bcl-xl antagonist 2

Bcl-xL antagonist 2 is an effective and selective antagonist of Bcl-xL with an IC50 of 91 nM and a Ki of 65 nM. Bcl-xL antagonist 2 induces apoptosis in cancer cells and can be used in studies about chronic lymphocytic leukemia and non-Hodgkin’s lymphoma.

A2B receptor antagonist 2 hydrochloride is an antagonist of adenosine receptor A2B (Ki = 2.30 μM for rA1, 6.8 μM for rA2A, 3.44 μM for hA2B).

AMPA receptor antagonist-2 is an AMPA receptor antagonist.

CRTh2 antagonist 2 is a selective and potent CRTH2 antagonist, IC50≤10 nM. CRTh2 antagonist 2 can be used to study the direction of androgenic alopecia.

TLR7/8/9 antagonist 2 is an orally active and highly bioavailable vTLR7/8/9 antagonist. TLR7/8/9 antagonist 2 inhibits HEK/hTLR7, HEK/hTLR8 and HEK/hTLR9 with IC50s of 0.011 μM, 0.029 μM and 0,052 μM, respectively. TLR7/8/9 antagonist 2 can be used to study auto-inflammatory diseases such as systemic lupus erythematosus or lupus nephritis.

Sigma-1 receptor antagonist 2 is a potent and selective antagonist of sigma 1 receptor (σ1 R) (σ1 and σ2 receptor with Kis of 3.88 and 1288 nM , respectively).

AHR antagonist 2 is an antagonist of the aryl hydrocarbon receptor. The IC50s for human AHR and mouse AHR are 0.885 and 2.03 nM, respectively.

Bcl-2-IN-16 is a Bcl-2 (B-cell lymphoma 2) inhibitor [1].

Compound 39, also known as CB2 receptor antagonist 2, is a potent CB2 antagonist exhibiting an IC50 of 0.33 μM. It engages in strong interactions with residues L17, W6.48, V6.51, and C7.42 [1].

Bcl-2-IN-14 (Compound 13c), a BCL-2 inhibitor, exhibits an inhibitory concentration (IC 50) of 0.471 μM, and is applicable in cancer research [1].

Bcl-2-IN-12 (Compound 1) is a potent Bcl-2 inhibitor with an IC50 value of 6 nM, utilized in cancer research [1].

Bcl-2-IN-15 (Compound 13d) is a Bcl-2 inhibitor with an IC50 of 363 nM, which impedes the proliferation of the NCI leukemia cancer cell line [1].

MrgprX2 antagonist-2 is a potent antagonist of MrgprX2. It holds potential for investigating skin inflammatory disorders.

Bcl-2-IN-5 is a potent inhibitor of BCL-2, demonstrating inhibitory concentrations (IC50) of 0.12 nM, 0.14 nM, and 0.22 nM against wild type Bcl-2, Bcl-2 D103Y, and Bcl-2 G101V, respectively. Additionally, it effectively suppresses cell growth in Bcl 2-G101V knock-in RS4;11 cells, with IC50 values of 0.2 nM and 0.44 nM.

Compound 29 is a 5-HT6R antagonist that acts by inhibiting the 5-HT6 receptor.

CB1 antagonist 2 (AM4113) is caimabinoid 1 (CB1) antagonist which inhibits CB1 in vivo with an IC50 of 25.5 nM.

Beclin1-Bcl-2 Interaction Inhibitor 1 effectively disrupts the binding of Beclin 1 to Bcl-2, and is utilized in cancer and neurodegeneration research [1].

Bcl-2-IN-13 is a potent inhibitor of Bcl-2, exhibiting an IC50 of 17 nM, and holds potential for use in cancer research [1].

OT-R antagonist 2 is a nonpeptide low molecular weight antagonist of OT-R .

PROTAC Bcl-xL degrader-3 is a potent ROTAC Bcl-xL degrader.

MCL-1/BCL-2-IN-4 is a selective and potent Mcl-1 and Bcl-2 dual inhibitor.

GPVI antagonist 2 (Compound 1) is a potential Glycoprotein VI (GPVI) antagonist, able to act on collagen (IC50: 0.35 μM), CRP (IC50: 0.80 μM), convulxin (IC50: 195.2 μM), thrombin (IC50. 81.38 μM). GPVI antagonist 2 is a promising anti-platelet agent.

TAT-BH4 (Bcl-xL) TFA, primarily localized at the mitochondria, inhibits apoptotic cell death. This compound comprises an eosin-labeled cysteine at the N-terminal and the protein transduction domain from the HIV TAT protein (amino acids 49 to 57), fused to the Bcl-xL BH4 peptide. It is utilized in research concerning diseases associated with accelerated apoptosis [1].

ET Receptor Antagonist 2 (Compound 16j) is an orally active ET receptor antagonist with an IC50 of 0.22 nM, suitable for pulmonary arterial hypertension (PAH) research. It has been shown to mitigate monocrotaline-induced PAH in a rat model [1].

Bcl-2-IN-9 is a novel, pro-apoptotic, low cytotoxic Bcl-2 inhibitor (IC50: 2.9 μM). Bcl-2-IN-9 downregulates Bcl-2 expression, induces apoptosis in cancer cells, and exhibits high selectivity for leukemia cells.

NOD1/2 Antagonist-1 is a potent dual inhibitor of nucleotide-binding oligomerization domain-like receptors 1 and 2 (NOD1/2), displaying inhibitory concentrations (IC50) of 1.13 μM for NOD1 and 0.77 μM for NOD2. It exhibits an acceptable half-life (T1/2) of 67.6 minutes. Additionally, NOD1/2 Antagonist-1 enhances the antitumor efficiency of Paclitaxel (PTX).

5-HT3 antagonist 2 is an antagonist of 5-HT3 receptor.

Protease-Activated Receptor-1 Antagonist 2 is an orally active antagonist of protease-activated receptor-1 (PAR-1), demonstrating significant potency with an IC 50 of 7 nM. It exhibits favorable pharmacokinetic characteristics, making it valuable in cardiovascular disease (CVD) research, including studies on atherosclerosis and restenosis [1].

Compound A-26, also known as FXR antagonist 2, is a diarylamide derivative that functions as a moderate FXR antagonist. It is utilized in researching hyperlipidemia and type 2 diabetes [1].

AT1R antagonist 2 is a potent AT1R selective ligand with good AT1R affinity (Ki: 26 nM).

EP2 receptor antagonist-2 (CID891729) is a compound that not only serves as an antagonist to the EP2 receptor, blocking its activation by PGE2, but also reduces lactate dehydrogenase (LDH) release triggered by N-methyl-D-aspartate (NMDA).

NMDA receptor antagonist 2 is a highly potent and orally active NR2B subtype-selective antagonist of the N-methyl-D-aspartate (NMDA) receptor. It exhibits remarkable binding affinities, with an IC50 of 1.0 nM and a Ki value of 0.88 nM. This compound finds valuable application in scientific investigations focusing on neuropathic pain and Parkinson’s disease.

CXCR2 antagonist 2 is a potent CXCR2 antagonist for cancer immunotherapy with an IC 50 value of 95 nM.

The compound is an a1/a3 adenosine receptor antagonist, which helps to treat (neurological) inflammatory diseases.

GRPR antagonist-2 is a potent antagonist of the gastrin-releasing peptide receptor (GRPR) and exhibits anticancer effects by being cytotoxic to certain cancer cells (able to act on HGC-27 cells (IC50: 0.77 μM) and Pan02 cells (IC50: 2.5 μM)).

Calcium Channel antagonist 2 is a calcium channel antagonist (IC50=5-20 μM) that can be used to study diseases due to Ca2+ channels like pain and diabetes.

AR antagonist 2 (compound 58) is a potent inhibitor of the androgen receptor (AR) (IC50: 0.95 μM).

LXR antagonist 2 (compound 10rr) is a potent LXR (liver X receptor) inverse agonist, acting on LXRβ (IC50: 0.36 μM) and LXRα (IC50: 2.25 μM). LXR antagonist 2 is an adipogenesis inhibitor that downregulates LXR target genes SREBP-1c, ACC, FAS and SCD-1. LXR antagonist 2 exhibits hypolipidemic activity in Triton WR-1339-induced hyperlipidemic mice.

GPR84 Antagonist 2, a potent and selective GPR84 antagonist (IC 50 = 8.95 nM), demonstrates oral activity and significantly enhances potency in calcium mobilization assays. It effectively inhibits neutrophil and macrophage chemotaxis following GPR84 activation, highlighting its research potential for ulcerative colitis.

PROTAC Bcl-xL degrader-1 is a potent PROTAC composed of a Bcl-xL (Bcl-2 family member) ligand-binding group, a linker, and an IAP E3 ligases binding group, demonstrating effectiveness as a Bcl-xL degrader. It exhibits toxicity towards human platelets and MyLa 1929 cells, with IC50 values of 62 nM and 8.5 μM, respectively [1].

PROTAC Bcl-xL ligand-1 serves as a ligand targeting Bcl-xL, essential in synthesizing PROTACs [1].

Bcl-2-IN-4, an orally active and selective inhibitor of Bcl-2, demonstrates potent efficacy with an IC50 value of 1.5 nM and exhibits more than 200-fold selectivity over Bcl-xL (IC50 of 411 nM). Additionally, it effectively inhibits the proliferation of RS4;11 cells, achieving an IC50 of 2.7 nM.

LPA2 antagonist 2 is ＞480-fold more selective than LPA3 (IC50 of 13.85 μM).LPA2 antagonist 2 is a selective LPA2 antagonist with an IC50 of 28.3 nM and a Ki of 21.1 nM.

Bcl-2/Mcl-1-IN-3 is a Bcl-2/Mcl-1 inhibitor that acts on Mcl-1 (Ki: 0.14 μM) and Bcl-2 (Ki: 0.23 μM) and can be used in cancer research.

Bcl-2/Mcl-1-IN-2 is a Bcl-2 (Ki: 4.70 μM) and Mcl-1 (Ki: 0.88 μM) inhibitor.Bcl-2/Mcl-1-IN-2 can be used in cancer research.

Dopamine D3 receptor antagonist-2 is a dopamine D3 receptor selective (Ki=2.16 nM) or multi-targeting dual ligand that shows potential effects in CNS disorders.

Estrogen receptor antagonist 2 is a selective down-regulator of estrogen receptor. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development. estrogen receptor antagonist 2 has research potential for breast cancer disease.

A2B receptor antagonist 2 is an antagonist of adenosine receptor A2B (Ki = 2.30 μM for rA1, 6.8 μM for rA2A, 3.44 μM for hA2B).

LTB4 antagonist 2, a carboxamide-acid compound, serves as an antagonist to leukotriene B4 (LTB4), possessing potential anti-inflammatory properties. It exhibits high affinity for the LTB4 receptor, with an inhibitory concentration (IC50) of 439 nM [1].

TAT-BH4 (Bcl-xL), primarily localized at the mitochondria, inhibits apoptotic cell death. This compound comprises an N-terminal eosin-labeled cysteine and the protein transduction domain of the HIV TAT protein (amino acids 49 to 57), fused to the Bcl-xL BH4 peptide. It serves as a tool for research into diseases characterized by accelerated apoptosis [1].