Acyltransferase
阻害剤の選択性比較
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S2187 | Avasimibe (CI-1011) | <1 mg/mL | 100 mg/mL | ''8 mg/mL |
| S3021 | Rimonabant (SR141716) | <1 mg/mL | 25 mg/mL | '''''2 mg/mL |
| S2674 | A922500 | <1 mg/mL | 86 mg/mL | '<1 mg/mL |
| S0820 | RP-64477 | <1 mg/mL | 100 mg/mL | ''''<1 mg/mL |
| S0359 | T863 (DGAT-3) | <1 mg/mL | 79 mg/mL | '''1.5 mg/mL |
| S9921 | PF-06424439 | 88 mg/mL | 88 mg/mL | '88 mg/mL |
| S4189 | Cyclandelate | <1 mg/mL | 55 mg/mL | 55 mg/mL |
| S9162 | Rubimaillin | -1 mg/mL | 22 mg/mL | -1 mg/mL |
| S7192 | PF-04620110 | <1 mg/mL | 49 mg/mL | <1 mg/mL |
| S7889 | Xanthohumol | <1 mg/mL | 70 mg/mL | '70 mg/mL |
亜型選択性的な製品
Acyltransferase製品
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S2187 |
Avasimibe (CI-1011)Avasimibe (CI-1011, PD-148515) inhibits ACAT with IC50 of 3.3 μM, also inhibits human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with IC50 of 2.9 μM, 13.9 μM and 26.5 μM, respectively. |
a, b, Melanoma-bearing mice were treated with avasimibe (Ava) or DMSO control (5 times) (control, n=9; avasimibe, n=8). c-e, STORM analysis of TCR clustering of tumour-infiltrating CD8+ T cells. c, Representative images. d, Ripley’s K-function analysis of TCR molecules. e, The r value at the maximal L(r)-r value of Ripley’s K-function curves (control, n=100; avasimibe, n=85). f, g, A combined therapy (avasimibe and anti-PD-1) or monotherapies (avasimibe or anti-PD-1) in treating melanoma (n=10). Avasimibe, 5 times; anti-PD-1, 4 times. h, i, Cytokine/granule productions of PD-1hi and PD-1lo tumour-infiltrating CD8+ T cells (control, n=12; avasimibe, n=11). |
|
| S3021 |
Rimonabant (SR141716)Rimonabant (SR141716) is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane. Rimonabant is also a dual inhibitor of acyl CoA:cholesterol acyltransferases(ACAT) 1 and 2 and inhibits mycobacterial MmpL3. |
||
| S2674 |
A922500A922500 (DGAT-1 Inhibitor 4a) is an inhibitor for human and mouse DGAT-1 with IC50 of 7 nM and 24 nM, respectively, good selectivity over related acyltransferases, hERG, and a panel of anti-targets. |
||
| S0820 |
RP-64477RP-64477 is a potent inhibitor of the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT). RP-64477 inhibits ACAT activity with IC50 of 113 nM, 503 nM, and 180 nM in human intestinal (CaCo-2), hepatic (HepG2) and monocytic (THP-1) cell assays, respectively. |
||
| S0359 |
T863 (DGAT-3)T863 (DGAT-3) is a potent, selective and orally active inhibitor of Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) tht acts on the acyl-CoA binding site of DGAT1 and inhibits DGAT1-mediated triacylglycerol formation in cells. |
||
| S9921新 |
PF-06424439PF-06424439 is a first orally bioavailable small-molecule inhibitor of DGAT2 with an IC50 of 14 nM. |
||
| S4189 |
CyclandelateCyclandelate (BS 572) is an effective inhibitor of rat hepatic acycloenzyme A: cholesterol acyltransferase (ACAT) with IC50 of 80 μM. |
||
| S9162 |
RubimaillinRubimaillin (Mollugin), found in the Chinese medical plant Rubia cordifola, is a dual inhibitor of acetyl-CoA cholesterol acyltransferase 1 (ACAT1) and acetyl-CoA cholesterol acyltransferase 2 (ACAT2), but is more selective for the ACAT2 isozyme. |
||
| S7192 |
PF-04620110PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM. |
||
| S7889 |
XanthohumolXanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects. Xanthohumol inhibits diacylglycerol acyltransferase 1 (DGAT1) and DGAT2 with both IC50 of 40 μM. Xanthohumol is also a potent antiviral agent against a series of DNA and RNA viruses. Xanthohumol induces growth inhibition and apoptosis in cancer cells. Phase 1. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S2187 |
Avasimibe (CI-1011)Avasimibe (CI-1011, PD-148515) inhibits ACAT with IC50 of 3.3 μM, also inhibits human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with IC50 of 2.9 μM, 13.9 μM and 26.5 μM, respectively. |
a, b, Melanoma-bearing mice were treated with avasimibe (Ava) or DMSO control (5 times) (control, n=9; avasimibe, n=8). c-e, STORM analysis of TCR clustering of tumour-infiltrating CD8+ T cells. c, Representative images. d, Ripley’s K-function analysis of TCR molecules. e, The r value at the maximal L(r)-r value of Ripley’s K-function curves (control, n=100; avasimibe, n=85). f, g, A combined therapy (avasimibe and anti-PD-1) or monotherapies (avasimibe or anti-PD-1) in treating melanoma (n=10). Avasimibe, 5 times; anti-PD-1, 4 times. h, i, Cytokine/granule productions of PD-1hi and PD-1lo tumour-infiltrating CD8+ T cells (control, n=12; avasimibe, n=11). |
|
| S3021 |
Rimonabant (SR141716)Rimonabant (SR141716) is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane. Rimonabant is also a dual inhibitor of acyl CoA:cholesterol acyltransferases(ACAT) 1 and 2 and inhibits mycobacterial MmpL3. |
||
| S2674 |
A922500A922500 (DGAT-1 Inhibitor 4a) is an inhibitor for human and mouse DGAT-1 with IC50 of 7 nM and 24 nM, respectively, good selectivity over related acyltransferases, hERG, and a panel of anti-targets. |
||
| S0820 |
RP-64477RP-64477 is a potent inhibitor of the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT). RP-64477 inhibits ACAT activity with IC50 of 113 nM, 503 nM, and 180 nM in human intestinal (CaCo-2), hepatic (HepG2) and monocytic (THP-1) cell assays, respectively. |
||
| S0359 |
T863 (DGAT-3)T863 (DGAT-3) is a potent, selective and orally active inhibitor of Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) tht acts on the acyl-CoA binding site of DGAT1 and inhibits DGAT1-mediated triacylglycerol formation in cells. |
||
| S9921新 |
PF-06424439PF-06424439 is a first orally bioavailable small-molecule inhibitor of DGAT2 with an IC50 of 14 nM. |
||
| S4189 |
CyclandelateCyclandelate (BS 572) is an effective inhibitor of rat hepatic acycloenzyme A: cholesterol acyltransferase (ACAT) with IC50 of 80 μM. |
||
| S9162 |
RubimaillinRubimaillin (Mollugin), found in the Chinese medical plant Rubia cordifola, is a dual inhibitor of acetyl-CoA cholesterol acyltransferase 1 (ACAT1) and acetyl-CoA cholesterol acyltransferase 2 (ACAT2), but is more selective for the ACAT2 isozyme. |
||
| S7192 |
PF-04620110PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM. |
||
| S7889 |
XanthohumolXanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects. Xanthohumol inhibits diacylglycerol acyltransferase 1 (DGAT1) and DGAT2 with both IC50 of 40 μM. Xanthohumol is also a potent antiviral agent against a series of DNA and RNA viruses. Xanthohumol induces growth inhibition and apoptosis in cancer cells. Phase 1. |
