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T79717mHTT-IN-2;化合物 mHTT-IN-2mHTT-IN-2
mHTT-IN-2 (compound 27) is a potent inhibitor of mutant huntingtin protein (mHTT), with an EC50 value of 0.066 μM. It specifically modulates the splicing of HTT RNA exons [49-50], acting as a splicing regulator for the HTT gene. Demonstrating inhibitory effects both in vitro and in vivo, mHTT-IN-2 has been tested in human HD stem cells and mouse BACHD models. Additionally, it is applicable in the investigation of branaplam-related peripheral neuropathy [1].
价 格:¥电议型 号:T79717产 地:中国大陆
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T79714HDAC3-IN-2;化合物 HDAC3-IN-2HDAC3-IN-2
HDAC3-IN-2 (compound 4i), a pyrazinyl hydrazide-based HDAC3 inhibitor with an IC50 of 14 nM, effectively targets triple-negative breast cancer cells. Demonstrating cytotoxic activity, HDAC3-IN-2 exhibits an IC50 of 0.55 μM against 4T1 cells and 0.74 μM against MDA-MB-231 cells. In vivo, it shows anti-tumor efficacy in tumor-bearing mouse models by selectively elevating acetylation of histones H3K9, H3K27, and H4K12, enhancing apoptosis-inducing proteins caspase-3, caspase-7, and cytochrome c, an
价 格:¥电议型 号:T79714产 地:中国大陆
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T79713JMJD3/HDAC-IN-1;化合物 JMJD3/HDAC-IN-1JMJD3/HDAC-IN-1
Compound A5b, also known as JMJD3/HDAC-IN-1, is a dual inhibitor that targets both JMJD3 (Jumonji domain-containing protein demethylase 3) and HADC1 (histone deacetylase, IC50 = 16 nM). It induces hypermethylation of histone H3K27 and hyperacetylation of H3K9, while also promoting apoptosis through the cleavage of caspase-7 and PARP. This compound has demonstrated the ability to effectively inhibit cancer cell cloning, migration, and invasion [1].
价 格:¥电议型 号:T79713产 地:中国大陆
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T79712TPH1-IN-1;化合物 TPH1-IN-1TPH1-IN-1
TPH1-IN-1 (compound 40) is a xanthine derivative that serves as an inhibitor of tryptophan hydroxylase TPH1, with an IC50 of 110.1 nM. Demonstrating robust in vitro activity and liver microsome stability, it effectively impedes the adipocyte differentiation of T3-L1 cells [1].
价 格:¥电议型 号:T79712产 地:中国大陆
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T79710PI3Kα/HDAC6-IN-1;化合物 PI3Kα/HDAC6-IN-1PI3Kα/HDAC6-IN-1
PI3Kα/HDAC6-IN-1 (compound 21j) is a dual inhibitor of PI3Kα and HDAC6, exhibiting IC50 values of 2.9 nM and 26 nM, respectively. It effectively hinders AKT(Ser473) phosphorylation and promotes the build-up of acetylated α-tubulin, while not influencing acetylated histones H3 and H4. The compound demonstrates potent anti-cancer efficacy by inhibiting the L-363 cell line with an IC50 of 0.17 μM [1].
价 格:¥电议型 号:T79710产 地:中国大陆
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T79690FIKK9.1-IN-1;化合物 FIKK9.1-IN-1FIKK9.1-IN-1
FIKK9.1-IN-1 (Compound 1), an antimalarial agent (IC50: 2.68 μg/mL), serves as a FIKK9.1 inhibitor by interacting with the ATP-binding residues within FIKK9.1, thereby disrupting the parasite life cycle and resulting in parasite death [1].
价 格:¥电议型 号:T79690产 地:中国大陆
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T79683HDAC/CD13-IN-1;化合物 HDAC/CD13-IN-1HDAC/CD13-IN-1
HDAC/CD13-IN-1 (Compound 12) is an inhibitor of both HDAC and CD13, with IC50 values of 0.34 μM for hCD13, 0.53 μM for porcine CD13, and 0.03, 0.06, and 0.02 μM for HDAC1, HDAC2, and HDAC3, respectively. This compound effectively suppresses the proliferation of MV4-11, K562, Jeko-1, and HL60 cancer cells, with IC50 ranges between 0.25-2.04 μM, and also induces apoptosis in these cells. Furthermore, HDAC/CD13-IN-1 demonstrates capabilities in hindering metastasis and invasion [1].
价 格:¥电议型 号:T79683产 地:中国大陆
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T79680PSEN1-IN-2;化合物 PSEN1-IN-2PSEN1-IN-2
PSEN1-IN-2 (Compound 13K) is a potent inhibitor of both PSEN1-APH1A and PSEN1-APH1B complexes, exhibiting IC50 values of 6.9 nM and 2.4 nM, respectively. As a PSEN1 inhibitor, it is utilized in Alzheimer´s disease research [1].
价 格:¥电议型 号:T79680产 地:中国大陆
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T79679PSEN1-IN-1;化合物 PSEN1-IN-1PSEN1-IN-1
PSEN1-IN-1 (Compound (+)-13b) functions as an inhibitor of PSEN1, displaying potent inhibition of the PSEN1-APH1A and PSEN1-APH1B complexes with respective IC50 values of 19 nM and 5.5 nM. This compound is utilized in Alzheimer´s disease research [1].
价 格:¥电议型 号:T79679产 地:中国大陆
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T79678PPARγ-IN-2;化合物 PPARγ-IN-2PPARγ-IN-2
"PPARγ-IN-2 (Compound 5a), a PPARγ inhibitor, exhibits an EC50 of 0.106 μM in inhibiting TG accumulation in 3T3-L1 preadipocytes. Furthermore, PPARγ-IN-2 counteracts obesity and associated metabolic syndrome induced by a high-fat cholesterol (HFC) diet and diminishes lipid accumulation in adipose tissue [1]."
价 格:¥电议型 号:T79678产 地:中国大陆
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T79665RUNX-IN-2;化合物 RUNX-IN-2RUNX-IN-2
RUNX-IN-2 (Compound Conjugate 3) covalently attaches to RUNX-binding sequences, preventing RUNX proteins from associating with their targets, thereby inhibiting cancer cell proliferation and inducing p53-dependent apoptosis. Furthermore, RUNX-IN-2 suppresses tumor development in PANC-1 xenograft mice and demonstrates notable alkylation efficiency and specificity [1].
价 格:¥电议型 号:T79665产 地:中国大陆
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T79664RUNX-IN-1;化合物 RUNX-IN-1RUNX-IN-1
RUNX-IN-1, also known as Compound Conjugate 1, covalently attaches to RUNX-binding sequences, thereby preventing RUNX proteins from associating with their specific targets. This compound triggers p53-dependent apoptosis and suppresses the proliferation of cancer cells. Furthermore, RUNX-IN-1 has demonstrated efficacy in impeding tumor progression in PANC-1 xenograft mice [1].
价 格:¥电议型 号:T79664产 地:中国大陆
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T79655CRM1-IN-2;化合物 CRM1-IN-2CRM1-IN-2
CRM1-IN-2 (Compound KL2) is a noncovalent inhibitor that targets CRM1, localizing it to the nuclear periphery, depleting its nuclear presence, and inhibiting its nuclear export function. It demonstrates the capability to inhibit the growth of colorectal cancer cells and induce apoptosis [1].
价 格:¥电议型 号:T79655产 地:中国大陆
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T79654CRM1-IN-1;化合物 CRM1-IN-1CRM1-IN-1
CRM1-IN-1 (Compound KL1), a noncovalent inhibitor of CRM1, promotes nuclear degradation of CRM1 with an IC50 of 0.27 μM, inhibits CRM1-mediated nuclear export, suppresses cell proliferation, and induces apoptosis in colorectal cancer cells [1].
价 格:¥电议型 号:T79654产 地:中国大陆
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T79653VISTA-IN-2;化合物 VISTA-IN-2VISTA-IN-2
VISTA-IN-2 (Compound 1) is a V-domain Ig suppressor of T-cell activation (VISTA) inhibitor that promotes the degradation of VISTA in cells via autophagy, reverses VISTA-related immunosuppression, and fortifies the antitumor responses of immune cells. Additionally, this compound stimulates antitumor immunity and suppresses tumor growth in a CT26 mouse model [1].
价 格:¥电议型 号:T79653产 地:中国大陆
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T79647VEGFR/PARP-IN-1;化合物 VEGFR/PARP-IN-1VEGFR/PARP-IN-1
VEGFR/PARP-IN-1 (Compound 14b) is a dual inhibitor of VEGFR and PARP with IC50 values of 191 nM and 60.9 nM, respectively. It impairs DNA damage repair pathways, promotes apoptosis, and halts cells in the G2/M phase. This compound demonstrates considerable antiproliferative activity against BRCA wild-type breast cancer cells, with IC50 values of 4.1 μM for MDA-MB-231 cells and 3.5 μM for MCF-7 cells, indicating its potential as an antitumor and anti-metastasis agent [1].
价 格:¥电议型 号:T79647产 地:中国大陆
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T79607h-NTPDase-IN-2;h-NTPDase抑制剂2hNTPDase-IN-2;hNTPDase-IN-2
h-NTPDase-IN-2 is a broad-spectrum NTPDase inhibitor that inhibits multiple h-NTPDas isoforms.
价 格:¥电议型 号:T79607产 地:中国大陆
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T79587hCA/VEGFR-2-IN-2;化合物 hCA/VEGFR-2-IN-2hCA/VEGFR-2-IN-2
Compound 8g (hCA/VEGFR-2-IN-2) is an indolinonylbenzenesulfonamide identified as a potential dual inhibitor targeting cancer-associated isozymes hCA IX/XII and the angiogenic receptor VEGFR-2. It demonstrates VEGFR-2 inhibition with an IC50 of 204 nM and high affinity for hCAs, exhibiting Kis of 3.6 nM for hCA IX, 16.1 nM for hCA II, 16.7 nM for hCA XII, and 75.3 nM for hCA I. Furthermore, compound 8g exhibits antiproliferative effects on breast cancer cells overexpressing VEGFR-2 [1].
价 格:¥电议型 号:T79587产 地:中国大陆
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T79572MAPK-IN-2;化合物 MAPK-IN-2MAPK-IN-2
MAPK-IN-2 (compound 3h) is an efficacious MAPK inhibitor with antineoplastic properties that significantly hinders proliferation across various cancer cell lines. It demonstrates robust suppression of the MAPK pathway (EGFR WT IC50 = 281 nM, c-MET IC50 = 205 nM, B-RAF WT IC50 = 112 nM, CDK4/6 IC50 = 95 and 184 nM, respectively) and exhibits pronounced activity against mutated forms of EGFR and B-RAF (EGFR T790M IC50 = 69 nM and B-RAF V600E IC50 = 83 nM) [1].
价 格:¥电议型 号:T79572产 地:中国大陆
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T79571AChE/Aβ-IN-2;化合物 AChE/Aβ-IN-2AChE/Aβ-IN-2
AChE/Aβ-IN-2 (compound 33) is a powerful, orally active acetylcholinesterase (AChE) inhibitor with an IC50 of 135 nM. It also functions as an NMDA receptor antagonist (GluN1-1b/GluN2B subunit combination) with an IC50 of 5.054 μM, inhibits Aβ aggregation, and exhibits favorable blood-brain barrier permeability. Additionally, it enhances cognitive and spatial memory in a rat model [1].
价 格:¥电议型 号:T79571产 地:中国大陆