-7 | Function Assay | 10mM | 48h | blocks autophagy induced by bortezomib | 21931937 | |
| HBx | Apoptosis Assay | 10mM | 48h | DMSO | increases cell death | 22020078 |
| Marc-145 | Function Assay | 5mM | 12/24/36h | reduces the PRRSV titers and the protein expression | 22119900 | |
| U937 | Function Assay | 2mM | 12h | decreases the autophagy ratio | 22155150 | |
| BGC-823 | Function Assay | 5mM | 2h | inhibits the rate of autophagic cells | 22322152 | |
| A549 | Function Assay | 0.1mM | 24h | suppresses SU11274-induced cell death | 22466960 | |
| pDCs | Function Assay | 10mM | 0.5h | reduces the induction of IFN-α by ssRNA40 | 22396599 | |
| HeLa | Apoptosis Assay | 5mM | 24h | induces caspase-dependent cell death | 22545128 | |
| U251 | Apoptosis Assay | 5mM | 24h | increases S1-induced cell death | 22579788 | |
| MCF-7 | Apoptosis Assay | 0.1mM | 6h | enhances sirtinol-induced apoptosis | 22751989 | |
| PC-3 | Apoptosis Assay | 2mM | 2h | increases ORI-induced cell death | 22745580 | |
| HCT116 | Apoptosis Assay | 5mM | 24h | DMSO | enhances apigenin-induced cell death | 24626522 |
| U2OS | Growth Inhibition Assay | 10mM | 24h | intensifies the growth inhibition induced by Dox | 24639013 | |
| A2780cp | Apoptosis Assay | 2.5mM | 1h | ddH2O | enhances cisplatin-induced cell death | 24817946 |
| HepG2 | Function Assay | 5mM | 4h | increases cellular levels of HL | 24713587 | |
| Microglia | Apoptosis Assay | 5mM | 24h | decreases hypoxia-induced cell death | 24818601 | |
| MDA-MB 231 | Apoptosis Assay | 5mM | 0.5h | modulates Tocomin® induced apoptosis | 24830781 | |
| PANC-1 | Apoptosis Assay | 1mM | 48h | DMSO | enhances bortezomib-induced cell viability loss | 24842158 |
| MDA-MB-231 | Function Assay | 2mM | 48h | promotes TM-induced cell death | 24970676 | |
| MDA-MB-231 | Function Assay | 2mM | 24h | inhibits autophagy induced by TM | 24970676 | |
| MCF-7 | Function Assay | 2mM | 48h | promotes TM-induced cell death | 24970676 | |
| MCF-7 | Function Assay | 2mM | 24h | inhibits autophagy induced by TM | 24970676 | |
| HepG2 | Apoptosis Assay | 3mM | 5h | reduces cell apoptosis induced by QDs | 22836595 | |
| HeLa | Apoptosis Assay | 10mM | 2h | decreases cell viability co-treatment with PEI | 23000135 | |
| SK-HEP-1 | Apoptosis Assay | 10mM | 1h | protects against autophagy and induces apoptosis in bufalin-treated cells | 22858649 | |
| MDA-MB231 | Function Assay | 5mM | 1h | increases resveratrol-mediated caspase activation and cell death | 23088850 | |
| PaCa44 | Apoptosis Assay | 2.5mM | 1h | reduces genipin-mediated apoptosis | 23124112 | |
| T-47D | Function Assay | 10mM | 2h | inhibits autophagy process and increases rapamycin induced apoptosis | 23300026 | |
| GTL-16 | Apoptosis Assay | 5mM | 24h | reduces cell viability as compared to cells treated with MET inhibitors | 23313490 | |
| U251MG | Function Assay | 3mM | 1h | suppresses LC3-II protein expression | 23338618 | |
| T24 | Function Assay | 10mM | 1h | reduces the cleavage of LC3 after baicalin treatment | 23354080 | |
| HUVECs | Function Assay | 3mM | 24h | blocks the protective effect of resveratrol by inhibiting autophagy | 23358928 | |
| MCF-7 | Function Assay | 5mM | 24h | inhibits starvation-induced autophagy | 23395679 | |
| Hela | Function Assay | 5mM | 24h | inhibits starvation-induced autophagy | 23395679 | |
| OR6 | Function Assay | 10mM | 72h | suppresses HCV replication and formation of autophagosomes | 23395875 | |
| HT-29 | Function Assay | 1mM | 48/96h | inhibits AMPK induces autophagic cell death | 23508272 | |
| SH-SY5Y | Cytotoxicity Assay | 5mM | 24h | increases PCN toxicity | 23525265 | |
| Saos-2 | Apoptosis Assay | 1mM | 96h | increases cell death induced by PCX | 23563171 | |
| 1321N1 | Cytotoxicity Assay | 5mM | 24h | protects cell against PCN-induced toxicity | 23525265 | |
| A2780 | Apoptosis Assay | 5mM | 24h | converts FTY720 with CDDP into an additive effect towards killing ovarian cancer cells | 23592281 | |
| OV2008 | Apoptosis Assay | 5mM | 24h | converts FTY720 with CDDP into an additive effect towards killing ovarian cancer cells | 23592281 | |
| PC12 | Function Assay | 10mM | 24h | water | inhibits chymotrypsin-like proteasomal activity. | 23603979 |
| SH-SY5Y | Apoptosis Assay | 5mM | 1h | abolishes celastrol neuroprotective effect | 23619395 | |
| SH-SY5Y | Function Assay | 1mM | 24h | inhibits the autophagy induced by TOCP | 23743148 | |
| HepG2 | Function Assay | 10mM | 24h | inhibits siTIGAR- and HBSS-induced autophagy | 23817040 | |
| HeLa | Function Assay | 10mM | 2h | suppresses LC3 II expressison | 23864738 | |
| HONE-1 | Function Assay | 5mM | 1h | represses 6r-mediated ROS production | 23892358 | |
| MCF7 | Function Assay | 5mM | 24h | increases CuO induced cell death | 23962629 | |
| HO8910 | Apoptosis Assay | 10mM | 12h | enhances B19-induced apoptosi | 23983610 | |
| SMMC-7721 | Apoptosis Assay | 5mM | 24h | attenuates TNF-α protection against serum starvation-mediated apoptosis | 24066693 | |
| Hep3B | Apoptosis Assay | 5mM | 24h | attenuates TNF-α protection against serum starvation-mediated apoptosis | 24066693 | |
| H460 | Function Assay | 10mM | 4h | increases cisplatin-induced cell death | 24173208 | |
| A549 | Function Assay | 10mM | 4h | inhibits autophagy induced by irradiation | 24142735 | |
| H1299 | Function Assay | 10mM | 4h | increases cisplatin-induced cell death | 24173208 | |
| WiDr | Function Assay | 10mM | 1h | inhibits PCBL-induced LC3 II expression | 24190489 | |
| LoVo | Apoptosis Assay | 5mM | 48h | enhances DCA-induced apoptosis. | 24201812 | |
| HepG2 E47 | Function Assay | 2.5mM | 48h | increases the toxicity of AA, BSO, and CCl4 | 24273738 | |
| RKO | Function Assay | 2mM | 1h | DMSO | enhances cell death by geldanamycin | 24291777 |
| Hep3B | Apoptosis Assay | 2mM | 12h | DMSO | inhibits AZD8055-induced cell death | 24297300 |
| ACHN-5968 | Apoptosis Assay | 5mM | 3h | enhances paclitaxel-mediated apoptosis | 24305604 | |
| Huh7 | Apoptosis Assay | 2mM | 12h | DMSO | inhibits AZD8055-induced cell death | 24297300 |
| UOK257 | Apoptosis Assay | 5mM | 3h | enhances paclitaxel-mediated apoptosis | 24305604 | |
| ECSCs | Apoptosis Assay | 10mM | 4h | decreases rapamycin-treated apoptosis | 24319109 | |
| MCF-7 | Function Assay | 10mM | 24h | inhibits the autophagy induced by chemotherapy drugs | 24315578 | |
| SGC-7901 | Apoptosis Assay | 2mM | 1h | increases CA-4 induced apoptosis | 24321340 | |
| SMMC-7721 | Apoptosis Assay | 2mM | 1h | increases CA-4 induced apoptosis | 24321340 | |
| T24 | Apoptosis Assay | 5mM | 1.5h | potentiates celecoxib-induced apoptosis | 24349176 | |
| NTUB1 | Apoptosis Assay | 5mM | 1.5h | potentiates celecoxib-induced apoptosis | 24349176 | |
| MG-63 | Apoptosis Assay | 10mM | 12h | enhances DP-induced apoptosis | 24358301 | |
| MG-63 | Apoptosis Assay | 0.5/1mM | 32h | enhances salinomycin-induced cell apoptosis | 24358342 | |
| MG-63 | Function Assay | 0.5/1mM | 48h | induces salinomycin-induced cell viability loss | 24358342 | |
| U2OS | Function Assay | 0.5/1mM | 48h | induces salinomycin-induced cell viability loss | 24358342 | |
| HGC-27 | Function Assay | 10mM | 1h | inhibits the cell viability loss by RAD001 or MK-2206 | 24416349 | |
| HCT116 | Apoptosis Assay | 5mM | 24h | enhances the apoptosis induced by apigenin | 24626522 | |
| A549 | Apoptosis Assay | 10mM | 48h | accelerates the reduction of cell viability induced by PTX | 24626722 | |
| Saos-2 | Apoptosis Assay | 10mM | 24h | intensifies the growth inhibition of the U2OS cells induced by Dox | 24639013 | |
| U2OS | Apoptosis Assay | 10mM | 24h | intensifies the growth inhibition of the U2OS cells induced by Dox | 24639013 | |
| HepG2 | Function Assay | 5mM | 4h | increases HL release | 24713587 | |
| A549 | Apoptosis Assay | 5mM | 48h | decreases the percentage of cell death and expression levels of caspase-3, Beclin-1 and LC3-II | 24706303 | |
| A2780cp | Apoptosis Assay | 2.5mM | 1h | ddH2O | enhances cisplatin-induced cell death | 24817946 |
| Microglia | Apoptosis Assay | 5mM | 24h | decreases hypoxia-induced cell death | 24818601 | |
| HT-29 | Apoptosis Assay | 1mM | 48h | DMSO | enhances bortezomib-induced cell viability loss | 24842158 |
| MDR | Apoptosis Assay | 10mM | 6h | strengthens the power of anticancer drugs | 25019701 | |
| H157 | Function Assay | 5mM | 2h | suppresses SPC induced accumulation of LC3-II | 25285628 | |
| A549 | Function Assay | 5mM | 2h | suppresses SPC induced accumulation of LC3-II | 25285628 | |
| A2780cp | Growth Inhibition Assay | 1mM | 1h | increases cisplatin-induced cell death | 25322694 | |
| NBL-W-S | Apoptosis Assay | 1mM | 6h | increases cell apoptosis induced by GANT-61 | 25323222 | |
| NBL-W-S | Growth Inhibition Assay | 1mM | 6h | enhances GANT-61 toxicity | 25323222 | |
| A549 | Apoptosis Assay | 5mM | 2h | DMSO | inhibits BDMC-induced apoptotic cell death | 25716561 |
| 95D | Apoptosis Assay | 5mM | 2h | DMSO | inhibits BDMC-induced apoptotic cell death | 25716561 |
| A549 | Growth Inhibition Assay | 3mM | 2h | DMSO | reduces growth inhibitory effect of BDMC | 25716561 |
| 95D | Growth Inhibition Assay | 3mM | 2h | DMSO | reduces growth inhibitory effect of BDMC | 25716561 |
| Nara-H | Growth Inhibition Assay | 5mM | 48h | enhances temsirolimusmediated suppression of Nara-H cell proliferation | 21805033 | |
| HUVECs | Function Assay | 10mM | 0.5h | decreases the AGE-BSAinduced autophagy leve | 21468592 | |
| HepG2 | Apoptosis Assay | 2mM | 1h | enhances radiation-induced cell death | 21453691 | |
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 29435139 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | |||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | |||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | |||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | |||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | |||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | |||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | |||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | |||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | |||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | |||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | |||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 29435139 | |||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | |||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | |||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | |||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | |||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | |||
| 클릭하여 더 많은 세포주 실험 데이터 보기 | ||||||
| 분자량 | 149.15 | 화학식 | C6H7N5 |
보관 (수령일로부터) | 3 years -20°C powder |
|---|---|---|---|---|---|
| CAS 번호 | 5142-23-4 | SDF 다운로드 | 원액 보관 | 용액은 불안정합니다. 신선하게 준비하거나 소량의 사전 포장된 크기를 구매하십시오. 수령 즉시 재포장하십시오. | |
| 동의어 | NSC 66389 | Smiles | CN1C=NC(=N)C2=C1N=CN2 | ||
|
In vitro |
DMSO
: 10 mg/mL
(67.04 mM)
50°C 수조에서 가온;
초음파 처리;
Ethanol : 10 mg/mL Water : 4 mg/mL |
|
In vivo |
|||||
1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)
2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)
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.
| Targets/IC50/Ki |
Autophagy
Vps34
(HeLa cells) 25 μM
PI3Kγ
(HeLa cells) 60 μM
|
|---|---|
| 시험관 내(In vitro) |
3-Methyladenine (3-MA)에 의한 Vps34 예방에 대한 약간의 선호도는 아마도 Vps34에 특이적인 소수성 고리에서 비롯되며, 이 고리는 이 화합물의 3-메틸기를 둘러쌉니다. 정상 및 기아 조건 모두에서 암세포 사멸을 유발하는 것으로 보고되었으며, Autophagy 억제 능력과 독립적으로 세포 이동 및 침습을 억제할 수 있어 Autophagy 억제 외의 기능을 가지고 있음을 시사합니다. 이 화합물은 Autophagy 억제와 무관한 카스파제 의존적 세포 사멸을 유발합니다. 5mM로 처리하면 GFP-LC3 점을 나타내는 포도당 결핍 HeLa 세포의 비율이 23%로 감소합니다. 3-MA로 처리된 세포에서는 12시간에서 48시간 사이에 LC3-I 수치가 증가하고 LC3-II 수치가 감소합니다. LC3-I에서 LC3-II로의 전환은 이 화합물에 의해 억제됩니다. HeLa 세포를 2.5mM 또는 5mM로 하루 동안 처리해도 세포 생존력에 영향을 미치지 않지만, 10mM로 하루 동안 처리하면 세포 생존력이 25.0% 감소합니다. 세포를 2.5, 5 또는 10mM로 이틀 동안 처리하면 각각 11.5%, 38.0%, 79.4%의 생존력 감소를 유발합니다. 이는 시간 및 용량 의존적으로 세포 생존력을 감소시키고, 노코다졸 유도 전중기 정지 기간을 유의하게 단축시킵니다. 3-MA에 의한 Autophagy 억제는 SU11274 유도 세포 사멸을 억제합니다. 장기간 처리(최대 9시간)하면 야생형 MEF에서 상당한 LC3 I에서 II로의 전환을 유도합니다. 3-MA에 의한 장기간 처리(wortmannin 제외)는 GFP-LC3 점/응집을 현저하게 증가시킵니다. 이 유도 LC3 전환 및 유리 GFP 방출은 ATG7 의존적입니다. 처리하면 p62 단백질 수준이 분명히 증가합니다. 이 화합물은 Atg5−/− MEF 및 DOX 매개 ATG5 결실 세포에서도 p62 수준을 증가시킵니다. 이는 클래스 I 및 클래스 III PI3K를 다른 시간적 패턴으로 억제합니다. 이 유도 LC3 I에서 LC3 II로의 전환은 야생형 세포에 비해 Tsc2−/− 세포에서 극적으로 손상됩니다. 이 화합물은 mTOR 복합체 1의 항-Autophagy 기능을 방해합니다. |
| 키나아제 분석 |
단백질 분해 분석
|
|
HeLa 세포는 24시간 동안 0.05 mCi/mL l-[U- 14C]발린으로 방사선 표지됩니다. 표지 기간이 끝난 후, 세포는 PBS로 세 번 헹궈집니다. 세포는 10mM 3-Methyladenine (3-MA)의 존재 유무와 관계없이 완전 배지 또는 EBSS에서 지정된 시간 동안 배양됩니다.
|
|
| 생체 내(In vivo) |
3-Methyladenine (3-MA)은 클래스 III PI3K에 대한 영향을 통해 Autophagy를 차단합니다. 이 화합물로 처리해도 지주막하 출혈(SAH) 그룹과 비교하여 출혈 정도를 변경하지 않습니다. 전처리하면 SAH + vehicle 그룹과 비교하여 신경학적 증상이 유의하게 악화됩니다. Autophagy는 적용 시 감소합니다. 반대로, SAH + 3-MA 그룹에서는 절단된 카스파제-3이 현저하게 상향 조절됩니다. 절단된 카스파제-3 발현의 상향 조절과 일치하게, SAH + 3-MA 그룹에서는 SAH + vehicle 그룹과 비교하여 오른쪽 피질의 TUNEL 양성 세포 수가 유의하게 증가했습니다. |
참조 |
|
| 방법 | 바이오마커 | 이미지 | PMID |
|---|---|---|---|
| Western blot | α-SMA / TGF-β / LC-3BI / LC-3B II / Beclin-1 / NF-κB p65 caspase-3 / caspase-9 / PARP VEGF APP / BACE1 / ADAM17 / Presenilin 1 / Presenilin 2 / Nicastrin / APH-1 / Pen-2 / LC3-1 / LC3-2 |
|
29296191 |
| Immunofluorescence | LC3 / Hif-α / COX2 |
|
29039446 |
| Growth inhibition assay | Cell viability |
|
26934124 |
질문 1:
I'm also wondering whether it can be dissolved in water, or maybe something like culture medium, normal saline solution to form 10mM solution.
답변:
As the reference (http://www.plosone.org/article/info%3Adoi%2F10.1371%2Fjournal. pone.0035665), it was found to inhibit autophagy at concentrations ranging from 1 to 10 mM and was directly dissolved into the culture medium at the indicated concentrations. And we tested the solubility of S2767, and found its solubility in DMEM is 31 mg/mL at about 40°C.