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T79733NLRP3-IN-20；化合物 NLRP3-IN-20NLRP3-IN-20
NLRP3-IN-20 (compound 11) is an orally administered inhibitor targeting the NLRP3 inflammasome, exhibiting potent inhibition with an IC50 of 25 nM against IL-1β secretion. It possesses excellent pharmacokinetic properties and has shown significant efficacy in models of non-alcoholic steatohepatitis, fatal septic shock, and colitis [1].
价 格：￥电议型 号：T79733产 地：中国大陆
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T79727EGFR/CDK2-IN-2；化合物 EGFR/CDK2-IN-2EGFR/CDK2-IN-2
EGFR/CDK2-IN-2 (compound 6a) serves as a dual inhibitor targeting both EGFR and CDK-2, exhibiting IC50 values of 19.6 nM and 87.9 nM, respectively. It promotes apoptosis in MCF-7 cells and halts cell cycle progression during the S phase. Additionally, this compound demonstrates notable anticancer activity, inhibiting MCF-7 cells with an IC50 of 0.39 μM [1].
价 格：￥电议型 号：T79727产 地：中国大陆
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T79726RET-IN-25；化合物 RET-IN-25RET-IN-25
RET-IN-25 (compound 6b) is an anticancer RET kinase inhibitor that demonstrates efficacy against medullary thyroid carcinoma (MTC), exhibiting half-maximal inhibitory concentrations (IC50s) of 3.6 μM at 3 days and 3.0 μM at 6 days in TT(C634R) MTC [1].
价 格：￥电议型 号：T79726产 地：中国大陆
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T79723PDK-IN-2；化合物 PDK-IN-2PDK-IN-2
PDK-IN-2 (Compound 1F), with an IC50 of 68 nM, is a potent PDK inhibitor that downregulates the expression of PDK1 and PDK4 in cells. It promotes mitochondrial bioenergetics, reduces glycolytic activity, and triggers apoptosis via the mitochondrial pathway. Additionally, PDK-IN-2 has been shown to impede tumor growth in a 4T1 syngeneic mouse model [1].
价 格：￥电议型 号：T79723产 地：中国大陆
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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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T79706TRK-IN-24；化合物 TRK-IN-24TRK-IN-24
TRK-IN-24 (compound 10g) is a selective inhibitor of Trk receptors, effectively targeting TRKA, TRKC, and mutant forms TRKA G595R, TRKA G667C, and TRKA F589L, with IC50 values of 5.21, 4.51, 6.77, 1.42, and 6.13 nM, respectively. It demonstrates antitumor activity in BaF3-CD74-NTRK1 G595R and BaF3-CD74-NTRK1 G667C xenograft models and inhibits the proliferation of Ba/F3 cells expressing single mutants SF, GK, and xDFG, with an IC50 range of 1.43-47.56 nM [1].
价 格：￥电议型 号：T79706产 地：中国大陆
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T79704CDK9-IN-28；化合物 CDK9-IN-28CDK9-IN-28
PROTAC CDK9/CycT1 Degrader-1 (compounds 10), a potent CDK9 inhibitor, serves as a target protein ligand for PROTAC synthesis. Exhibiting substantial anti-proliferative activity in solid tumors [1], this compound is instrumental in the targeted degradation of CDK9/CycT1.
价 格：￥电议型 号：T79704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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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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T79676SARS-CoV-2 3CLpro-IN-21；化合物 SARS-CoV-2 3CLpro-IN-21SARS-CoV-2 3CLpro-IN-21
SARS-CoV-2 3CLpro-IN-21 (Compound D6) is an irreversible, covalent inhibitor of SARS-CoV-2 3CL pro, demonstrating potent inhibition with an IC50 of 0.03 μM. Additionally, it exhibits inhibitory activity against SARS-CoV-1 3CL pro with an IC50 of 0.12 μM [1].
价 格：￥电议型 号：T79676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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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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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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T79631CDK9-IN-26；化合物 CDK9-IN-26CDK9-IN-26
CDK9-IN-26, also known as compound 1, is a potent inhibitor of Cyclin-Dependent Kinase 9 (CDK9) with an IC50 value of 0.18 μM.[1]
价 格：￥电议型 号：T79631产 地：中国大陆
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T79630CDK9-IN-25；化合物 CDK9-IN-25CDK9-IN-25
CDK9-IN-25 (compound 4a), an imidazopyrazine derivative, functions as a CDK9 inhibitor with an IC50 of 0.24 μM. It also exhibits affinity for the main protease of COVID-19 and demonstrates antiviral activity against human coronavirus 229E, with an IC50 of 63.28 μM [1].
价 格：￥电议型 号：T79630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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T79596FLT3-IN-20；化合物 FLT3-IN-20FLT3-IN-20
FLT3-IN-20 (compound 34f) is a potent FLT3 inhibitor, demonstrating IC50 values of 1 nM for FLT3-D835Y and 4 nM for FLT3-ITD. It exhibits anti-proliferative effects on FLT3-ITD-positive AML cell lines, with IC50s of 7 nM in MV4-11 and 9 nM in MOLM-13, as well as 4 nM in a MOLM-13 variant harboring the FLT3-ITD-D835Y mutation. FLT3-IN-20 is utilized in cancer research [1].
价 格：￥电议型 号：T79596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
