61
10
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T12079 |
ML604440
|
Proteasome | Proteases/Proteasome; Ubiquitination |
ML604440 是一种特异性的、有效的、细胞可渗透的蛋白酶体 β1i (LMP2) 亚基抑制剂,能够破坏 MHC I 类细胞表面表达,IL-6 分泌以及 naïve T helper 向 17 T helper 细胞的分化。它可以改善实验性结肠炎和 EAE 疾病。 | |||
T9756 |
AZD-9574
|
PARP | Chromatin/Epigenetic; DNA Damage/DNA Repair |
AZD-9574 是 SSB 位点的 PARP1 特异性抑制剂。 AZD-9574 具有抗癌活性,可用于 HRD+ 乳腺癌和晚期实体恶性肿瘤的研究。 | |||
T20689 |
Temocaprilat
RNH-5139,RS-5139,RNH 5139,RNH5139,替莫普利,RS5139,RS 5139 |
Angiotensin-converting Enzyme (ACE) | Metabolism |
Temocaprilat (RS5139) 是一种血管紧张素转换酶 (ACE) 抑制剂。 Temocaprilat 通过缺乏 EHBR 的 cMOAT 有效地从胆汁中排泄,而许多其他 ACE 抑制剂对 cMOAT 的亲和力较低。 | |||
T26396 |
6-Hydroxy-DOPA
6-羟基-DL-多巴,6-Hydroxy-DL-DOPA |
DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
6-Hydroxy-DOPA 是 RAD52 的变构抑制剂,可用于癌症研究。它在体外抑制 BRCA 缺陷癌细胞的增殖,也抑制 APE1。 | |||
T69638 |
VT-105
VT 105 |
Others | Others |
VT-105 是一种强效的选择性 TEAD 自棕榈酰化抑制剂,可抑制 NF2 缺陷间皮瘤的增殖和肿瘤生长。 | |||
T76735 |
Mupadolimab
CPI-006 |
CD73 | Immunology/Inflammation |
Mupadolimab (CPI-006) 是一种人源化 FcγR 结合缺陷型 IgG1 抗 CD73抗体,具有潜在的抗癌活性,可激活 CD73POS B 细胞。 | |||
T26326 |
VU0285655-1
VU-0285655,VU0285655,BML 280,VU 0285655,BML280,BML-280 |
TNF; Phospholipase; Interleukin | Apoptosis; Immunology/Inflammation; Metabolism |
VU0285655-1(BML-280) 是一种有效的选择性磷脂酶 D2 (PLD2) 抑制剂,可抑制PLD2 缺陷细胞的增殖。VU0285655-1 对高糖诱导的 caspase-3 裂解和细胞活力降低有抑制作用。VU0285655-1 可用于研究糖尿病视网膜病。 | |||
T11593 |
I-OMe-Tyrphostin AG 538
I-OMe-AG 538 |
IGF-1R; PI3K | PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
I-OMe-Tyrphostin AG 538是一种特异性 IGF-1R 抑制剂和 PI5P4Kα的 ATP 竞争性抑制剂(IC50:1 µM)。I-OMe-Tyrphostin AG 538可抑制 IGF-1R 介导的信号传导,并对营养缺乏的 PANC1细胞具有优先细胞毒性。 | |||
T37558 |
Necrostatin-5
Nec-5 |
RIP kinase; Necroptosis | Apoptosis; NF-κB |
Necrostatin-5 (Nec-5)是一种RIP1激酶的选择性抑制剂,也是一种细胞坏死抑制剂,可防止TNF-α处理的fadd 缺陷Jurkat 细胞死亡,EC50值为240 nM。 | |||
T3424 |
Ezutromid
BMN 195,VOX-C1100,依珠曲米,SMT C1100 |
Others | Others |
Ezutromid (BMN 195) 是一种具有口服活性的、首创的苯并恶唑 utrophin 调节剂,EC50=0.91 μM。它抑制人肝微粒体 CYP1A2 酶活性,IC50=5.4 μM。它可用于 Duchenne 型肌营养不良症 (DMD) 的研究。 | |||
T63228 |
Simmiparib
SMOCL-9112 |
Apoptosis; PARP | Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair |
Simmiparib (SMOCL-9112) 是一种新型有效的 PARP1 和 PARP2 抑制剂,是一种Olaparib 衍生物。Simmiparib 在同源重组修复 (HR) 缺陷细胞中诱导 DNA 双链断裂 (DSB) 和 细胞周期阻滞,从而促使细胞凋亡 (apoptosis)。Simmiparib 可用于研究帕金森病、阿尔茨海默病、乳腺癌和黑色素瘤。 | |||
T36491 |
POMHEX
|
Glucokinase | Metabolism |
Pomhex 是一种具有抗癌活性的细胞渗透性强效烯醇化酶抑制剂,可用于癌症致死率的研究。Pomhex是一种外消旋混合物,是一种强效且具有选择性的ENO2抑制剂。 | |||
T10936 |
D-I03
DI03 |
DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
D-I03 是一种选择性的RAD52 抑制剂,Kd 为 25.8 µM。D-I03 抑制 RAD52 依赖性单链退火 (SSA) 和 D 环形成,IC50 分别为 5 µM 和 8 µM。D-I03 抑制 BRCA1 和 BRCA2 缺陷细胞的生长,并抑制顺铂诱导的 RAD52 病灶形成,但对 RAD51 无影响。 | |||
T9088 |
Topovale
ARC111,ARC 111,ARC-111,Topoval |
Topoisomerase | DNA Damage/DNA Repair |
Topovale (ARC111) 是一种有效的拓扑异构酶 I 抑制剂。Topovale 抑制缺氧介导的缺氧诱导因子 1alpha 的积累。 Topovale 对一组癌细胞表现出低 nM 细胞毒性。与 P388 细胞相比,在 CPT 抗性拓扑异构酶 I (TOP1) 缺陷的 P388/CPT45 细胞中,Topovale 细胞毒性和 Topovale 诱导的细胞凋亡减少了 > 100 倍。 | |||
T9543 |
Syk Inhibitor II hydrochloride
|
Others | Others |
Syk Inhibitor II hydrochloride 信号传导的影响在狼疮中可能很突出。 | |||
T26168 |
Rufigallol
AI3 00865,AI3-00865,AI300865 |
||
Rufigallol (AI3-00865) 是一种具有六个羟基的电子缺失的盘状分子,是诱导非平面AIE 分子形成DLC 的良好单元,是一种蒽醌衍生物。Rufigallol 诱导获得了DLC 特性,而TPE 基团的引入使分子结构在聚集状态下具有良好的荧光。Rufigallol 在体外的显著的协同抗疟作用,在体内与维生素C 和酮类化合物一起使用具有协同作用并显示出抗疟活性。 | |||
T35449 |
α-(difluoromethyl)-DL-Arginine
DFMA,RMI 71897,α-(difluoromethyl)-DL-Arginine |
Others | Others |
α-(difluoromethyl)-DL-Arginine (RMI 71897) 是一种酶激活的、不可逆的大肠杆菌(Ki = 800 μM)、铜绿假单胞菌和肺炎克雷伯菌精氨酸脱羧酶抑制剂。在0.01 mM 时,它已被证明可以防止渗透胁迫诱导的燕麦叶片细胞精氨酸脱羧酶活性和腐胺合成的增加。当α-(difluoromethyl)-DL-Arginine 与多种多胺类似物联用时,能在10 mM 的最低浓度下抑制克氏锥虫在哺乳动物宿主细胞中的生长,并在T 细胞受体α缺陷小鼠模型中阻止小锥虫的生长。 | |||
T71757 | SC-10914 | ||
SC10914 is a highly potent PARP inhibitor (PARP1 IC50 = 7.87 nM) with potent anti-proliferative activity against human BRCA deficient tumor cells (MDA-MB-436, BRCA1 deficient, IC50 = 4.03 nM, Capan-1 BRCA2 deficient, IC50 = 11.66 nM) and PTEN deficient tumor cells (HGC-27,PTEN deficient, IC50 = 0.35 μM). SC10914 showed potent anti-tumor activity in BRCA1/2 mutant tumor models and better pharmacokinetics profile has the potential to be selected as the clinical candidate for the treatment of treat... | |||
TP2228 |
C3bot(154-182)
C3bot (154-182) |
Others | Others |
transferase-deficient neurotrophic fragment of clostridial C3 protein | |||
T33551 |
N(alpha)-Acetylfusarinines
Nalpha-Acetylfusarinines |
||
N(alpha)-Acetylfusarinines is a group of naturally occurring hydroxamic acids produced by unidentified species of Penicillium when grown on iron-deficient media. | |||
T11913 |
LY88074 Methyl ether
|
Others | Others |
LY88074 Methyl ether is effective in inhibiting conditions associated with estrogen deprivation syndrome, such as osteoporosis and hyperlipidemia, which occur due to various estrogen-deficient states. | |||
T69456 |
Melagatran monohydrate
|
||
Melagatran monohydrate is a thrombin inhibitor. Melagatran prevents tissue factor expression in human platelet-monocyte heterotypic complexes. Melagatran reduces advanced atherosclerotic lesion size and may promote plaque stability in apolipoprotein E-deficient mice. | |||
T12203L |
Necrostatin 2
|
Others | Others |
Necrostatin 2 is an effective necroptosis inhibitor. Necrostatin 2 is also a RIPK1 inhibitor. EC50 for inhibition of necroptosis in FADD-deficient Jurkat T cells treated with TNF-α is 0.05 μM. | |||
T68934 | VT101 free base | ||
VT101 is a TEAD Auto-palmitoylation inhibitor that Selectively Inhibit Proliferation and Tumor Growth of NF2-deficient Mesothelioma. VT101 inhibited the firefly luciferase reporter dose-dependently and had no 204 effect on the Renilla luciferase reporter. | |||
T71424 | VT-102 free base | ||
VT-102 is a TEAD Auto-palmitoylation inhibitor that Selectively Inhibit Proliferation and Tumor Growth of NF2-deficient Mesothelioma. VT102 inhibited the firefly luciferase reporter dose-dependently and had no 204 effect on the Renilla luciferase reporter. | |||
T37023 |
MB 0223
|
||
Dynamin-related GTPase DRP1 partial inhibitor (IC50 = 1.2 μM). Selective for DRP1 over other dynamin-related GTPases, OPA1 and DYN1. Increases mitochondrial DNA levels in mfn1- knockout MEFs deficient in mitochondrial fusion. Mallat et al (2018) Discovery and characterization of selective small molecule inhibitors of the mammalian mitochondrial division dynamin, DRP1. Biochem.Biophys.Res.Commun. 499 556 PMID:29601815 | |||
T69955 |
JPI-547 HCl
|
||
JPI 547, also known as NOV 1402, is an oral inhibitor of PARP 1/2 and Tankyrase 1/2. JPI-547 demonstrated anti-tumor activity in BRCA-deficient xenograft models as a single-agent and in combination with chemotherapy and immune checkpoint inhibitors. | |||
TQ0032L |
Rosiptor acetate
AQX-1125,AQX 1125,AQX1125,AQX-1125 acetate |
||
Rosiptor is a potent and selective SHIP1 activator. AQX-1125 inhibits Akt phosphorylation in SHIP1-proficient but not in SHIP1-deficient cells, reduces cytokine production in splenocytes, inhibits the activation of mast cells and inhibits human leukocyte | |||
T40950 |
A3334
|
||
A3051, is a robust and orally active inhibitor of CXXC5-DVL with an IC 50 of 63.06 nM. Its applications include research into phenotypes associated with obesity, diabetes, and NASH that are induced by high fat diet (HFD) and methionine-choline deficient diet (MCD). | |||
T80566 |
Temtokibart
|
||
Temtokibart为一种IgG1λ2抗体,靶向IL22RA1并进行人源化处理,由剔除谷氨酰胺合成酶基因的细胞所表达。 | |||
T79873 |
TNG-462
|
Histone Methyltransferase | Chromatin/Epigenetic |
TNG-462(化合物1143)作为一种口服有效的PRMT5抑制剂,适用于研究MTAP缺失型及/或MTA累积型癌症。 | |||
T61243 |
MAT2A-IN-5
|
||
MAT2A-IN-5, a potent inhibitor of MAT2A, effectively targets the abnormally elevated expression of MAT2A found in various tumor types such as gastric, colon, liver, and pancreatic cancers. By reducing the proliferative activity of MTAP-deficient cancer cells, MAT2A-IN-5 exhibits potential in cancer research applications [1]. | |||
T60639 |
SLEC-11
|
||
SLEC-11 可在E-钙粘蛋白缺陷细胞中作为合成致死(SL)的先导化合物出现,具有治疗胃癌的潜力。 | |||
T61672 | MAT2A-IN-7 | ||
MAT2A-IN-7, a potent inhibitor of the enzyme MAT2A, demonstrates efficacy in targeting the abnormally elevated expression of MAT2A observed in gastric, colon, liver, and pancreatic cancers. Furthermore, MAT2A-IN-7 effectively reduces the proliferative activity specifically in MTAP-deficient cancer cells, thus highlighting its potential for cancer research applications [1]. | |||
T22801 |
GNE-617 hydrochloride (1362154-70-8 free base)
GNE-617 hydrochloride |
Others | Others |
GNE-617 hydrochloride is a potent and competitive inhibitor of nicotinamide phosphoribosyltransferase (IC50: 5nM). GNE-617 hydrochloride reduces the NAD levels in a > 95% reduction in both NAPRT1-deficient and NAPRT1-proficient cell lines and exerts (EC50 | |||
T62910 | Antibacterial agent 62 | ||
Antibacterial agent 62 是一种新型氧化还原循环抗结核化合物,对生长和营养缺乏的表型耐药非生长细菌表现出显著的杀菌作用。 | |||
T71147 | PBS-1086 | ||
PBS-1086 is a novel dual inhibitor of the canonical and noncanonical NF-κB pathways, increasing the magnitude and duration of initial EGFR inhibitor response in multiple NSCLC models, decreasing PDHK1 expression, and suppressing phosphorylation of the PDHK1 protein substrate PDHA1 in a panel of PTEN-deficient cell lines. | |||
T81376 |
PROTAC SMARCA2 degrader-2
|
PROTACs | PROTAC |
PROTACSMARCA2 degrader-2,作为一种高效的SMARCA2/4PROTAC降解剂,在HeLa HiBiT检测中显示出极低的IC50值(<0.1 μΜ)。该化合物对于SMARCA4相关或缺陷癌症研究具有潜在应用价值。 | |||
T62100 |
MAT2A-IN-6
|
||
MAT2A-IN-6 是一种 MAT2A 的有效抑制剂。其中 MAT2A 在几种类型的肿瘤中(包括胃癌、结肠癌、肝癌和胰腺癌)的表达水平异常升高。MAT2A-IN-6 能够减少 MTAP 缺陷癌细胞的增殖活性。MAT2A-IN-6 对癌症疾病表现出潜在的研究价值。 | |||
T63603 |
MAT2A-IN-3
|
||
MAT2A-IN-3 是 MAT2A 的有效抑制剂。其中 MAT2A 的表达水平在包括胃癌、结肠癌、肝癌和胰腺癌在内的几种类型的肿瘤中显著升高。MAT2A-IN-3 能够抑制 MTAP 缺陷型癌细胞的增殖活性。MAT2A-IN-3 对癌症疾病表现出研究潜力。 | |||
T76308 |
Gastric Inhibitory Polypeptide (1-30), porcine
|
||
Gastric Inhibitory Polypeptide (1-30), porcine 缺乏天然胃抑制多肽 (GIP) C 端 12 个氨基酸残基,能够增强胰岛素和生长抑素的释放而发挥生物活性。 | |||
T77973 |
YD23
|
PROTACs | PROTAC |
YD23是一种SMARCA2PROTAC,其作用机理为诱导SMARCA2蛋白的降解。鉴于SMARCA2与SMARCA4具有合成致死关系,YD23进一步能减少多个基因(包涵细胞周期以及细胞生长调控基因)增强子的染色质可及性,特别是在缺乏SMARCA4的细胞中。 | |||
T73023 |
PARP1-IN-12
|
||
PARP1-IN-12 是一种有效的PARP1抑制剂,其IC50值为 2.99 nM。PARP1-IN-12 具有较好的抗癌细胞增殖活性,可诱导细胞凋亡并使细胞周期停滞在 G2/M 期。PARP1-IN-12 能在BRCA 缺陷的细胞中诱导 DNA 双链断裂 (DSBs)。 | |||
T79819 |
AMB639752
|
||
AMB639752为一种高效DGKα抑制剂,能通过抑止整合体内DGKα活性,复原因重复刺激导致的SAP缺失型淋巴细胞的细胞死亡(RICD)。此化合物适合于X连锁淋巴增生性疾病1(XLP-1)的相关研究。 | |||
T81803 |
MFN2 agonist-1
|
||
MFN2 agonist-1 (B-A/l) 是一种有效促进缺陷细胞中MFN2表达的化合物,能够促进线粒体融合。在表达CMT2A突变型MFN2 T105M的小鼠培养神经元中,MFN2 agonist-1能够逆转线粒体的“聚集”现象(指静态线粒体聚集体的形成)并恢复其运动性。 | |||
T62290 | SKLB-197 | ||
SKLB-197 能够作用于 ATR (IC50: 0.013 μM),但对其他 402 种蛋白激酶的活性极弱或无活性。在体外和体内,SKLB-197 对 ATM 缺陷型肿瘤具有显著的抗肿瘤作用。 | |||
T78959 | ATR-IN-23 | ATM/ATR | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
ATR-IN-23 (Compound 34) 是一种选择性ATR抑制剂,其IC50为 1.5 nM。该化合物对LoVo细胞表现出抗增殖活性,并对HT-29细胞产生合成致死效果,适用于研究DNA损伤反应(DDR)缺陷癌症。 | |||
T63975 |
MAT2A-IN-1
|
||
MAT2A-IN-1 是 MAT2A 的有效抑制剂,能够 MTAP 缺陷型癌细胞的增殖活性。其中 MAT2A 在几种类型肿瘤中表达水平异常高,包括胃癌、结肠癌、肝癌和胰腺癌。MAT2A-IN-1 对癌症疾病表现出研究潜力。 | |||
T74743 |
M47
|
||
M47 是一种小分子,可选择性地破坏隐花色素 1 (CRY1) 的稳定性并增加细胞核中 CRY1 的降解。M47 增强Ras 转化的 P53 缺陷小鼠皮肤成纤维细胞系的细胞凋亡,并延长 p53 基因敲除小鼠的寿命。M47 可用于癌症研究。 | |||
T36370 |
4-Methylumbelliferyl-α-L-Iduronide (free acid)
|
||
4-Methylumbelliferyl-α-L-iduronide (free acid) is a fluorogenic substrate for α-L-iduronidase, an enzyme found in cell lysosomes that is involved in the degradation of glycosaminoglycans such as dermatan sulfate and heparin sulfate. 4-Methylumbelliferyl-α-L-iduronide is cleaved by α-L-iduronidase to release the fluorescent moiety 4-methylumbelliferyl (4-MU). 4-MU fluorescence is pH-dependent with excitation maxima of 320 and 360 nm at low (1.97-6.72) and high (7.12-10.3) pH, respectively, and an... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T4886 |
Dihydrouracil
二氢尿嘧啶,5,6-Dihydrouracil |
Endogenous Metabolite | Metabolism |
Dihydrouracil (5,6-Dihydrouracil) 是一种尿嘧啶的代谢产物,能够作为鉴定二氢嘧啶脱氢酶 (DPD) 缺陷的标志物。 | |||
T13482 |
2'-O-Methyladenosine
|
Endogenous Metabolite | Metabolism |
2'-O-Methyladenosine 是甲基化腺嘌呤的残基,在正常人群和腺苷脱氨基酶缺乏病人的尿液中均可被检测到。它显示出独特的降血压活性。 | |||
T4719 |
1,4-D-Gulonolactone
D-Gulonic acid γ-lactone,D-(-)-古洛糖酸-1,4-内酯 |
Others; Endogenous Metabolite | Metabolism; Others |
1,4-D-Gulonolactone (D-Gulonic acid γ-lactone) (也称为还原性抗坏血酸,RAA) 是 L-gulono-1,4-lactone oxidoreductase (EC 1.1.3.8)的底物,催化植物和动物中l -抗坏血酸(维生素C)生物合成的最后一步。enzyme L-Gulono-1,4-lactone oxidase 在容易患坏血病、缺乏维生素c的动物(如人类)中缺失。1,4-D-Gulonolactone 存在于人体血液中,并被用作比较运动引起的氧化应激变化的标志物之一。 | |||
TMA2106 | (-)-Sparteine | P450 | Metabolism |
Sparteine is a class 1a antiarrhythmic agent, a sodium channel blocker. The deficient debrisoquine hydroxylation of Sparteine is due to the absence of P-450IID1 protein in the livers of poor metabolizers. | |||
T62625 |
11-O-Methylpseurotin A
|
||
11-O-Methylpseurotin A为一种(PKS/NRPS)混合聚酮合成酶-非核糖体肽合成酶化合物,其特性为选择性抑制Hof1缺失菌株。 | |||
TN3921 |
Effusanin B
|
Antifection | Microbiology/Virology |
Effusanin B shows antibacterial activity. It exhibits DNA-damaging activity in assay which employes DNA-repair deficient (RAD 52Y) and repair proficient (RAD +) yeast strains. | |||
TN1778 |
Isoformononetin
异刺芒柄花素,黄豆苷元杂质 |
IL Receptor; Antifection | Immunology/Inflammation; Microbiology/Virology |
Isoformononetin shows fungitoxic activity against Cladosporium sphaerospermum; it also has immunomodulatory activity, it inhibits the differentiation of Th17 cells and B-cell lymphopoesis to promote osteogenesis in estrogen-deficient bone loss conditions. | |||
TN3719 |
Cristacarpin
|
p38 MAPK; ROS; CDK; Antifection; p53 | Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation; MAPK; Microbiology/Virology |
Cristacarpin exhibits moderate but selective activity towards DNA repair-deficient yeast mutants. It promotes endoplasmic reticulum (ER) stress, leading to sub-lethal reactive oxygen species (ROS) generation and which eventually terminates by triggering s | |||
TN3920 |
Effusanin A
|
Raf; Antifection | MAPK; Microbiology/Virology |
Effusanin A 是一种存在于Isodon rugosus 之中的天然产物。 它具有 DNA 损伤和抗菌作用。 | |||
TN2945 |
3-Hydroxybakuchiol
|
ATPase; Caspase | Apoptosis; Membrane transporter/Ion channel; Proteases/Proteasome |
3-Hydroxybakuchiol exerts cytotoxic and anti-proliferative effects on the TA3/Ha mouse mammary adenocarcinoma cell line and induces a decrease in the mitochondrial transmembrane potential, the activation of caspase-3, the opening of the mitochondrial perm |