Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T18787 |
TD-165
|
Others; Ligand for E3 Ligase | Others; PROTAC |
TD-165 是一种基于 PROTAC 技术的 CRBN 降解剂。它包括一个 CRBN 配体结合基团,一个 linker 和一个 VHL 结合基团。 | |||
T8763 |
PTGR2-IN-1
PTGR2-IN-22 |
Others | Others |
PTGR2-IN-1 是有效的 PTGR2抑制剂,IC50为 ~0.7 μM。它能够提高转染 PTGR2 的 HEK293T 细胞 15-keto-PGE2 依赖的 PPARγ 转录活性。 | |||
T23389 |
SR1664
SR 1664 |
PPAR | DNA Damage/DNA Repair; Metabolism |
SR1664 是一种PPARγ拮抗剂,与结合PPARγ,可有效抑制 Cdk5 介导的PPARγ磷酸化,IC50为80 nM,Ki 为 28.67 nM。 | |||
T7802 |
M1001
|
HIF/HIF Prolyl-Hydroxylase; HIF | Angiogenesis; Chromatin/Epigenetic; Metabolism |
M1001 是较弱的HIF-2α激动剂,直接与 HIF-2α PAS-B 结构域结合,Kd=667 nM,能够提高 HIF-2α-ARNT 复合体之间的稳定性。 | |||
T9853 |
STING activator Compound 53
|
STING | Immunology/Inflammation |
基于 oxindole 核心结构的 STING activator Compound 53 在永生化细胞和原代细胞中表现出强大的 STING(人 EC50 185 nM)的靶向功能激活以及与 STING 激活一致的细胞因子诱导指纹。 | |||
T2345 |
PTC-209
PTC209,PTC 209 |
BMI-1; Autophagy | Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
PTC-209 是特定的BMI-1抑制剂,不可逆转地损害结直肠癌起始细胞,在 HEK293T 细胞系中的IC50为 0.5 μM。它有抗骨髓瘤活性并损害肿瘤微环境。 | |||
T7416 |
WS-12
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
WS-12 是有效的TRPM8激动剂,EC50为 39 nM。 | |||
T19459 |
N1-Methylpseudouridine
N1-甲基-假尿苷,1-Methylpseudouridine |
Others | Others |
N1-Methylpseudouridine (1-Methylpseudouridine) 是一种甲基假尿苷,翻译性能比 5 mC 和 5 mC/N1-Methylpseudouridine 高。通过提高核糖体密度,mRNA 中的 N1-Methylpseudouridine 以 eIF2α 依赖性和独立机制增强翻译。 | |||
T22372 |
MYF-01-37
1-[3-Methyl-3-[3-(trifluoromethyl)anilino]pyrrolidin-1-yl]prop-2-en-1-one |
Others; YAP | Others; Stem Cells |
MYF-01-37 (1-[3-Methyl-3-[3-(trifluoromethyl)anilino]pyrrolidin-1-yl]prop-2-en-1-one) 是共价TEAD 抑制剂,靶向 Cys380,能够可逆地抑制 YAP/TEAD 相互作用。 | |||
T6178 |
PTC-209 hydrobromide
PTC-209 HBr |
BMI-1; Autophagy | Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
PTC-209 hydrobromide (PTC-209 HBr) 是一种特定的BMI-1抑制剂,能不可逆转地损害结直肠癌起始细胞,也可损害肿瘤微环境,有抗骨髓瘤活性。它在 HEK293T 细胞系中的IC50为 0.5 μM。 | |||
T7506 |
Yoda 1
|
Piezo Channel | Membrane transporter/Ion channel |
Yoda 1 是Piezo1激动剂,能够激活纯化的 Piezo1 通道。 | |||
T7329 |
C-178
|
STING | Immunology/Inflammation |
C-178 是 STING 选择性共价抑制剂,与 Cys91 结合抑制小鼠中由不同的激活剂引起的 STING 反应。 | |||
T37587 |
ML 209
|
ROR | Metabolism |
ML-209 是一种视黄酸相关的孤儿受体 RORγ 拮抗剂 (IC50= 1.1 μM)。ML-209 抑制 HEK293t 细胞中 RORγt 转录活性(IC50= 300 nM)。ML-209 不抑制细胞中 RORα。ML-209 对鼠 Th17 细胞分化具有选择性抑制,而不影响幼稚 CD4+ T 细胞分化为 Th1 和调节性 T 细胞。 | |||
T14084 |
ABL127
|
Others | Others |
ABL127 is a selective and covalent inhibitor of protein methylesterase 1 (PME-1). In HEK293T and MDA-MB-231 cells, the IC50s values are 6.4 nM and 4.2 nM , respectively. | |||
T36976 | SGC 6870 | ||
Potent and selective protein arginine methyltransferase 6 (PRMT6) inhibitor (IC50 = 77 nM). Exhibits selectivity over all other PRMTs and 23 methyltransferases. In HEK293T cells overexpressing PRMT6, inhibits asymmetric dimethylation of H3R2 (IC50 = 0.8 μM) Negative control SGC 6870N (Cat. No. 7184) also available. | |||
T60524 | HIF-1α-IN-4 | ||
HIF-1α-IN-4 是 HIF-1α抑制剂,在 HEK293T 细胞中的IC50值为 24 nM,具有潜在的抗肿瘤作用。 HIF-1α-IN-4 在缺氧条件下下调 VEGF 和 PDK1 mRNA 的表达。 | |||
T75948 |
K-(D-1-Nal)-FwLL-NH2 TFA
|
||
K-(D-1-Nal)-FwLL-NH2 TFA is a potent and high-affinity inverse agonist of the ghrelin receptor, exhibiting Ki values of 4.9 nM in COS7 cells and 31 nM in HEK293T cells. This compound effectively inhibits ghrelin receptor-mediated Gq- and G13-dependent signaling pathways. | |||
T36799 | UNC 2399 | ||
Biotinylated UNC 1999 (Cat.No. 4904, IC50 = 17 nM). Enriches lysine methyltransferase EZH2 from HEK293T cells. Negative control also avilable. 0 | |||
T61702 | SRI-37240 | ||
SRI-37240 is a powerful inhibitor of premature termination codons (PTCs). It effectively suppresses CFTR nonsense mutations and induces changes in cellular translation termination at PTCs in HEK293T cells. Additionally, when combined with G418, SRI-37240 restores CFTR function in primary bronchial epithelial cells [1]. | |||
TP1894 |
K-(D-1-Nal)-FwLL-NH2
|
||
High affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). Blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways. | |||
T80174 |
BmP02
|
Potassium Channel | Membrane transporter/Ion channel |
BmP02是源自中国蝎(Buthus martensi Karsch)毒液的化合物,功能为选择性Kv1.3通道阻断剂及对Kv4.2具有高选择性的调节剂。该化合物能够在HEK293T细胞中延缓Kv4.2的失活过程,EC50值约为850 nM。此外,BmP02能抑制心室肌细胞中的瞬时外向钾电流(Ito)。 | |||
T80457 |
ω-Conotoxin Bu8
|
Calcium Channel | Membrane transporter/Ion channel; Metabolism |
ω-Conotoxin Bu8为含25个氨基酸残基和3个二硫键的ω-芋螺毒素。该化合物能选择性地抑制HEK293T细胞内表达的大鼠CaV2.2介导的Ba2+去极化激活电流,表现出高效的IC50值为89 nM。 | |||
T38146 |
Chloroguanabenz (acetate)
|
||
Chloroguanabenz is an antiprion agent and a derivative of the α2-adrenergic receptor agonist guanabenz . It inhibits prion formation in yeast and mammalian cell-based assays. Chloroguanabenz reduces the levels of both soluble and aggregated forms of the truncated Huntingtin derivative Htt48 in an HEK293T cellular model of Huntington's disease. | |||
T36942 |
SSAA09E1
SSAA09E1 |
||
SSAA09E1 is an inhibitor of severe acute respiratory syndrome coronavirus (SARS-CoV) viral entry.1It reduces infection of HEK293T cells transiently transfected with angiotensin-converting enzyme 2 (ACE2) by an HIV-based virus system pseudotyped with SARS-CoV surface glycoprotein (EC50= 6.7 μM). SSAA09E1 also inhibits the proteolytic activity of cathepsin L (IC50= 5.33 μM) but not cathepsin B when used at a concentration of 20 μM. 1.() | |||
T60532 | HIF-1α-IN-5 | ||
HIF-1α-IN-5 是 HIF-1α的抑制剂,在 HEK293T 细胞中的 IC50值为 24 nM,也可抑制 MAO-A 的活性。 在缺氧条件下, HIF-1α-IN-5可下调 VEGF 和 PDK1 mRNA 的表达。HIF-1α-IN-5 具有用于癌症研究的潜力。 | |||
T36740 | Guanosine 5’-diphosphate (sodium salt hydrate) | ||
Guanosine 5’-diphosphate (GDP) is a purine nucleotide and biosynthetic precursor of guanosine 5’-triphosphate .1It has been used to study the conformations of GTPases.2GDP (100 μM) activates sulfonylurea receptor 2B (SUR2B) linked to the inward-rectifier potassium channel 6.1 (Kir6.1) in HEK293T cells in a patch-clamp assay.3 1.Berg, J.M., Tymoczko, J.L., and Stryer, L.Biochemistry(2002) 2.Vetter, I.R., and Wittinghofer, A.The guanine nucleotide-binding switch in three dimensionsScience294(5545)... | |||
T37414 |
CAY10771
|
||
CAY10771 is a dual agonist of farnesoid X receptor (FXR) and peroxisome proliferator-activated receptor δ (PPARδ).1It activates FXR and PPARδ in reporter assays using HEK293T cells (EC50s = 0.94 and 1.5 μM, respectively) and is selective for these receptors over retinoic acid receptor α (RARα), retinoid X receptor α (RXRα), PPARα, PPARγ, and liver X receptor α (LXRα) at 10 μM. 1.Schierle, S., Neumann, S., Heitel, P., et al.Design and structural optimization of dual FXR/PPARδ activatorsJ. Med. Ch... | |||
T36275 |
xStAx-VHLL
|
||
Selective peptide-based β-catenin Degrader. Comprises a β-catenin-targeted stapled peptide, xStAx, linked to a VHL-binding peptide. Reduces β-catenin levels in HEK293T cells and colorectal cancer cell lines. Selectively degrades β-catenin over other Wnt signaling pathway components. Inhibits tumor growth in APCmin/+ mice, with constitutively active Wnt signaling, and reduces survival of patient-derived colorectal cancer cell organoids. | |||
T35541 |
Lipoxygenin
|
||
Lipoxygenin is an inhibitor of 5-lipoxygenase (5-LO) with an IC50value of 5 μM for inhibition of 5-LO product synthesis in isolated human granulocytes stimulated with the cation ionophore A23187 .1It inhibits hedgehog-dependent signaling in Shh-LIGHT2 cells and TGF-β-, activin A-, bone morphogenic protein (BMP)-, or Wnt-dependent signaling in HEK293T cells (IC50s = 9.3, 3.2, 8.2, 9.6, and 3.7 μM, respectively, in luciferase reporter assays). Lipoxygenin (5 and 10 μM) increases levels of troponin... | |||
T36998 |
7β,27-dihydroxy Cholesterol
7β,27-DHC,7β,27-dihydroxy Cholesterol |
||
7β,27-dihydroxy Cholesterol is an oxysterol and agonist of retinoic acid receptor-related orphan receptor γ (RORγ) and RORγt. [1] It activates RORγ- or RORγt-dependent signaling with EC50 values of 691 and 1,045 nM, respectively, in reporter assays using HEK293T cells expressing the recombinant human receptors. 7β,27-dihydroxy Cholesterol is selective for RORγ and RORγt over a panel of eight additional nuclear receptors at 30 µM. It increases IL-17A production in Th17-polarized isolated hum... | |||
T37447 |
UZH1
UZH1 |
||
UZH1 is a racemate of UZH1a and UZH1b. UZH1a is a potent and selective METTL3 inhibitor, with an IC50 of 280 nM. UZH1b (IC50=28 μM) is essentially inactive. UZH1 can be used for epitranscriptomic modulation of cellular processes. UZH1 has antitumor activity. UZH1 also can be used as a chemical probe for studying METTL3[1]. UZH1a (2.5-160 μM; 72 h) inhibits the growth of MOLM-13, HEK293T, and U2Os cells, with IC50s of 11 μM, 67 μM, and 87 μM, respectively[1].UZH1b (2.5-160 μM; 72 h) inhibits the ... | |||
T35773 |
Gliotoxin-13C13
Gliotoxin-13C13 |
||
Gliotoxin-13C13is intended for use as an internal standard for the quantification of gliotoxin by GC- or LC-MS. Gliotoxin is an immunosuppressive mycotoxin produced by pathogenic strains ofAspergillusand other fungi with diverse biological activities.1,2,3,4,5,6,7,8It inhibits 20S proteasomal chymotrypsin activity (IC50= 10 μM), blocking the degradation of IκBα and preventing the activation of NF-κB.2,3Gliotoxin induces apoptosis in monocytes and dendritic cells and reduces phagocytosis by neutr... | |||
T83676 |
Tianeptine Metabolite MC5 sodium
|
||
Tianeptine metabolite MC5是一种来自非典型抗抑郁化合物tianeptine的活性代谢物,通过β-氧化形成。此代谢物在使用表达人类μ-阿片受体(MOR)而非人类δ-阿片受体(DOR;EC50s = 0.454和 >100 µM, 分别)的HEK293T细胞进行的生物发光共振能量转移(BRET)试验中,特异性诱导G蛋白激活。在野生型小鼠上,30 mg/kg剂量的Tianeptine metabolite MC5可减少强迫游泳测试中的静止时间,但在MOR敲除小鼠中则不会,表明其具有MOR依赖的抗抑郁样活性。 | |||
T35817 |
Photoswitchable PAD Inhibitor (technical grade)
|
||
Photoswitchable PAD inhibitor is a photoactivated protein arginine deiminase (PAD) inhibitor and a derivative of BB-Cl-amidine that contains an azobenzene photoswitch allowing optical control of PAD activity.1 Without photoactivation, it is a weak inhibitor of PAD2 (IC50 = >100 μM) and is less potent than BB-Cl-amidine in inhibiting citrulline production in vitro (kinact/KIs = 2,300, 600, 1,000, and 10,510 M-1min-1 for PAD1-4, respectively) and does not inhibit histone H3 citrullination in HEK29... | |||
T83769 |
TC 14012 hydrochloride
H-Arg-Arg-Nal-Cys-Tyr-Cit-Lys-D-Cit-Pro-Tyr-Arg-Cit-Cys-Arg-NH2 |
||
TC 14012是一种化学肽模拟的拮抗剂,针对趋化因子(C-X-C motif)受体4(CXCR4;IC50 = 2.9 nM)和CXCR7激动剂。它能在表达CXCR7的HEK293T细胞中诱导β-arrestin招募(EC50 = 350 nM)。TC 14012可减少HIV在MT-4细胞中的细胞病理效应(EC50 = 0.4 nM),并以CXCR4依赖的方式抑制HIV在体外进入(IC50 = 19.3 nM)。它还能抑制由趋化因子(C-X-C motif)配体12(CXCL12)在MDA-MB-231乳腺癌细胞和人脐静脉内皮细胞(HUVECs)中诱导的迁移,当使用浓度范围从10到1,000 nM时。在通过左前降(LAD)冠状动脉结扎诱导的急性心肌梗死小鼠模型中,TC 14012(10 mg/kg)能减少梗死面积。 |