51
6
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T7012 |
VO-Ohpic trihydrate
VO-Ohpic |
PTEN; Autophagy | Autophagy; PI3K/Akt/mTOR signaling |
VO-Ohpic trihydrate (VO-Ohpic) 是一种有效的磷酸酶和张力蛋白同源物(PTEN)抑制剂,IC50 为 35 nM。 | |||
T6667 |
SF1670
PTP CD45 Inhibitor,PTPase CD45 Inhibitor |
Phosphatase; PTEN; Autophagy | Autophagy; Metabolism; PI3K/Akt/mTOR signaling |
SF1670 (PTPase CD45 Inhibitor) 是一种特异性 PTEN 抑制剂,IC50 为 2 μM。 | |||
T12075 |
ML-180
SR1848 |
Others | Others |
ML-180 (SR1848) 是孤儿核受体肝受体同源物 1 (LRH-1;NR5A2) 的反向激动剂(IC50:3.7 µM)。它不抑制类固醇生成因子 1 (SF-1;NR5A1; IC50>10 µM)。 它具有潜在的抗依赖 LRH-1 癌症作用。 | |||
T7953 |
BpV(HOpic)
bpV (HOpic) |
PTEN | PI3K/Akt/mTOR signaling |
BpV(HOpic) (bpV (HOpic)) 是 PTEN 选择性抑制剂,IC50=14 nM。BpV(HOpic) 具有神经保护作用。 | |||
T8954 |
ML179
ML-179 |
Others | Others |
ML179 是一种有效的选择性肝受体同源物 1 (LRH1, NR5A2) 反向激动剂,IC50 为 320 nM。 | |||
T60194 |
N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(N-ethylcyclopropanecarboxamido)-4-methyl-4′-morpholino-[1,1′-biphenyl]-3-carboxamide
|
Histone Methyltransferase | Chromatin/Epigenetic |
N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(N-ethylcyclopropanecarboxamido)-4-methyl-4′-morpholino-[1,1′-biphenyl]-3-carboxamide 是一种强效的、选择性的Enhancer of Zeste Homolog 2 (EZH2),对EZH2 WT 和EZH2-Y641F 的IC50分别为37.6nM 和79.1nM。 | |||
T10087 |
24-Norursodeoxycholic acid
nor-UDCA |
Others | Others |
24-Norursodeoxycholic acid (nor-UDCA) 是一种侧链缩短的 UDCA 的 C23 同系物,表现出有效的抗胆汁淤积,抗炎和抗纤维化活性。 | |||
T6360 |
3-deazaneplanocin A HCl
|
Others; Histone Methyltransferase | Chromatin/Epigenetic; Others |
3-deazaneplanocin A HCl 是组蛋白甲基转移酶 (EZH2) 和 S-腺苷同型半胱氨酸水解酶 (AHCY) 抑制剂。 | |||
TP1936L1 |
RFRP3(human) acetate(311309-27-0 free base)
|
Neuropeptide Y Receptor | GPCR/G Protein; Neuroscience |
RFRP3(human) acetate(311309-27-0 free base) 是一种人类 GnIH 肽同源物,是一种有效的促性腺激素分泌抑制剂,可抑制 Ca2+ 动员。它是一种 NPFF1 受体激动剂,它抑制毛喉素诱导的 cAMP 产生,IC50 为 0.7 nM。 | |||
T64363 |
(Iso)-RJW100
|
Others | Others |
(Iso)-RJW100 是一种有效的肝受体同源物 1 (LRH-1,NR5A2) 和类固醇生成因子-1 (SF-1,NR5A1) 激动剂,pEC50 分别为 6.4 和 7.2。 | |||
T10616 |
BRM/BRG1 ATP Inhibitor-1
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
BRM/BRG1 ATP Inhibitor-1 是变构双 Brahma 同源物 (BRM)/SWI/SNF 相关的基质相关肌动蛋白依赖性调节剂,染色质亚家族 A 成员 2 和 BRG1/SMARCA4 ATP 酶活性抑制剂,IC50值低于 0.005 μM。 | |||
TP1899L1 |
Hemokinin 1 (human) acetate(491851-53-7 free base)
|
Neurokinin receptor | GPCR/G Protein; Neuroscience |
Hemokinin 1 (human) acetate(491851-53-7 free base) 是一种内源性 P 物质同系物,是速激肽 NK1 受体的选择性激动剂(NK1、NK3 和 NK2 受体的 IC50 值分别为 1.8、370 和 480 nM)。在体外对 B 细胞具有增殖和抗凋亡作用,在体内具有抗高血压作用。 | |||
T3352 |
XL413
|
cholecystokinin; Casein Kinase; Pim; CDK | Cell Cycle/Checkpoint; Chromatin/Epigenetic; GPCR/G Protein; JAK/STAT signaling; Metabolism; Stem Cells |
XL413 是一种口服生物可利用的细胞分裂周期 7 同源物 (CDC7) 激酶抑制剂,具有潜在的抗肿瘤活性,IC50值为 3.4 nM。它对 pMCM 的 EC50值为 118 nM,对 CK2 和 PIM1 的 IC50值分别为 215 和 42 nM。 | |||
T38680 |
RJW100
|
Others | Others |
RJW100是一种化合物,作为肝受体同源体1(LRH-1, NR5A2)和类固醇生成因子-1(SF-1, NR5A1)的强效激动剂,分别展现出6.6和7.5的pEC50值。此外,RJW100能强力激活miR-200c(miRNA-200c, microRNA-200c)启动子。 | |||
T29231 |
ZLD1039
ZLD-1039,ZLD 1039 |
Histone Methyltransferase | Chromatin/Epigenetic |
ZLD1039 是一种口服有效的、高选择性 EZH2 抑制剂。ZLD1039 高效抑制 EZH2 野生型及 Y641F 和 A677G 突变型,IC50 分别为 5.6、15 和 4.0 nM。ZLD1039 抑制乳腺肿瘤的生长和转移。 | |||
TP1937L1 |
RFRP-1 (human) acetate(311309-25-8 free base)
|
Neuropeptide Y Receptor | GPCR/G Protein; Neuroscience |
RFRP-1 (human) acetate(311309-25-8 free base) 是一种有效的内源性 NPFF 受体激动剂(NPFF2 和 NPFF1 的 EC50 值分别为 0.0011 和 29 nM)。它减弱离体大鼠和兔心肌细胞的收缩功能。降低心率、每搏输出量、射血分数和心输出量,并增加大鼠的血浆催乳素水平。 GnIH 同系物。 | |||
T34952 |
Trinactin
Akd1D,Akd 1D,Akd-1D |
||
Trinactin is a nonactin homolog that has Immunosuppressive effects. | |||
T22483 |
(±)-Octanoylcarnitine chloride
|
Others | Others |
(±)-Octanoylcarnitine chloride is a homolog of acetylcarnitine chloride. | |||
T12122 | MTH1-IN-2 | MTH1 | DNA Damage/DNA Repair |
MTH1-IN-2 is an inhibitor of MutT homolog 1 (MTH1), with anti-tumor activity. | |||
T70927 |
UCD74A HCl
|
||
UCD74A HCl is a cell impermeant homolog of UCD38B, inhibitor of uPA (urokinase plasminogen activator). | |||
T26605 |
Alyssin
|
||
Alyssin is a sulforaphane homolog and antioxidant. It induces phase II enzymes and increases Nrf2 levels in adenocarcinoma cells. It decreases the metabolism of polycyclic aromatic hydrocarbons, supressing the risk of carcinogenesis in vitro. | |||
T11436 |
GNA002
|
Histone Methyltransferase | Chromatin/Epigenetic |
GNA002 is a highly potent, specific, and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor (IC50: 1.1 μM). | |||
T61963 |
SOS1-IN-3
|
||
SOS1-IN-3 是有效的SOS1抑制剂(IC50=5 nM)。SOS1-IN-3 显示出抗癌活性。 | |||
T70469 |
AK-42
|
||
AK-42 is a novel potent and specific inhibitor of CLC-2, displaying unprecedented selectivity over CLC-1, the closest CLC-2 homolog, and exhibiting no off-target engagement against a panel of 61 common channels, receptors, and transporters expressed in brain tissue. | |||
T70328 |
HDM-201 succinate
|
||
HDM-201 succinate is an orally bioavailable human double minute 2 homolog (HDM2) inhibitor with potential antineoplastic activity. | |||
T6292 |
3-Deazaneplanocin A
|
Histone Methyltransferase | Chromatin/Epigenetic |
3-Deazaneplanocin A 是组蛋白甲基转移酶(EZH2)和 S-腺苷同型半胱氨酸水解酶 (AHCY) 抑制剂。 | |||
T10189 |
7-[4-(2-Piperidinyl)ethoxy]benzoyl Raloxifene
|
Others | Others |
7-[4-(2-Piperidinyl)ethoxy]benzoyl Raloxifene is a liver receptor homolog-1 (LRH-1) antagonist (IC50: 3.1 μM). | |||
T82880 |
Biotin-H10
|
||
Biotin-H10,作为一种特异性抑制剂,针对前梯度蛋白2 (AGR2),其KD值为6.4 nM。此化合物能有效抑制癌细胞活力。 | |||
T26776 |
Berteroin
OR-009512,KB-47947,LP-088984,KB47947,LP088984 |
||
Berteroin is an erucin homolog and potential antioxidant. It is present in cruciferous vegetables, including rucola salad leaves, Chinese cabbage and mustard oil. It decreases the release of pro-inflammatory cytokines in LPS-stimulated macrophages. It als | |||
TP1936 |
RFRP-3(human)
RFRP 3 (human) |
||
Agonist of the NPFF1 receptor (IC50 = 0.7 nM for inhibition of forskolin-induced cAMP production). Homolog of gonadotropin-inhibitory hormone (GnIH); inhibits activity of gonadotropin-releasing hormone (GnRH) neurons. | |||
TP1899 |
Hemokinin 1, human
Hemokinin 1 (human) |
||
Endogenous substance P homolog that is a selective agonist at the tachykinin NK1 receptor (IC50 values are 1.8, 370 and 480 nM for NK1, NK3 and NK2 receptors respectively). Has proliferative and antiapoptotic actions on B-cells in vitro and is antihyperte | |||
T83818 |
Isoguanosine-5'-O-triphosphate sodium
2-Hydroxyadenosine 5’-triphosphate,2-hydroxy ATP,isoGTP |
||
Isoguanosine-5'-O-triphosphate是guanosine 5'-triphosphate(GTP)的一个异构体且是crotonoside的磷酸化形式。与GTP不同,Isoguanosine-5'-O-triphosphate不促进微管组装。在逆转录酶实验中,Isoguanosine-5'-O-triphosphate(2 mM)能抑制转录并诱导T到C的突变。它已被用于确定phosphofructokinase和mutT homolog 1(MTH1)的底物特异性。 | |||
T78292 |
Ifinatamab
Anti-Human B7-H3 |
||
Ifinatamab为一抗人B7同源3蛋白(HumanB7-H3)的单克隆免疫球蛋白G1-kappa,属于糖型α免疫调节剂类。 | |||
T62003 |
SOS1-IN-13
|
||
SOS1-IN-13 是有效的SOS1抑制剂。SOS1-IN-13抑制 SOS1 和 pERK 的IC50分别为 6.5 nM 和 327 nM。SOS1-IN-13 在抗癌研究中具有一定的价值。 | |||
T61723 | SS-RJW100 | ||
SS-RJW100 is an enantiomer of RJW100, known as a racemic agonist that targets two nuclear receptors: liver receptor homolog 1 (LRH-1) and steroidogenic factor 1 (SF-1). In vitro experiments reveal that SS-RJW100 promotes the recruitment of coregulator protein fragments and enhances the interaction with the transcriptional intermediary factor 2 (Tif2) coactivator specifically for LRH-1. Additionally, SS-RJW100 disrupts the allosteric activation networks of LRH-1, displaying suboptimal thermal sta... | |||
T62959 |
LRH-1 modulator-1
|
||
LRH-1 modulator-1 是一种有效的 LRH-1 (肝受体同源物 -1) 调节剂/激动剂。LRH-1 modulator-1 能够诱导抗炎细胞因子 IL-10,对炎症细胞因子 IL-1b 和 TNFa 表现出抑制作用。LRH-1 modulator-1 在肠道类器官中具有抗炎活性。 | |||
T74675 |
MS8815
|
PROTACs | PROTAC |
MS8815 是 zeste 同源物2(EZH2)PROTAC 降解剂,具有选择性。MS8815 对 EZH2有抑制活性,IC50值为 8.6 nM。MS8815 可用于三阴性乳腺癌 (TNBC) 研究。 | |||
TP1937 |
RFRP-1(human)
RFRP-1 (human) |
||
Potent endogenous NPFF receptor agonist (EC50 values are 0.0011 and 29 nM for NPFF2 and NPFF1, respectively). Attenuates contractile function of isolated rat and rabbit cardiac myocytes. Reduces heart rate, stroke volume, ejection fraction and cardiac out | |||
T37422 |
Ras Inhibitory Peptide
|
||
Son of sevenless homolog 1 (Sos1) is a guanine nucleotide exchange factor (GEF) that directs the exchange of Ras-GDP to Ras-GTP by binding to SH3 domains of the growth factor receptor-bound protein 2 (Grb2), leading to the activation of ERK. Ras inhibitory peptide is a synthetic peptide that contains the sequence PVPPR, which corresponds to a region within human Sos1 that interacts with an SH3 domain of Grb2. It specifically blocks the interaction of the GEF with Grb2, preventing an interaction ... | |||
T35477 | BSJ-Bump | ||
Negative control for BSJ-03-123 . Displays binding and no degradation of Cdk6 in vitro. Brand et al (2019) Homolog-selective degradation as a strategy to probe the function of CDK6 in AML. Cell Chem.Biol. 26 300 PMID:30595531 | |||
T63273 |
KU-177
|
||
KU-177 是一种有效的 Hsp90ATP 酶同系物 1 (Aha1) 抑制剂,能够消融 Aha1 驱动的 Hsp90 依赖性 tau 聚集增强。KU-177 能够阻碍 Aha1/Hsp90 相互作用,其IC50 值为 4.08 μM,但对Hsp90的再折叠荧光素酶的能力不造成影响。KU-177 可以阻碍癌细胞生长,诱导其凋亡 (apoptosis),能够用于研究 Tau 病。 | |||
T37234 |
(±)14(15)-EpETE
|
||
EDHF (endothelium-derived hyperpolarizing factor) is an unidentified mediator released from vascular endothelial cells in response to acetylcholine and bradykinin which is distinct from the NOS- (nitric oxide) and COX-derived (prostacyclin) vasodilators. Cytochrome P450 (CYP450) metabolism of polyunsaturated fatty acids, produces epoxides such as (±)14(15)-EpETrE which are prime candidates for the actual active mediator. However, the CYP450 metabolites of eicosapentaenoic acid and docosahexaenoi... | |||
T75866 |
RFRP-3(human) TFA
|
||
RFRP-3 (Neuropeptide VF(124-131))(human) TFA,一种人 GnIH 肽同源物,是一种促性腺激素分泌抑制 Ca2+动员的有效抑制剂。RFRP-3(human) TFA 是一种NPFF1受体激动剂,它抑制 forskolin 诱导的 cAMP 生成的 IC50值为 0.7 nM。 | |||
T73231 |
RR-RJW100
|
||
RR-RJW100是RJW100的对映异构体之一,后者为核受体肝受体同源物1(LRH-1)和类固醇生成因子1(SF-1)的激动剂。相比于另一对映异构体SS-RJW100,RR-RJW100展现出更强的LRH-1激活能力。此化合物在调节代谢稳态方面具有潜力,因而在糖尿病、肝病以及炎症性肠病等疾病的研究中有所应用。 | |||
T37235 |
(±)16(17)-EpDPA
(±)16,17-EpDPE,(±)16,17 EDP,(±)16,17-epoxy Docosapentaenoic Acid,(±)16,17-epoxy DPA,(±)16(17)-EpDPA |
||
EDHF (endothelium-derived hyperpolarizing factor) is an unidentified mediator released from vascular endothelial cells in response to acetylcholine and bradykinin which is distinct from the NOS- (nitric oxide) and COX-derived (prostacyclin) vasodilators.[1],[2]Cytochrome P450 (CYP450) metabolism of polyunsaturated fatty acids produces epoxides such as (±)14(15)-EET which are prime candidates for the actual active mediator.[3] However, the CYP450 metabolites of eicosapentaenoic acid and docosahex... | |||
T14925 |
Cenisertib
AS-703569,R-763 |
Akt; Bcr-Abl; STAT | Angiogenesis; Cytoskeletal Signaling; JAK/STAT signaling; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors |
Cenisertib 是一种有效的 ATP 竞争性的多激酶抑制剂,对 Aurora-kinase-A/B,ABL1,AKT,STAT5, FLT3 的活性具有抑制作用,对FER 及其同源物的激酶也显示出抑制作用。Cenisertib 通过抑制肿瘤肥大细胞 (MC) 中几种不同分子靶标的活性抑制其生长,也抑制异种移植模型中胰腺癌,乳腺癌,结肠癌,卵巢癌和肺癌以及白血病的肿瘤生长。 | |||
T38028 |
(R)-(+)-Docosahexaenyl-1'-Hydroxy-2'-Propylamide
|
||
N-Acyl ethanolamines (NAEs) have diverse biological actions that are strongly affected by the associated acyl group. Docosahexaenoyl ethanolamide (DHEA) has potential signaling roles in cancer, inflammation, and neurological development and functioning. At least some of DHEA's effects are mediated through cannabinoid (CB) receptors, while some NAEs also act as vanilloid receptor agonists and voltage-gated K+ channel blockers. (R)-(+)-Docosahexaenyl-1'-hydroxy-2'-propylamide is a homolog of DHEA,... | |||
T35812 |
CAY10591
CAY10591 |
||
Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). Human SIRT1 is the homolog of yeast silent information regulator 2 (Sir2) and has been shown to regulate the activity of the p53 tumor suppressor and inhibit apoptosis. Small molecule activators of SIRT1, such as resveratrol, extend lifespan in yeast and C. elegans in a manner that resembles caloric restriction. CAY10591 has been identified as an activator of the enzyme SIRT1. This com... | |||
T65598 | Cefminox sodium | ||
Cefminox (Sodium) is a new cephamycin antibiotic possessing a D-amino acid moiety derived from D-cysteine at the C-7B side chain. Cefminox is active against a wide range of bacteria, especially Gram-negative and anaerobic bacteria. Cefminox shows excellent in vivo efficacy (ED50) which is higher than would be expected from its in vitro activity (MIC). Moreover, cefminox possesses more potent activity in suppression of bacterial regrowth than other cephems[1]. Cefminox (Sodium) was the most activ... | |||
T37743 |
N-octadecanoyl-L-Homoserine lactone
|
||
Quorum sensing is a regulatory system used by bacteria for controlling gene expression in response to increasing cell density. This regulatory process manifests itself with a variety of phenotypes including biofilm formation and virulence factor production. Coordinated gene expression is achieved by the production, release, and detection of small diffusible signal molecules called autoinducers. The N-acylated homoserine lactones (AHLs) comprise one such class of autoinducers, each of which gener... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6S2116 |
Ginkgolic acid C17:1
银杏酸 C17:1,银杏酸C17:1 |
Phosphatase; PTEN | Metabolism; PI3K/Akt/mTOR signaling |
Ginkgolic acid C17:1 是分离自银杏叶中,通过诱导PTEN 和SHP-1酪氨酸磷酸酶抑制组成型和诱导型 STAT3 活化。它具有抗癌活性。 | |||
TN1362 |
Afzelin
阿福豆苷,Kaempferol-3-O-rhamnoside |
PTEN; p38 MAPK; TNF; Mitochondrial Metabolism; Antibacterial; Prostaglandin Receptor; Autophagy | Apoptosis; Autophagy; GPCR/G Protein; Immunology/Inflammation; MAPK; Metabolism; Microbiology/Virology; PI3K/Akt/mTOR signaling |
Afzelin (Kaempferol-3-O-rhamnoside) 具有多种细胞活性,例如 DNA 保护、抗菌、抗氧化和抗炎以及 UV 吸收活性,并且可以通过 UV 吸收和细胞活性的组合保护人体皮肤免受 UVB 引起的损伤。 Afzelin 减轻线粒体损伤,增强线粒体生物合成并降低线粒体自噬相关蛋白、parkin 和 putative kinase 1 的水平。 | |||
T3780 |
Oroxin B
Hypocretin-2,木蝴蝶苷B |
Apoptosis; PTEN; Antioxidant; PI3K; Autophagy | Apoptosis; Autophagy; oxidation-reduction; PI3K/Akt/mTOR signaling |
Oroxin B (Hypocretin-2) 是从传统中草药木蝴蝶中分离出来的黄酮类天然产物,在恶性淋巴瘤细胞中诱导肿瘤抑制性 ER 应激。它通过上调 PTEN,下调 COX-2,VEGF,PI3K 和 p-AKT,对肝癌细胞具有明显的抑制作用,诱导细胞早期凋亡。 | |||
T2S1635 |
3-Isomangostin
|
MTH1 | DNA Damage/DNA Repair |
3-Isomangostin 可从莽吉柿壳中提取的一种天然产物,是一种乙酰胆碱酯酶选择性抑制剂,也是一种有效的人醛糖还原酶抑制剂,IC50 为 3.48 uM。它抑制 MutT 同源物 1 (MTH1),IC50 为 52 nM。它具有清除自由基、抗疟原虫和抗癌的活性。 | |||
T25827 |
Monactin
|
||
Monactin is a Marcrotetrolide antibiotic produced by cycloheximide producing species of Streptomyces. It is a homolog of nonactin from the same species. | |||
T19128 | 3-Pyridineacetic acid | Others | Others |
3-Pyridineacetic acid is a homolog of nicotinic acid, a breakdown product of nicotine and other tobacco alkaloids. |