| DC24105 |
MK-0591（Quiflapon ）
Featured
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A potent, specific and orally active 5-Lipoxygenase-activating protein (FLAP) inhibitor with IC50 of 1.6 nM in FLAP binding assay. |
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| DC11556 |
trans-AUCB |
A potent, specific and orally bioavailable soluble epoxide hydrolase (sEH) inhibitor with IC50 of 1.3 nM. |
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| DC21802 |
VU 0364849 |
A potent, specific BMP receptor activin receptor-like kinase 3 (ALK3) antaognist with Ki of 5.4 nM. |
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| DC21807 |
VU 0465350
Featured
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VU 0465350 is a potent, specific BMP receptor activin receptor-like kinase 3 (ALK3) antaognist with Ki of 92.3 nM; shows no activity for ALK2/4/5, also shows affinity for TGFBR2, VEGFR2 and AMPK; blocks SMAD phosphorylation in vitro and in vivo, and enhances liver regeneration after partial hepatectomy. |
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| DC21693 |
SRI-29329 |
A potent, specific CDC-like kinase (CLK) inhibitor with IC50 of 78, 16 and 86 nM for CLK1, 2 and4, respectively. |
|
| DC21794 |
VH 298
Featured
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A potent, specific cell-active VHL E3 ubiquitin ligase inhibitor that inhibits VHL/HIF-α interaction with Kd of 90 nM in ITC assays. |
|
| DC23985 |
Laduviglusib trihydrochloride
Featured
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Laduviglusib (CHIR-99021) trihydrochloride is a well-characterized small molecule inhibitor that specifically targets glycogen synthase kinase-3 alpha and beta (GSK-3α/β). It exhibits potent inhibitory activity with IC50 values of 10 nM for GSK-3α and 6.7 nM for GSK-3β. Importantly, it demonstrates high selectivity, being over 500-fold more selective for GSK-3 compared to other kinases such as CDC2 and ERK2, as well as a broad range of other protein kinases. |
|
| DC21150 |
PR-924 |
A potent, specific immunoproteasome LMP7 subunit inhibitor with IC50 of 25 nM, >100-fold selectivity over β5c, β1i, β1c, β2i and β2c subunits (IC50>3 uM). |
|
| DC21773 |
UK-101 |
A potent, specific immunoproteasome β1i (LMP2) subunit inhibitor with IC50 of 104 nM, 144- and 10-fold selectivity over β1c and β5 subunit respectivey. |
|
| DC21527 |
PR-893 |
A potent, specific immunoproteasome β5 subunit inhibitor with IC50 of 17 nM, 21-fold and 13-fold selectivity for β5 over LMP7 and LMP2 subunits, respecitvely.. |
|
| DC21365 |
NC-005 |
A potent, specific immunoproteasome β5 subunit inhibitor with IC50 of 44 nM, 105 and 225-fold selectivity over β2i and β1i subunit, respecitvely. |
|
| DC21528 |
PR-825 |
A potent, specific immunoproteasome β5 subunit inhibitor.. |
|
| DC24007 |
R-1479
Featured
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A potent, specific inhibitor of HCV NS5B polymerase and HCV replication (IC50=1.28 uM, replicon assay). |
|
| DC22758 |
SI-113 |
A potent, specific inhibitor of the SGK1 kinase activity, induces autophagy, apoptosis and ER stress in cancer cells. |
|
| DC20998 |
ES 936 |
A potent, specific mechanism-based human NAD(P)H: quinone oxidoreductase 1 (NQO1) inhibitor that demonstrates efficient inactivation of NQO1 at 100 nM in in cellular systems. |
|
| DC22823 |
Tariquidar methanesulfonate hydrate |
A potent, specific P-gp inhibitor with Kd of 5.1 nM. |
|
| DC21849 |
YU-101 |
A potent, specific proteasome β5 subunit inhibitor with IC50 of 0.26 uM, 7.3 and 17.3-fold selectivity over β2i and β1i subunit, respecitvely.. |
|
| DC26068 |
BMS-753 |
A potent, specific RARα agonist with Ki of 2 nM, displays no significant effects on RARγ in reporter based assays.. |
|
| DC22661 |
AB1 |
A potent, specific S1P2 receptor (Edg-5) antagonist with IC50 of 3 nM, with no agonistic or antagonistic activities on other S1PRs. |
|
| DC24060 |
YM-155 hydrochloride
Featured
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A potent, specific survivin inhibitor that inhibits survivin promoter activity with IC50 of 0.54 nM. |
|
| DC22864 |
KSP-IA |
A potent, specific, allosteric and cell-active inhibitor of KSP with IC50 of 11 nM. |
|
| DC22865 |
CK-0106023
Featured
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A potent, specific, allosteric inhibitor of KSP motor domain ATPase with Ki of 12 nM. |
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| DC21318 |
ML 171 |
A potent, specific, cell-active NADPH oxidase1 (Nox1) inhibitor that strongly blocks ROS generation in HT29 cells with IC50 of 0.129 uM. |
|
| DC20890 |
ChoK-α inhibitor CK37
Featured
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A potent, specific, competitive inhibitor of choline kinase-α (Chok-α) by targeting the choline binding site; significantly increases LC3II expression in MCF-7 and MCF-7/TAM cells, increases the size and number of autophagosome, causes MCF-7 and MCF-7/TAM |
|
| DC21110 |
HCI-2389 |
A potent, specific, irreversible NIMA-related Kinase 2 (NEK2) inhibitor with IC50 of 16.65 nM. |
|
| DC26079 |
GW 803430
Featured
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A potent, specific, orally active melanin concentrating hormone receptor 1 (MCHR1) inhibitor with kI of 3.8 nM, >100-fold selectivity over a battery of GPCRs, ion channels and enzymes. |
|
| DC20928 |
CRT0066101
Featured
|
A potent, specific, orally active pan-PKD (protein kinase D) inhibitor with biochemical IC50 of 1, 2.5 and 2 nM for PKD1, 2, and 3 respectively. |
|
| DC22550 |
TAK-220 |
A potent, specific, orally bioavailable CCR5 antagonist that blocks the binding of MIP-1α to CCR5 with IC50 of 1.4 nM. |
|
| DC22540 |
Pasireotide
Featured
|
Pasireotide (SOM230), a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide also exhibits antisecretory, antiproliferative, and proapoptotic activity.
At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Pasireotide acetate) usually boasts enhanced water solubility and stability. |
|
| DC22539 |
Pasireotide L-aspartate salt |
A potent, stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (pKi=8.2/9.0/9.1/<7.0/9.9 for sst1/2/3/4/5, respectively). |
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