| DC47561 |
MHY-1685
Featured
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MHY-1685, a novel mammalian target of rapamycin (mTOR) inhibitor, provides opportunities to improve hCSC-based myocardial regeneration.
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| DC47562 |
VB124
Featured
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VB-124 is a potent and selective MCT4 inhibitor. VB124 might redirect glycolytic carbon flux into mitochondrial pyruvate oxidation. VB 124 bolcks lactate import (IC50=8.6nM), and export (IC50=19nM) in MDA-MB-231 cells that are engineers to express MCT4 as the only major plasma membrane lactate transporter. |
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| DC47581 |
BMS-986278
Featured
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BMS-986278 is a potent lysophosphatidic acid receptor 1 (LPA1) antagonist, with a human LPA1 Kb of 6.9 nM. |
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| DC47591 |
JAK-IN-14
Featured
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JAK-IN-14 is a potent and selective JAK1 inhibitor, with an IC50 of <5 μM. JAK-IN-14 is >8-fold more selective for JAK1 than JAK2 and JAK3 (Patent WO2016119700A1, compound 16). |
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| DC47604 |
GPS491
Featured
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GPS491 (EC50 = 0.47 μM) suppresses expression of the HIV-1 structural protein Gag and alters HIV-1 RNA accumulation, decreasing the abundance of RNAs encoding the structural proteins while increasing levels of viral RNAs encoding the regulatory proteins. |
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| DC47608 |
EZH2-IN-2
Featured
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EZH2-IN-2 is a EZH2 inhibitor extracted from patent WO2018133795A1, Compound Example 69, with an IC50 of 64 nM. EZH2-IN-2 can be used for the research of cancer or precancerous condition related to EZH2 activity. |
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| DC47614 |
EEDi-5273
Featured
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EEDi-5273 is an exceptionally potent and orally efficacious embryonic ectoderm development (EED) inhibitor with IC50 of 0.2 nM and inhibits the KARPAS422 cell growth with IC50 of 1.2 nM. EEDi-5273 demonstrates an excellent PK and ADME profile, and its oral administration leads to complete and persistent tumor regression in the KARPAS422 xenograft model with no signs of toxicity. |
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| DC47616 |
EPZ-719
Featured
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EPZ-719 is a novel and potent SETD2 inhibitor ( IC50 = 0.005 μM) with a high selectivity over other histone methyltransferases. |
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| DC47621 |
Seclidemstat mesylate
Featured
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Seclidemstat (SP-2577) mesylate is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat mesylate promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat mesylate can be used for the research of Ewing Sarcoma. |
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| DC47622 |
Cyclizine
Featured
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Cyclizine is a piperazine first-generation antagonist of histamine 1 receptor. |
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| DC47635 |
GLP-1R modulator L7-028
Featured
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GLP-1R modulator L7-028 is an allosteric modulator enhancing GLP-1 binding to GLP-1R via a transmembrane site (EC50 11.01 ± 2.73 μM). |
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| DC47678 |
M435-1279
Featured
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M435-1279 is a UBE2T inhibitor. M435-1279 acts inhibit the Wnt/β-catenin signaling pathway hyperactivation through blocking UBE2T-mediated degradation of RACK1. |
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| DC47680 |
PSMA-Val-Cit-PAB-MMAE
Featured
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PSMA-Val-Cit-PAB-MMAE is a novel small-molecule PSMA-targeted conjugate based on the monomethyl auristatin E for the chemotherapy of prostate cancer. |
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| DC47683 |
Mesdopetam hemitartrate
Featured
|
Mesdopetam (IRL790) hemitartrate is a dopamine D3 receptor antagonist (Ki=90 nM; IC50=9.8 μM for human recombinant D3 receptor) with psychomotor stabilizing properties. Mesdopetam hemitartrate is used for the research of motor and psychiatric complications in Parkinson disease. |
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| DC47703 |
BPR1R024
Featured
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BPR1R024 is an orally active and selective CSF1R inhibitor with IC50 of 0.53 nM. BPR1R024 specifically inhibits protumor M2-like macrophage survival with a minimal effect on antitumor M1-like macrophage growth. |
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| DC47713 |
GCPII-IN-1 TFA
Featured
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GCPII-IN-1 TFA is a glutamate carboxypeptidase II (GCPII, or PSMA) inhibitor scaffold with a Ki of 44.3 nM. |
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| DC47717 |
TAK-020
Featured
|
TAK-020 is a covalent Btk inhibitor, which becomes the clinical candidate. |
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| DC47718 |
AS-1763
Featured
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AS-1763 is an orally available, potent, and selective BTK inhibitor and shows excellent potency against both wild/C481S mutant BTKs with IC50 of 0.85 nM/0.99 nM. |
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| DC47721 |
JNJ-67569762
Featured
|
JNJ-67569762 is a tetrahydropyridine-based BACE1 inhibitor targeting the S3 pocket with IC50 of 2.7 nM and shows 71-fold selectivity over BACE2. |
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| DC47754 |
Disitamab vedotin
Featured
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Disitamab vedotin (RC48) is an antibody-drug conjugate (ADC) comprising a monoclonal antibody against human epidermal growth factor receptor 2 (HER2) conjugated via a cleavable linker to the cytotoxic agent monomethyl auristatin E. Disitamab vedotin enhances antitumor immunity. |
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| DC47763 |
Vevorisertib trihydrochloride
Featured
|
Vevorisertib (ARQ 751) (trihydrochloride) is an orally active, potent and selective pan-AKT serine/threonine kinase inhibitor against AKT1 (IC50=0.55 nM), AKT2 (IC50=0.81 nM), and AKT3 (IC50=1.31 nM). Vevorisertib (trihydrochloride), as a single agent or in combination with other anti-cancer agents, can be used for the research of solid tumors with PIK3CA / AKT / PTEN mutations. |
|
| DC47768 |
BMS-963272
Featured
|
BMS-963272 is a potent, selective MGAT2 inhibitor with IC50 of 7.1 nM/18 nM (hMGAT2/mMGAT2) and shows excellent efficacy, safety, and tolerability profile. |
|
| DC47779 |
LysoTracker Red
Featured
|
LysoTracker Red (LysoTracker Red DND-99) is a paraformaldehyde fixable probe that concentrates into acidic compartments of cells and tissues. LysoTracker Red is an indicator of cell death in a manner similar to other standard assays (Annexin, terminal dUTP nick end labeling, Nile blue sulfate, neutral red, and acridine orange). LysoTracker Red is a marker for late endosomes and lysosomes. |
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| DC47813 |
OG 488, acid
Featured
|
OG 488, acid, a fluorescent pH indicator, has many applications in biochemistry and neurosciences. |
|
| DC47821 |
Ricinine
Featured
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Ricinine is a pyridine alkaloid found in the seeds and leaves of the castor oil plant (Ricinus communis). While Ricinus communis is primarily known for producing ricin, a highly toxic protein, ricinine itself is a less toxic compound and has been studied for its potential pharmacological properties, including hepatoprotective effects. |
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| DC47823 |
Lepidiline A
Featured
|
Lepidiline A shows cytotoxic activity against HL-60 cells with an IC50 of 32.3 μM. |
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| DC47847 |
Lepidiline C
Featured
|
Lepidiline C shows cytotoxic activity against HL-60 cells with an IC50 of 27.7 μM. |
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| DC47396 |
Abaloparatide (BA058)
Featured
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Abaloparatide (BA058, BIM-44058, ITM-058) is a novel 34-amino acid peptide selected to be a potent and selective activator of the parathyroid hormone receptor (PTH1R) signaling pathway with an IC50 of 0.117 nM in SOST analysis. |
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| DC58041 |
BMS-986176
Featured
|
AAK1-IN-1(BMS-986176) is a chemical probe for AAK1 and BIKE that potently targets the ATP-binding site (AAK1 Ki = 9.1 nM; BIKE Ki = 17 nM). Regarding kinase selectivity, only three kinases were observed to bind SGC-AAK1-1 within 30-fold of the KD of AAK1 in a KINOMEscan assay (DiscoverX) at 1 μM followed by KD determinations: RIOK1 (KD = 72 nM), RIOK3 (KD = 290 nM), and PIP5K1C (KD = 260 nM). In a live cell NanoBRET assay (Promega) SGC-AAK1-1 has potency for ectopically expressed full-length AAK1- and BIKE-Nluc fusion proteins (AAK1 IC50 = 230 nM; BIKE IC50 = 1.5 μM). |
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| DC58042 |
MRTX-282
Featured
|
MRTX-282 is a novel KRas G12D inhibitor. |
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