PAT1inh-B01 is a small-molecule, selective SLC26A6 (putative anion transporter 1, PAT1) inhibitor, could fully inhibit PAT1-mediated anion exchange with IC50 of 350 nM.

UNC0737 is a negative control of UNC0638 and the N-methyl analog of UNC0638. UNC0737 was designed to eliminate the hydrogen bond interaction seen in the G9a-UNC0224 cocrystal structure between Asp1083 of G9a and the secondary amino group at the 4-position of UNC0224's quinazoline ring3. UNC0737 was >300-fold less potent than UNC0638 in G9a and GLP biochemical assays. As expected, UNC0737 was a poor inhibitor of G9a (IC50 = 5,000 ± 200 nM (n = 2)) and GLP (IC50 > 10,000 nM (n = 2)) in the SAHH-coupled assays.

A novel protein kinase affinity probe...

SN38 NHS ester is the NHS ester derivative of SN38. SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 inhibits DNA and RNA synthesis. SN38 NHS ester can be used for the synthesis of antibody-drug conjugates (ADCs).

PF-06648671 is a potent γ-secretase modulator with IC50 of 8.9 nM against Aβ42. PF-06648671 has favorable brain availability in rodent, which translated into excellent central exposure in human and robust reduction of amyloid β (Aβ) 42 in cerebrospinal fluid (CSF).

DFV890 (IFM-2427) is apotent, selective and orally active inhibitor of NLRP3 inflammasome, directly binds to NLRP3 and locks the protein in an inactive conformation,prevents NLRP3 inflammasome assembly in response to sterile danger signals.

GSK-484 is a potent, highly selective and reversible protein arginine deiminase PAD4 inhibitor with IC50 of 80 nM in FP binding assay (0.2 mM Ca), 50 nM in PAD4 NH3 release inhibition assay.

AZD0780 is the first oral small molecule PCSK9 inhibitor for the treatment of hypercholesterolemia.

G150 is a highly selective human cyclic GMP-AMP synthase (h-cGAS) inhibitor with an IC50 of 10.2 nM. G150 represses dsDNA-triggered interferon expression, and G150 can be used for the research of inflammatory.

G140 is a potent and selective inhibitor of cyclic GMP-AMP synthase (cGAS), with IC50s of 14.0 nM and 442 nM for h-cGAS and m-cGAS, respectively. G140 has anti-inflammatory activity.

GDC-1971 showed outstanding potency in biochemical and cell models, and it had a predicted human PK profile that suggested it would achieve target engagement at reasonable doses. GDC-1971 showed an IC50 below the limit of detection of the assay (≪0.001 μM), while that IC50 shifted to 0.17 μM in the same biochemical assay with the constitutively active E76K SHP2 mutant.

diABZI STING agonist-1 is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively.

LY2562175 is a potent and selective FXR agonist, with an EC50 of 193 nM.

Pradigastat (LCQ-908) is a potent, selective and orally active diacylglycerol acyltransferase 1 (DGAT1) inhibitor. Pradigastat has anti-obesity and anti-diabetic effects.

PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.

PF-06928215 (PF06928215) is a high affinity Cyclic GMP-AMP synthase (cGAS) inhibitor with Kd of 200 nM, IC50 of 4.9 uM.

RBN013209 is a potent CD38 inhibitor and is useful in the treatment of cancer.

AT-511, the free base form of AT-527, against several coronaviruses, including SARS-CoV-2, the causative agent of COVID-19. In normal human airway epithelial (HAE) cell preparations, the average concentration of AT-511 required to inhibit replication of S

BC1618 is a novel Fbxo48 inhibitor and prevent pAmpkα degradation with MEC (minimal efficacious concentration) of 0.6 μM.

E3L-4133, also known as E3 ligase Ligand 5, is an E3 ligase Ligand that can be used in PROTAC (proteolysis targeting chimera) technology to engage an E3 ubiquitin ligase. PROTAC is a two-headed molecule capable of removing specific unwanted proteins. E3L-4133 has CAS#1264754-13-3. The last 4 digits was used for name.

G10 (STING Agonist 1) is a novel human-specific STING agonist.

Endovion (NS 3728, SCO-101) is an potent anion channel inhibitor that blocks the Volume Regulated Anion Channels (VRAC).

USL311 is a CXCR4 receptor antagonist which prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4. USL311 inhibits CXCR4 activation and decreases proliferation and migration of CXCR4-expressing tumor cells.

Phthalazinone pyrazole is a potent inhibitor of Aurora A kinase (IC50 = 31 nM).

ML251, a potent nanomolar T. brucei and T. cruzi phosphofructokinase (PFK) inhibitor, inhibits T. brucei PFK (IC50=0.37 μM) and T. cruzi PFK (IC50=0.13 μM). ML251 can be used for the research of parasite.

SU14813 is an oral, multitargeted tyrosine kinase inhibitor (TKI) targeting vascular endothelial growth factor receptors (VEGFR), platelet-derived growth factor receptors (PDGFR), Kit, and fms-like tyrosine kinase 3 (FLT-3).

SJB2-043 is an inhibitor of the native USP1/UAF1 complex with IC50 of 544 nM.SJB2-043 causes a dose-dependent decrease in ubiquitin-specific protease 1 (USP1) levels and a concomitant degradation of inhibitor of DNA-binding-1 (ID1) protein in the K562 cells at a micromolar drug concentration. SJB2-043 also causes a decrease in the levels of other ID proteins, namely ID2 and ID3 in K562 cells. SJB2-043 causes a dose-dependent decrease in the number of viable K562 cells, with an EC50 of approximately 1.07 μM. Moreover, SJB2-043 induces apoptosis of K562 cells in a dose-dependent manner.

AS 602801(Bentamapimod) is a novel, orally active inhibitor of JNK.

Rhonin is a first small-molecule ligand of the RHO GDP-dissociation inhibitor 1 (RHOGDI1), binds to RHOGDI (Ki=2.2 uM), is an inhibitor of Hh-induced osteogenesis.Rhonin interferes with its function by disrupting the interaction between RHOGDI and RHO GTPases.Rhonin alters the subcellular localization of RHO GTPases.Rhonin inhibited RHOGDI1-mediated extraction of RAC1 from liposomes, Rhonin increased the levels of GTP-bound RHO GTPases, did not alter the total levels of the three RHO GTPasesRhonin an inhibitor of Hh-induced osteogenesis, but does not efficiently target canonical Hh signaling and SMO, directly targets RHOGDI, impairs RHOGDI function.

KAL-21404358 (KAL21404358) is a small-molecule, allosteric inhibitor of K-Ras(G12D), binds to K-Ras(G12D) P110 site with KD of 88 uM in MST assay; KAL-21404358 disrupts the K-RasG12D-B-Raf interaction using a NanoBiT split luciferase assay, and to impair the Raf-MEK-ERK and the PI3K-AKT signaling pathways. KAL-21404358 exhibited specificity for K-RasG12D over K-RasWT, H-RasWT, Rap1a, R-Ras and R-Ras2.