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SR-31747 is a sigma ligand with immunosuppressive and anti-inflammatory properties. SR-31747 blocks cell proliferation by inhibiting sterol isomerase .
SR-1114 is a first-in-class PROTAC ENL degrader. SR-1114 elicits rapid, CRBN-dependent degradation of ENL with DC50s of 150 nM, 311 nM, and 1.65 μM in MV4;11 , MOLM-13, and OCI/AML-2 cells, respectively .
SR-717 is a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively. SR-717 is a stable cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic. Antitumor activity .
SR1555 is a specific retinoic acid receptor-related orphan nuclear receptor γ (RORγ) inverse agonist with an IC50 value of 1 μM. SR1555 not only inhibits TH17 cell development and function but also increases the frequency of T regulatory cells, as well as inhibits the expression of IL-17. SR1555 can be used for researching autoimmune diseases .
SIAIS117 is a potent Brigatinib-PROTAC degrader. SIAIS117 is a ALK PROTAC based on Brigatinib and VHL-1 conjunction. SIAIS117 can degrade ALK G1202R point mutation effectively. SIAIS117 blocks the growth of SR and H2228 cancer cell lines. SIAIS117 has the potentially anti-proliferation ability of small cell lung cancer .
SR-31747 free base is a sigma ligand with immunosuppressive and anti-inflammatory properties. SR-31747 blocks cell proliferation by inhibiting sterol isomerase .
SR-4133 is a potent and highly CK1ε selective inhibitor with an IC50 of 58 nM. SR-4133 binds to the ATP-binding site of CK1ε. SR-4133 displays nanomolar growth inhibition of bladder cancer cells, and inhibits the phosphorylation of 4E-BP1 .
SR1555 hydrochloride is the hydrochloride salt form of SR1555 (HY-120785). SR1555 hydrochloride is an inverse agonist for retinoic acid receptor-related orphan nuclear receptor γ (RORγ) with an IC50 of 1 μM. SR1555 hydrochloride inhibits the development and function of pro-inflammatory TH17 cell, increases the frequency of anti-inflammatory T regulatory (Treg) cells. SR1555 hydrochloride can be used for research about autoimmune diseases .
SR-3-65 (compound 6) is a Indisulam (HY-13650) derivative,and inhibits the migration of gastric cancer cells. SR-3-65 attenuates PI3K/AKT/GSK-3β/β-catenin signaling pathway .
SR 33805 (analog) is an orally active Ca 2+ channel blocker that selectively inhibits the proliferation of smooth muscle cells. SR 33805 (analog) reduces calcium uptake by blocking calcium channels, thereby inhibiting smooth muscle cell proliferation induced by serum, platelet-derived growth factor, and basic fibroblast growth factor. SR 33805 (analog) significantly reduces intimal thickening following endothelial injury in rabbits. SR 33805 (analog) shows promise for cardiovascular disease research, such as in early atherosclerosis .
SR-717 free acid is a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively. SR-717 free acid is a stable cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic. Antitumor activity .
SR 142948 is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 shows blood-brain permeability and can be used in study of psychiatric disorders .
SR 142948 dihydrochloride is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 dihydrochloride antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 dihydrochloride blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 dihydrochloride shows blood-brain permeability and can be used in study of psychiatric disorders .
SR-4835 is a potent, highly selective and ATP competitive dual inhibitor of CDK12/CDK13 (CDK12: IC50=99 nM, Kd=98 nM; CDK13: Kd=4.9 nM). SR-4835 acts in synergy with DNA-damaging chemotherapy and PARP inhibitors and provokes triple-negative breast cancer (TNBC) cell death .
HDL376 is a scavenger receptor class B type I (SR-BI) inhibitor. HDL376 directly inhibits SR-BI-mediated lipid transport in cells and in liposomes reconstituted with purified SR-BI (IC50 = 0.22 μM). HDL376 can be used for the research of atherosclerotic coronary artery disease .
Tirapazamine (SR259075) is an anticancer agent that shows selective cytotoxicity for hypoxiccells in solid tumors, thereby inducing single-and double-strand breaks in DNA, base damage, and cell death. Tirapazamine is an anticancer and bioreductive agent.Tirapazamine (SR259075) can enhance the cytotoxic effects of ionizing radiation in hypoxic cells .
Bayer-18 is an inhibitor for TYK2. Bayer-18 inhibits the viability of ALCL cell K299, SR786, Mac1 and Mac2a with IC50 of 2-3 µM, and induces apoptosis in K299 and SR786 .
SR18662 is a potent inhibitor of Krüppel-like factor five (KLF5) with an IC50 of 4.4 nM and an analogue of ML264 (HY-19994) with improved inhibitory potency against colorectal cancer cells. SR18662 can be used for the study of colorectal cancer .
ML179 (SR-1309) is a inverse LRH1 (Liver receptor homologue-1) agonist with IC50 of 320 nM. ML179 shows anti-proliferation activity in MDA-MB-231 cells. ML179 has the potential for the research of ER-negative breast cancer .
BLT-1, a thiosemicarbazone copper chelator, is a selective scavenger receptor B, type 1 (SR-BI) inhibitor. BLT-1 inhibits the transfer of lipids between high-density lipoproteins (HDL) and cells mediated by SR-BI. BLT-1 is a potent HCV entry inhibitor .
SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects .
PK 130 is a 2-nitroimidazole derivative that demonstrated potent hypoxic cellular radiosensitization in vitro as assessed by aerobic and hypoxic radiosensitivity of Chinese hamster V79 cells. PK 130 and PK 110 were more potent than SR-2508 at the same concentrations at 0.1 and 1.0 mM. The relative radiosensitization produced by PK 130 and PK 110 at 0.1 mM was comparable to that of 1.0 mM SR-2508. However, at 0.1 mM, the therapeutic effects of PK 130 and PK 110 were only modestly aerobic radiosensitizing. The relative radiosensitization of PK 130 and PK 110 at 0.1 mM was further enhanced by the reduction of glutathione (GSH) levels (less than 5% of control levels) by L-cysteine sulfoxide (BSO). The results of this study encourage the in vivo tumor radiosensitization evaluation of PK 130 and PK 110.
Apomine (SR-45023A) is an antineoplastic agent that inhibits the mevalonate/isoprenoid pathway in cholesterol synthesis.
Apomine can accelerate the degradation of 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR). Apomine can also inhibit the growth of various types of cancer cells, including lung cancer, colon cancer, breast cancer, and skin cancer. In addition, Apomine is able to induce apoptosis in tumor cell lines derived from leukemia, colon cancer, liver cancer, ovarian cancer, and breast cancer .
Brinazarone (SR 33287) is an inhibitor for acid lysosomal sphingomyelinase, and leads to cellular lipidosis. Brinazarone potentiates the cytotoxic effects of anti-Thy 1.2 AT15E RTA-IT on T2 cells and anti-CD5 T101 on CEM cells .
SIAIS164018 is a PROTAC-based ALK and EGFR degrader, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 exhibits better property than Brigatinib (HY-12857) .
SIAIS164018 hydrochloride is a PROTAC-based ALK and EGFR degrader, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 hydrochloride strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 hydrochloride exhibits better property than Brigatinib (HY-12857) .
LK1/2-IN-3 (compound 3) is a potent and selective CLK1 and CLK2 inhibitor with IC50 values of 1.1, 2.1, 130, 260, 260 nM for CLK1, CLK2, SRPK1, SRPK2, SRPK3, respectively. CLK1/2-IN-3 shows anti-proliferative activity. CLK1/2-IN-3 reduces the levels of endogenous phosphorylated SR proteins and increases the expression of S6K mRNAs .
Stemregenin 1 (GMP) (SR1 (GMP)) is Stemregenin 1 Y-15001) in GMP grade. GMP-grade small molecules can be used as auxiliary reagents in cell therapy. Stemregenin 1 is a potent aryl hydrocarbon receptor (AhR) antagonist with IC50 of 127 nM.
SR 57227A Free base is a highly selective compound for both peripheral and central 5-HT3 receptors and acts as an inhibitor of NMDA receptor-mediated responses in rat cortical pyramidal cells, demonstrating antidepressant-like effects in rats while reducing isolation-induced aggressive behavior.
SARS-CoV-2 3CLpro-IN-26 (Compound (S,R)-4y) is an allosteric inhibitor for SARS-CoV-2 3CLpro with an IC50 of 0.43 μM. SARS-CoV-2 3CLpro-IN-26 exhibits good cell permeability and is able to effectively cross the cell membrane, after co-incubation with Vero-E6 cells .
Neihulizumab (ALTB-168) is an immune checkpoint agonistic antibody that binds to human CD162 (PSGL-1), leading to downregulation of activated T-cells. Neihulizumab can be uesd for steroid-refractory acute graft-versus-host-disease (SR-aGVHD), psoriasis, psoriatic arthritis and ulcerative colitis research .
LBM22 is a CDC2-like kinase 2 (CLK2) inhibitor with the IC50 of 3.9 nM. LBM22 has antiproliferative activity and inhibits serine/arginine-rich (SR) protein phosphorylation. LBM22 down-regulates the expression of Wnt-related proteins and anti-apoptotic proteins and can be used for study of non-small cell lung cancer .
PPI-2458 is a potent, orally active, selective and irreversible inhibitor of methionine aminopeptidase-2 (MetAP-2). PPI-2458 can be used for arthritis and lymphoma research .
Neihulizumab (ALTB-168) is an immune checkpoint agonistic antibody that binds to human CD162 (PSGL-1), leading to downregulation of activated T-cells. Neihulizumab can be uesd for steroid-refractory acute graft-versus-host-disease (SR-aGVHD), psoriasis, psoriatic arthritis and ulcerative colitis research .
PPI-2458 is a potent, orally active, selective and irreversible inhibitor of methionine aminopeptidase-2 (MetAP-2). PPI-2458 can be used for arthritis and lymphoma research .
SREC-I/SCARF1 Protein acts as a multifunctional mediator, facilitating Ac-LDL binding and degradation, suggesting a role in lipid metabolism and adhesion. Involved in neurite-like outgrowth, it interacts with SREC2 and AVIL, forming a complex molecular network. The protein's diverse roles underscore its significance in various cellular processes beyond lipid metabolism. SREC-I/SCARF1 Protein, Human (HEK293, His) is the recombinant human-derived SREC-I/SCARF1 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of SREC-I/SCARF1 Protein, Human (HEK293, His) is 402 a.a., .
SARS-CoV-2 3CLpro-IN-26 (Compound (S,R)-4y) is an allosteric inhibitor for SARS-CoV-2 3CLpro with an IC50 of 0.43 μM. SARS-CoV-2 3CLpro-IN-26 exhibits good cell permeability and is able to effectively cross the cell membrane, after co-incubation with Vero-E6 cells .
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