Others

CAT # Product Name Description
CPDD2004 CU CPT 9a CU-CPT-9a is a specific antagonist of TLR8.
CPD1221 Revefenacin; TD 4208; GSK1160724; Yupelri Revefenacin (TD-4208; GSK1160724) is a potent mAChR antagonist; has a high affinity on M3 receptor with a Ki of 0.18 nM
CPD2807 BAY 293 BAY-293 is a potent SOS1 inhibitor that blocks RAS activation via disruption of the RAS-SOS1 interaction. BAY-293) selectively inhibits the KRAS-SOS1 interaction with an IC50 of 21 nM and is a valuable chemical probe for future investigations.
CPD1841 Resmetirom; MGL3196; VIA 3196 Resmetirom, or MGL-3196, shows outstanding safety in a rat heart model and is efficacious in a preclinical model at doses that showed no impact on the central thyroid axis.
CPDD1633 Adavivint; SM 04690; LORECIVIVINT A novel small molecule Wnt pathway inhibitor with EC50 of 3 nM in vitro; induces hMSC differentiation into mature, functional chondrocytes and decreases cartilage catabolic marker levels; significantly improves Osteoarthritis Research Society International (OARSI) histology scores and biomarkers in a rodent OA model.
CPDD1230 Verucerfont; GSK 561679; GSK 561679A; NBI 77860 Verucerfont, also known as GSK561679 and NBI77860, is a CRF-1 antagonist. Verucerfont blocks the CRH-1 receptor, and so reduces ACTH release following chronic stress.
CPDD1644 Rilzabrutinib; PRN1008 PRN1008 is a potent, selective and reversible covalent inhibitor of BTK ((IC50 = 1.3 ± 0.5 nM).) with extended PD effects in vivo.
CPD1017 Bardoxolone; CDDO; RTA 401 Bardoxolone is a novel nuclear regulator factor (Nrf-2) activator.
CPD112243 CCR2 antagonist 3 CCR2 antagonist 3 is an antagonist of chemokine receptor 2 (CCR2).
CPD108542 Tirabrutinib; ONO-4059 Tirabrutinib (ONO-4059) is an orally effective, highly selective Bruton's Tyrosine Kinase (BTK) inhibitor.
CPD110808 RMC 0331; RM 023 RMC-0331 (RM-023) is a highly efficient, selective, and orally bioavailable SOS1 inhibitor.
CPDB1593 Telaglenastat; CB-839 CB-839 an is orally bioavailable inhibitor of glutaminase, with potential antineoplastic activity.
CPD114656 (R)-Pirtobrutinib (R) Pirtobrutinib is a less active isomer of Pirtobrutinib. Pirtobrutinib is a highly selective and non covalent next-generation BTK inhibitor.
CPD2500 Olutasidenib; FT-2102 Olutasidenib is a potent, selective inhibitor of mutant Isocitrate dehydrogenase (IDH)1 for the treatment of acute myeloid leukemia
CPD9951 Batefenterol;GSK 961081; TD-5959 Batefenterol is a muscarinic antagonist and β2-adrenergic receptor (β2-AR) agonist (Kis = 1.4, 1.3, and 3.7 nM, for hM2, hM3, and hβ2-AR, respectively in a radioligand binding assay).
CPD3619 RTA dh404;CDDO-dhTFEA
CPD3236 methyl (4aS,6aR,6bR,8aR,12aR,12bR,14aR,14bS)-11...
CPDD0995 Bardoxolone methyl; CDDO Methyl ester; CDDOMe; ... The synthetic oleanane triterpenoid CDDO (Item No. 81035) is a Nrf2 activator that inhibits proliferation and induces differentiation and apoptosis in various cancer cells.
CPD100616 Emricasan Emricasan, also known as IDN 6556 and PF 03491390, is a first-in-class caspase inhibitor in clinical trials for the treatment of liver diseases. Emricasan (IDN-6556) decreases liver injury and fibrosis in a murine model of non-alcoholic steatohepatitis. IDN6556 facilitates marginal mass islet engraftment in a porcine islet autotransplant model. Oral IDN-6556 may lower aminotransferase activity in patients with chronic hepatitis C. Orally-administered PF-03491390 is retained in the liver for prolonged periods with low systemic exposure, exerting a hepatoprotective effect against alpha-fas-induced liver injury in a mouse model.
CPD100615 Q-VD-Oph QVD-OPH, also known as Quinoline-Val-Asp-Difluorophenoxymethylketone, is a broad spectrum caspase inhibitor with potent antiapoptotic properties. Q-VD-OPh prevents neonatal stroke in P7 rat: a role for gender. Q-VD-OPh has anti-leukemia effects and can interact with vitamin D analogs to increase HPK1 signaling in AML cells. Q-VD-OPh reduces trauma-induced apoptosis and improves the recovery of hind-limb function in rats after spinal cord injury
CPD100614 Z-DEVD-FMK Z-DEVD-fmk is a cell-permeable, irreversible inhibitor of caspase-3. Caspase-3 is a cysteinyl aspartate-specific protease which plays a central role in apoptosis.
CPD100613 Z-IETD-FMK MDK4982, also known as Z-IETD-FMK, is a potent, cell-permeable, irreversible inhibitor of caspase-8 and granzyme B., The Caspase-8 Inhibitor II controls the biological activity of Caspase-8. MDK4982 effectively inhibits influenza virus-induced apoptosis in HeLa cells. MDK4982 also inhibits granzyme B. MDK4982 has CAS#210344-98-2.
CPD100612 Z-VAD-FMK Z-VAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor. Z-VAD-FMK inhibits caspase processing and apoptosis induction in tumor cells in vitro (IC50 = 0.0015 - 5.8 mM).
CPD100611 Belnacasan Belnacasan, also known as VX-765, is designed to inhibit Caspase, which is an enzyme that controls the generation of two cytokines, IL-1b and IL-18. VX-765 has been shown to inhibit acute seizures in preclinical models. In addition, VX-765 has shown activity in preclinical models of chronic epilepsy. VX-765 had been dosed in over 100 patients in phase-I and phase-IIa clinical trials relating to other diseases, including a 28-day phase-IIa clinical trial in patients with psoriasis. It has completed the treatment phase of a phase-IIa clinical trial of VX-765 that enrolled approximately 75 patients with treatment-resistant epilepsy. The double-blind, randomized, placebo-controlled clinical trial was designed to evaluate the safety, tolerability and clinical activity of VX-765.
CPD100610 Maraviroc Maraviroc is an antiviral, potent, non-competitive CKR-5 receptor antagonist that inhibits binding of HIV viral coat protein gp120. Maraviroc inhibits MIP-1β-stimulated γ-S-GTP binding to HEK-293 cell membranes, indicating its ability to inhibit chemokine-dependent stimulation of GDP-GTP exchange at the CKR-5/G protein complex. Maraviroc also inhibits the downstream event of chemokine-induced intracellular calcium redistribution.
CPD100609 Resatorvid Resatorvid, also known as TAK-242, is a cell-permeable inhibitor of TLR4 signaling, blocking LPS-induced production of NO, TNF-α, IL-6, and IL-1β in macrophages with IC50 values of 1-11 nM. Resatorvid binds selectively to TLR4 and interferes with interactions between TLR4 and its adaptor molecules. Resatorvid provides neuroprotection in experimental traumatic brain injury: implication in the treatment of human brain injury
CPD100608 ASK1-Inhibitor-10 ASK1 Inhibitor 10 is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1). It is selective for ASK1 over ASK2 as well as MEKK1, TAK-1, IKKβ, ERK1, JNK1, p38α, GSK3β, PKCθ, and B-RAF. It inhibits streptozotocin-induced increases in JNK and p38 phosphorylation in INS-1 pancreatic β cells in a concentration-dependent manner.
CPD100607 K811 K811 is an ASK1-specific inhibitor that prolongs survival in a mouse model of amyotrophic lateral sclerosis. K811 efficiently prevented cell proliferation in cell lines with high ASK1 expression and in HER2-overexpressing GC cells. Treatment with K811 reduced sizes of xenograft tumors by downregulating proliferation markers.
CPD100606 K812 K812 is an ASK1-specific inhibitor discovered to prolong survival in a mouse model of amyotrophic lateral sclerosis.
CPD100605 MSC-2032964A MSC 2032964A is a potent and selective ASK1 inhibitor (IC50 = 93 nM). It blocks LPS-induced ASK1 and p38 phosphorylation in cultured mouse astrocytes and suppresses neuroinflammation in a mouse EAE model. MSC 2032964A is orally bioavailable and brain penetrant.

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