About 31 results found for searched term "CB1-IN-1" (0.773 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M5944 | Ruxolitinib phosphate | JAK |
| INCB018424 phosphate; INCB 018424 phosphate; INCB-018424 phosphate; Ruxolitinib | ||
| Ruxolitinib phosphate(INCB018424 phosphate) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3. | ||
| M9652 | CB1-IN-1 | Cannabinoid |
| DBPR211; BPRCB1184 | ||
| CB1-IN-1 is a novel potent restricted CB1R antagonist with Ki of 0.3 nM and 21 nM for CB1R and CB2R, respectively. | ||
| M14069 | Numidargistat dihydrochloride | Others |
| CB-1158 dihydrochloride; INCB01158 dihydrochloride | ||
| Numidargistat (CB-1158) dihydrochloride is a potent and orally active inhibitor of arginase, with IC50s of 86 nM and 296 nM for recombinant human arginase 1 and recombinant human arginase 2, respectively. Immuno-oncology agent. | ||
| M42232 | ABCB1-IN-1 | P-glycoprotein |
| ABCB1-IN-1 is a potent ABCB1 inhibitor. | ||
| M1787 | INCB18424 | JAK |
| Ruxolitinib | ||
| Ruxolitinib (INCB018424) is a first-in-class, potent, selective JAK1/2 inhibitor with an IC50 of 3.3 nM/2.8 nM. It is more than 130-fold more selective for JAK1, JAK2, and JAK3 than JAK3. It can be used in studies related to pemphigus, myelofibrosis and vitiligo. | ||
| M2720 | INCB024360 analogue | IDO |
| INCB14943 | ||
| INCB024360 is a potent IDO1 inhibitor (IC50 value of 10 nM) with desirable pharmaceutical properties. | ||
| M2981 | Rimonabant | Cannabinoid |
| SR141716 | ||
| Rimonabant is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane. | ||
| M3030 | S-Ruxolitinib | JAK |
| S-Ruxolitinib; INCB18424 | ||
| S-Ruxolitinib is the chirality of INCB018424, which is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3. | ||
| M5290 | (±)-SLV-319 | Cannabinoid |
| (±)-Ibipinibant; BMS-646256 | ||
| (±)-SLV319 (Ibipinabant) is a potent and selective CB1 receptor antagonist (Ki = 7.8 nM). Exhibits 1000-fold selectivity for CB1 over CB2 receptors. Inhibits CP 55,940-induced hypotension and WIN 55,212-2-induced hypothermia in vivo. | ||
| M5315 | Baricitinib phosphate | JAK |
| INCB028050; LY3009104 | ||
| Baricitinib phosphate(INCB 028050; LY 3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. | ||
| M5482 | CB1954 | Others |
| Tretazicar | ||
| CB1954(Tretazicar) is a anticancer prodrug that is converted in the presence of the enzyme NQO2 and co-substrate caricotamide ( EP-0152R) (EP) into a potent cytotoxic bifunctional alkylating agent. It can be activated by NAD(P)H quinone oxidoreductase 2. | ||
| M5555 | Decloxizine dihydrochloride | Histamine Receptor |
| UCB 1402 dihydrochloride | ||
| Decloxizine dihydrochloride(UCB-1402; NSC289116) is a histamine 1 receptor antagonist. | ||
| M6136 | Epacadostat | IDO |
| INCB024360 | ||
| Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM and displays high selectivity over other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO). | ||
| M8629 | Cbz-B3A | Others |
| Cbz-B3A is a potent and selective inhibitor of mTORC1 signaling that inhibits the phosphorylation of eIF4E binding protein 1 (4EBP1) and blocks 68% of translation. | ||
| M8641 | LP117 | Others |
| LP117 is a pirinixic acid derivative that interferes with ATP-binding cassette (ABC) transporter ABCB1-mediated substrates transport, including vincristine, vinorelbine, paclitaxel, and actinomycin D, but not doxorubicin, rhodamine 123, or JC-1. | ||
| M8876 | Itacitinib | JAK |
| INCB039110 | ||
| Itacitinib (INCB039110) is a potent, selective JAK1 inhibitor with an IC50 value of 2 nM for human JAK1. It has oral bioactivity and potential anti-tumor activity. | ||
| M9141 | SGC-CBP30 | Epigenetic Reader Domain |
| Sgc-cbp30 is a potent and highly selective CBP/ P300 bromine domain inhibitor (Kd of 21 nM and 32 nM against CBP and P300, respectively), which is 40 times more selective than BRD4 [BRD4(1)]. Sgc-cbp30 strongly reduces the secretion of IL-17A in Th17 cells and has anti-inflammatory effects. | ||
| M9561 | A-485 | Histone Acetyltransferase |
| A-485 is a potent and selective HAT inhibitor of p300/CBP in vitro with an IC50 of 10 nM in a p300 TR-FRET assay and 3 nM in a CBP TR-FRET assay with selectivity > 1000-fold over closely related HATs. | ||
| M9596 | Pemigatinib | FGFR |
| INCB054828 | ||
| Pemigatinib (INCB054828) is an orally effective, selective FGFR inhibitor with IC50 values of 0.4 nM, 0.5 nM, 1.2 nM, and 30 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.Pemigatinib exhibited anti-tumor activity in mouse xenograft models with FGFR1, FGFR2, or FGFR3-altered human tumors in a mouse xenograft model exhibiting antitumor activity. | ||
| M10373 | CB-103 | Notch |
| CB103; Limantrafin | ||
| CB-103 is a first-in-class, orally active inhibitor of the Notch transcription activation complex. CB-103 inhibits Notch signaling in primary human T cell acute lymphoblastic leukemia and other Notch-dependent human tumor cell lines, and concomitantly induces cell cycle arrest and apoptosis. | ||
| M10731 | ICCB-19 hydrochloride | Autophagy |
| ICCB-19 hydrochloride is a TRADD (TNFRSF1A associated via death domain) inhibitor. ICCB-19 hydrochloride binds to the N-terminal domain of TRADD (TRADD-N), breaking its binding to TRADD-C and TRAF2. ICCB-19 hydrochloride is an indirect inhibitor of RIPK1 kinase activity. ICCB-19 hydrochloride effectively induces autophagy and degradation of long-lived proteins. | ||
| M10891 | Taranabant | Others |
| MK-0364 | ||
| Taranabant is a potent and selective cannabinoid 1 (CB1) receptor reverse agonist that inhibits binding and the functional activity of multiple agonists, acting on human CB1R,Ki 0.13 nM. | ||
| M11354 | INCB086550 | PD-1/PD-L1 |
| PD-1/PD-L1-IN-8 | ||
| INCB086550 selectively inhibited PD-L1 with IC50 of 3.1 nM, 4.9 nM and 1.9 nM for human, rhesus monkey and rat pD-L1, respectively. INCB086550 could not inhibit the binding of PD-L2 to PD-1 at 10 μM. INCB086550 significantly inhibits the PD-1/PD-L1 signaling axis by binding to PD-L1 protein, leading to PD-L1 dimerization and internalization, and has good tumor suppressive effect in a variety of mouse tumor models. | ||
| M11512 | CBL0137 hydrochloride | p53 |
| Curaxin-137 hydrochloride; CBL-C137 hydrochloride | ||
| CBL0137 hydrochloride is an inhibitor of FACT, the histone molecule chaperone. FACT promotes the formation of chromatin transcription complexes. CBL0137 hydrochlorideye also activated p53 and inhibited NF-κB, with EC50 values of 0.37 and 0.47 μM, respectively. | ||
| M13389 | ACBI1 | PROTAC |
| ACBI1 is an effective and synergistic PROTAC inhibitor of SMARCA2, SMARCA4 and PBRM1, with DC50 of 6 nM, 11 nM and 32 nM in MV-4-11 cells, respectively. ACBI1 can induce antiproliferative effect and apoptosis. | ||
| M13820 | GNE-049 | Epigenetic Reader Domain |
| GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively. | ||
| M14248 | Dofequidar fumarate | P-glycoprotein |
| MS-209 | ||
| Dofequidar fumarate(MS-209 fumarate), an orally active quinoline compound, has been reported to overcome MDR by inhibiting ABCB1/P-gp, ABCC1/MDR-associated protein 1, or both. | ||
| M17348 | Olivetol | Cannabinoid |
| Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2. Olivetol also inhibits CYP2C19 and CYP2D6 activity, with IC50s of 15.3 μM, 7.21 μM and Kis of 2.71 μM, 2.87 μM, respectively. | ||
| M20613 | PF-CBP1 HCl | Epigenetic Reader Domain |
| PF-CBP1 HCl is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively. | ||
| M21098 | INCB13739 | Hydroxysteroid dehydrogenase |
| INCB13739 is an orally effective, selective and tissue-specific 11β-HSD1 (11β-hydroxysteroid dehydrogenase 1) inhibitor with IC50 values of 3.2 nM (11β-HSD1 enzyme) and 1.1 nM (11β-HSD1 PBMC), respectively.INCB13739 can be used in type 2 diabetes mellitus (T2DM) and obesity studies. | ||
| M21109 | Inobrodib | Epigenetic Reader Domain |
| CCS1477; CBP-IN-1; CBP/p300-IN-4 | ||
| Inobrodib (CCS1477, CBP-IN-1) is an orally active, potent and selective p300/CBP inhibitor. inobrodib binds to p300 and CBP with Kd values of 1.3 and 1.7 nM and has a 170/130 fold selectivity compared to BRD4 with a Kd of 222 nM. Inobrodib (CCS1477) acts by inhibiting the expression and function of androgen receptor (AR) and by inhibiting c-Myc. | ||
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