49
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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T11014 |
DFP00173
|
Aquaporin | Membrane transporter/Ion channel |
DFP00173 是一种aquaporin-3 (AQP3)的选择性抑制剂。它对 AQP3 的选择性高于同源 AQP 亚型 AQP7 和 AQP9。它能够抑制小鼠和人 AQP3,IC50值为 ~0.1-0.4 μM。 | |||
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。 | |||
T8806 |
Fluzoparib
HS10160,SHR3162,氟唑帕利 |
PARP | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Fluzoparib (SHR3162) 是口服活性 PARP1抑制剂,IC50为1.46±0.72 nM,在体内具有良好的药代动力学特性,具有抗肿瘤活性,可用于癌症研究。它选择性地抑制同源重组修复(HR) 缺陷细胞的增殖,并使 HR 缺陷细胞对细胞毒性药物敏感。 | |||
T2276 |
RI-1
RI-1; 3-氯-1-(3,4-二氯苯基)-4-(4-吗啉基)-1H-吡咯-2,5-二酮,RI1,RAD51 inhibitor 1 |
DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
RI-1 (RAD51 inhibitor 1) 是一种选择性 RAD51的抑制剂,IC50值为 5-30 μM,可以破坏人类细胞中的同源重组。它在半胱氨酸 319 处与 RAD51 蛋白表面共价结合,并通过直接结合到 RAD51 细丝中蛋白质亚基之间的界面的蛋白质表面来灭活 RAD51。 | |||
T31409 |
DFHO
|
||
DFHO 是一种激发后可散发黄色荧光的 Corn 同源配体,用于活细胞中 RNA 的成像。 | |||
T8880 |
PFM01
|
Others | Others |
PFM01 是 MRE11核酸内切酶抑制剂,是 N-烷基化的 Mirin 衍生物。它可以通过非同源末端连接 (NHEJ) 和同源重组 (HR) 调节双链断裂修复 (DSBR)。 | |||
T2628 |
RI-2
|
DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
RI-2 是一种可逆的RAD51抑制剂,IC50值为 44.17 μM,可抑制人体细胞中的同源重组修复。 | |||
T63427 |
NRX-103094
NRX103094,NRX 103094 |
Wnt/beta-catenin | Cytoskeletal Signaling; Stem Cells |
NRX-103094 是一种有效的 β-catenin 与 同源 E3 ligase SCFβ-TrCP 的相互作用增强剂,可增强 pSer33/Ser37 β-catenin 与 β-TrCP 的亲和力,EC50 为 62 nM,Kd 为 0.6 nM。 | |||
T6960L |
PU-H71 HCl
PU-H71 HCl(873436-91-0 Free base),Zelavespib HCl |
HSP; DNA/RNA Synthesis | Cell Cycle/Checkpoint; Cytoskeletal Signaling; DNA Damage/DNA Repair; Metabolism |
PU-H71 HCl (Zelavespib HCl) 是一种新型Hsp90抑制剂,是一种新型嘌呤基类似物,也是一种可能是CIRT的一种有前途的放射增敏剂。PU-H71 HCL 在许多恶性肿瘤临床前模型中显示出抗肿瘤活性。PU-H71 HCL 对 Rad51 和Ku70 的蛋白表达水平有抑制作用,这可能与双链断裂修复的同源重组途径和非同源末端连接途径有关。 | |||
T23840 |
BUR1
BMP upregulator-1,1-{1-苯基-1H-吡唑并[3,4-D]嘧啶-4-基}哌啶,BMP upregulator 1,BUR 1,BUR-1 |
CDK | Cell Cycle/Checkpoint |
BUR1 是一种酿酒酵母细胞周期蛋白依赖性激酶 (CDK),与在转录延伸中起作用的哺乳动物 Cdk9 同源。 | |||
T63730 |
NRX-103095
|
Wnt/beta-catenin | Cytoskeletal Signaling; Stem Cells |
NRX-103095 是一种有效的 β-catenin 与 同源 E3 ligase SCFβ-TrCP 的相互作用增强剂,增强 pSer33/Ser37 β-catenin 与 β-TrCP 的亲和力,EC50 为 163 nM。 | |||
T23974 |
DDRI-18
DDRI18,DDRI 18 |
DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
DDRI-18 是一种调节 DNA 损伤反应的新型小分子抑制剂,具有增敏活性和抗癌活性,抑制非同源末端连接 (NHEJ) DNA 修复过程,增强抗癌 DNA 损伤化合物的细胞毒性作用。 | |||
T8637 |
DMNB
6-Nitroveratraldehyde,6-硝基藜芦醛 |
DNA-PK | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
DMNB (6-Nitroveratraldehyde) 可用于合成no-carrier-added 6-[18F]fluoro-L-DOPA (6-FDOPA)。它可用于研究多巴胺能系统的PET。 | |||
T4339 |
YU238259
|
DNA-PK; Others | DNA Damage/DNA Repair; Others; PI3K/Akt/mTOR signaling |
YU238259 是一种新型的同源依赖性 DNA 修复 (HDR) 抑制剂,在基于细胞的 GFP 报告基因检测中不抑制非同源末端连接 (NHEJ),可研究癌症。 | |||
T14565 |
BI-671800
AP-761,Cmpd A |
GPR; Prostaglandin Receptor | Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation |
BI-671800 (AP-761) 是高特异性的前列腺素 D2 受体拮抗剂,对哮喘有研究潜力,对人和小鼠 CRTH2 转染细胞中 PGD2 结合 CRTH2 的 IC50值分别为 4.5 和 3.7 nM。 | |||
T10981 |
DCZ0415
|
Apoptosis; Others; NF-κB | Apoptosis; NF-κB; Others |
DCZ0415 在体外、体内和耐药性骨髓瘤患者的原代细胞中诱导抗骨髓瘤活性。它是一种 TRIP13 抑制剂,可损害非同源末端连接的修复并抑制 NF-κB 活性。 | |||
TQ0232 |
UNC0646
UNC 0646 |
Histone Methyltransferase | Chromatin/Epigenetic |
UNC0646 是一种有效的、选择性的同源蛋白赖氨酸甲基转移酶 G9a 和 GLP 抑制剂,IC50分别为 6 和 15 nM,对 G9a/GLP 的选择性比 SETD7、SUV39H2、SETD8 和 PRMT3 高。它降低 MDA-MB-231 细胞中H3K9me2的水平,IC50为 26 nM。 | |||
TP1120L |
IRBP acetate(211426-18-5 free base)
Interphotoreceptor Retinoid Binding Protein Fragment IRBP |
Others | Others |
IRBP acetate(211426-18-5 free base) (Interphotoreceptor Retinoid Binding Protein Fragment IRBP) 是一种含有 20 个残基的肽,是一种主要的致病表位。它存在于间质视觉色素结合蛋白肽(IRBP 161-180)的第一个同源重复序列中,可诱导葡萄膜炎后(EAU)。 | |||
T83976 |
ARB-272572 hydrochloride
ARB-272572 hydrochloride(2368182-63-0 Free base) |
PD-1/PD-L1 | Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation |
ARB-272572 hydrochloride 是一种小分子 PD-L1 抑制剂,对PD-1/PD-L1 HTRF的 IC50 值为 400 pM。ARB-272572 hydrochloride 通过诱导 PD-L1 蛋白同源相互作用来抑制 PD-1/PD-L1 细胞信号传导。 | |||
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。 | |||
T11067 |
VX-984
M9831 |
DNA-PK | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
VX-984 (M9831) 是一种可口服的、具有选择性的的、可透过血脑屏障的 DNA-PK 抑制剂。VX-984 对非同源性末端 NHEJ 的接合具有抑制作用,可作用于 DSBs 使 DNA 双链断裂。VX-984常见于对胶质母细胞瘤 (GBM) 和非小细胞肺癌 (NSC-LC) 的研究。 | |||
T4567 |
Sulfaphenazole
Plisulfan,Raziosulfa,Depocid,磺胺苯吡唑,Depotsulfonamide |
P450; Antibacterial | Metabolism; Microbiology/Virology |
Sulfaphenazole (Plisulfan) 是一种 CYP2C9的特异性抑制剂,抑制 CYP2C9介导的亚油酸动脉粥样硬化和促炎症效应,增加 AP-1的氧化应激和激活。 | |||
T63516 |
NRX-252114
NRX252114,NRX 252114 |
Wnt/beta-catenin | Cytoskeletal Signaling; Stem Cells |
NRX-252114 (NRX252114) 能够诱导突变体 β-catenin 的降解。NRX-252114 是一种 β-catenin 与 同源 E3 ligase SCFβ-TrCP 的相互作用的高效增强剂,能够加强 pSer33/S37A β-catenin 与 β-TrCP 的结合,EC50 为 6.5 nM,Kd 为 0.4 nM。 | |||
T33546 |
Mytilus scp
Mytilus small cardioactive peptide |
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Mytilus scp isolated from Mytilus edulis is homologous to small cardioactive peptides from Aplysia. | |||
T68398 |
MI-223
|
||
MI-223 is an inhibitor of Mcl-1-stimulated homologous recombination (HR) DNA repair, which leads to sensitization of cancer cells to hydroxyurea- or olaparib-induced DNA replication stress. | |||
T40980 |
Palmitic acid-13C2
Palmitic acid-13C2 |
||
Palmitic acid-13C2 is the 13C-labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells. | |||
T40141 |
Palmitic acid-13C16 sodium
Palmitic acid-13C16 sodium |
||
Palmitic acid-13C16 sodium, a 13C-labeled form of the naturally occurring saturated fatty acid Palmitic acid sodium, is prevalent in animals and plants. This compound can trigger the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in mouse granulosa cells. | |||
TP1120 |
Interphotoreceptor Retinoid Binding Protein Fragment (IRBP)
IRBP,Interphotoreceptor Retinoid Binding Protein Fragment IRBP |
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Interphotoreceptor Retinoid Binding Protein Fragment (IRBP) is a 20-residue peptide, which is a major pathogenic epitope. It exists in the first homologous repeat of interstitial visual pigment Binding Protein peptide (IRBP 161-180) and can induce post-uv | |||
T80902 |
Umesolerbart
|
||
Umesolerbart (REGN5714) 是一种特异性针对Bet v1的mAb。它能结合于桤木科植物、榛树和鹅耳枥相关的同源过敏原。 | |||
T63846 |
Gefapixant citrate
|
||
Gefapixant citrate 是口服具有活力的 P2X3 受体 (P2X3R) 拮抗剂,能够作用于人同源重组 hP2X3 (IC50: ~30 nM)和 hP2X2/3 (IC50: 100-200 nM)。Gefapixant citrate 能够用于研究慢性咳嗽与膝骨关节炎。 | |||
T76399 |
PKI(5-22)amide
|
||
PKI(5-22)amide 是环 AMP 依赖性蛋白激酶 (PKA) 抑制剂的活性片段。PKI(5-22)amide 抑制PKA 激活,但不能减弱 CRF1 受体的同源脱敏作用。 | |||
T39423 |
Palmitic acid-13C sodium
|
||
Sodium palmitate-13C is the 13C-labeled variant of palmitic acid, a long-chain saturated fatty acid prevalent in animals and plants. This compound has been shown to induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer-binding protein homologous protein (CHOP) in mouse granulosa cells. | |||
T74501 | NHEJ inhibitor-1 | ||
NHEJ inhibitor-1 (Compound C2) 是一种三功能 Pt(II) 复合物,可缓解非同源末端连接 (NHEJ)/同源重组 (HR) 相关的双链断裂 (DSB) 修复,从而避免非小细胞肺对顺铂的耐药性。NHEJ inhibitor-1 抑制损伤修复蛋白 Ku70 和 Rad51,从而使肿瘤对活性分子重新敏感。NHEJ inhibitor-1 还诱导 ROS 产生和MMP 降低。 | |||
T62184 |
NRX-2663
|
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NRX-2663 是一种 β-catenin 与同源 E3 ligaseSCFβ-TrCP 的相互作用增强剂,对β-catenin 与 β-TrCP 的结合具有增强作用 (Kd: 54.8 nM, EC50: 22.9 nM)。 | |||
T36435 |
SP 10
|
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Peptide originally derived from SARS-CoV Spike (S) protein; corresponds to amino acid residues 668 to 679. Highly potent inhibitor of SARS-CoV S protein and ACE2 interaction (IC50 = 1.88 nM in biochemical assay). Inhibits interaction of SARS-CoV S protein and Vero E6 cells in vitro. Please note, this peptide displays 80% sequence identity to homologous site on SARS-CoV-2 S-protein (residues 689-697). | |||
T36046 |
LH1306
|
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LH1306 is an inhibitor of the interaction between programmed cell death 1 (PD-1) and its ligand PD-L1 that has an IC50 value of 25 nM in a homologous time-resolved fluorescence (HTRF) assay.1 It increases the activation of Jurkat cells expressing PD-1 in co-culture with U2OS or CHO cells expressing PD-L1 (EC50s = 334 and 4,214 nM, respectively, in reporter assays). |1. Basu, S., Yang, J., Xu, B., et al. Design, synthesis, evaluation, and structural studies of C2-symmetric small molecule inhibito... | |||
T78970 |
Antitumor agent-96
|
Apoptosis | Apoptosis |
Antitumor agent-96 (Compound D34) 为一种有效的MRE11抑制剂,能够结合MRE11并通过抑制其内切酶功能来下调HR通路,进而诱导CM细胞的凋亡(apoptosis)。 | |||
T10890 | CRTh2 antagonist 3 | Others | Others |
CRTh2 antagonist 3 is a powerful chemokine receptor homologous molecule expressed on Th2 cell (CRTh2) antagonists. CRTh2 antagonist 3 enhanced the activity of PDK1 on short peptide substrates with EC50 of 2 μM and Kd of 8.4 μM. CRTh2 antagonist 3 has the | |||
T80024 |
Cationic Bovine Serum Albumin
cBSA, chemically modified cationic bovine serum albumin |
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Cationic Bovine Serum Albumin(带正电荷的牛血清白蛋白)是由583个氨基酸组成的蛋白质,具有三个同源的全α结构域。该蛋白质与Tanshinone IIA联用,在缺血性脑卒中中展现出显著的神经保护作用。 | |||
T36703 |
CAY10760
|
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CAY10760 is an inhibitor of the protein-protein interaction between RAD51 recombinase and BRCA2 (EC50= 19 μM in a cell-free competitive ELISA).1It decreases homologous recombination by 54% in wild-typeBRCA2-expressing BxPC-3 pancreatic cancer cells when used at a concentration of 20 μM. CAY10760 (20 μM) decreases proliferation of BxPC-3, as well as mutantBRCA2-expressing Capan-1, cancer cells when used alone or in combination with the poly(ADP-ribose) polymerase (PARP) inhibitor olaparib . 1.Bag... | |||
T28536 |
RI(dl)-2 TFA
RI(dl)-2 |
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RI(dl)-2 TFA 是一种有效的选择性 RAD51 介导的 D 环形成 (RAD51-mediated D-loop formation) 抑制剂,IC50为 11.1 μM,并抑制人细胞中的同源重组 (HR) 活性,IC50为 3.0 μM。 | |||
T36047 |
LH1307
|
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LH1307 is an inhibitor of the interaction between programmed cell death 1 (PD-1) and its ligand PD-L1 that has an IC50 value of 3 nM in a homologous time-resolved fluorescence (HTRF) assay.1 It increases the activation of Jurkat cells expressing PD-1 in co-culture with U2OS or CHO cells expressing PD-L1 (EC50s = 79 and 763 nM, respectively, in reporter assays). |1. Basu, S., Yang, J., Xu, B., et al. Design, synthesis, evaluation, and structural studies of C2-symmetric small molecule inhibitors o... | |||
T72560 | Antitumor agent-81 | ||
Antitumor agent-81 (化合物 5 a) 是一种低细胞毒性的 P62-RNF168激动剂,能促进 P62与RNF168的相互作用。Antitumor agent-81 诱导RNF168介导的H2A 泛素化减少,并损害同源重组介导的 DNA 修复。Antitumor agent-81 还能以剂量依赖的方式抑制小鼠异种移植肿瘤的生长。 | |||
T82631 |
Cys-Gly-Tyr-Gly-Pro-Lys-Lys-Lys-Arg-Lys-Val-Gly-Gly
|
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Cys-Gly-Tyr-Gly-Pro-Lys-Lys-Lys-Arg-Lys-Val-Gly-Gly 是一种含有 13 个氨基酸残基的合成多肽,其中 7 个氨基酸与 SV40 T 抗原具有同源性。该多肽具备诱导核转运的能力。 | |||
T36034 | CAY10774 | ||
CAY10774 is an inhibitor of the protein-protein interaction between programmed cell death 1 (PD-1) and its ligand PD-L1 (IC50= 15 nM in a homologous time-resolved fret (HTRF) assay).1It increases the activation of Jurkat cells expressing PD-1 in co-culture with artificial antigen-presenting cells (aAPCs) expressing PD-L1 (EC50= 6.6 μM in a reporter assay). CAY10774 increases surface expression of PD-1 on primary human CD4+and CD8+T cells co-cultured with aAPCs. 1.Konieczny, M., Musielak, B., Koc... | |||
T79925 |
T4 UvsX Recombinase
|
DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
T4 UvsX Recombinase 促进双链DNA模板上DNA复制的启动,通过催化模板DNA与同源单链DNA引物间的突触形成。此酶显著增强了T4 DNA聚合酶全酶在线性单链DNA模板上进行的回跳(发夹引物)DNA合成反应。 | |||
T82847 |
BNP (1-21), Pro (Human)
|
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BNP (1-21), Pro (Human) 是一种由21个氨基酸组成的心脏激素多肽。作为B型利钠肽(BNP)的一部分,与心房利钠肽高度同源,共同构成了心脏的双利钠肽系统。BNP 主要参与心脏发生的调节,并涉及向子宫外环境过渡的生理进程。 | |||
T36570 |
KUS121
|
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KUS121 is a valosin-containing protein (VCP) modulator that inhibits VCP ATPase activity (IC50= 330 nM).1It inhibits cell death, ATP depletion, and upregulation of C/EBP-homologous protein (CHOP) induced by tunicamycin, an inducer of ER stress, in HeLa cells when used at concentrations of 20, 50, and 50 μM, respectively. KUS121 (100 μM) inhibits ATP depletion and cell death induced by oxygen-glucose deprivation (OGD) in rat primary cortical neurons in anin vitromodel of cerebral ischemia.2It red... | |||
T83854 |
BRC4wt TFA
|
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BRC4wt是一种从人类BRCA2的BRC4重复区(1521-1536)衍生而来的乙酰化肽,并且是BRCA2与RAD51之间的蛋白质-蛋白质相互作用的抑制剂。当与阳离子穿膜肽(Arg)9结合时,BRC4wt缩短了体外DNA复制轨迹长度,并降低了由DNA拓扑异构酶I抑制剂坎普特西汀引起的DNA损伤的同源修复频率,同时也增强了聚(ADP-核糖)聚合酶(PARP)抑制剂奥拉帕尼在HeLa人类宫颈癌细胞和U2OS人类骨肉瘤细胞中诱导的细胞死亡,但在非癌症细胞hTERT RPE-1、MRC-5或MCF-10A中则不然。 |
Cat. No. | Product Name | Target | Signaling Pathways |
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TN2444 |
Batatasin IV
山药素IV,山药 |
Others | Others |
Batatasin IV 从 Dioscorea opposita 中鉴定出来,Dioscorea opposita 是一种同源药用植物,通常用作日常生活中的食物。 |