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MRT 10. Group: Biochemicals. Grades: Purified. CAS No. 330829-30-6. Pack Sizes: 10mg, 50mg. US Biological Life Sciences.
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Adagrasib
Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction [1] [2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: MRTX849. CAS No. 2326521-71-3. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg; 100 mg; 500 mg. Product ID: HY-130149.
CCG-100602
CCG-100602 inhibits RhoA/C-mediated, SRF-driven luciferase expression in PC-3 prostate cancer cells with an IC50 value of 9.8 μM. CCG-100602 specifically blocks the nuclear localization of MRTF-A, thereby inhibiting the fibrogenic transcription factor SRF. Synonyms: CCG-100602; 1207113-88-9; 1-[3,5-bis(trifluoromethyl)benzoyl]-N-(4-chlorophenyl)piperidine-3-carboxamide; CHEMBL603141; compound 4g [PMID: 19963382]; 1-(3,5-bis(trifluoromethyl)benzoyl)-N-(4-chlorophenyl)piperidine-3-carboxamide; CCG100602; CCG 100602; GTPL6764; SCHEMBL1534209; BDBM50436237; AKOS040744973; MS-28902; HY-120855; CS-0079376; Q27075763; [3,5-bis(trifluoromethyl)benzoyl]-N-(4-chlorophenyl)piperidine-3-carboxamide; 1-[3,5-bis (trifluoromethyl)benzoyl]-N-(4-chlorophenyl)-3-piperidinecarboxamide. Grade: 98%. CAS No. 1207113-88-9. Molecular formula: C21H17ClF6N2O2. Mole weight: 478.8.
Crospovidone
United States Pharmacopeia (USP) Reference Standard. Group: Pharmacopeia & metrological institutes standardseuropean pharmacopoeia (ph. eur.)pharmacopoeial standards. Alternative Names: K 85 (vinyl polymer), PVP K 29/32, Polyvinylpyrrolidon XL, PVP-K 10, PVP-K 90K95, Polyvidon XL, K 30W, MRTU 8457-79, YK 001, Polyvidone, Protagent, Neohemodes, Kollidon K 60, N-Vinylpyrrolidone polymer, PVP 10, Polyvinylpyrrolidone, Agrimer 15, Poly(N-vinyl-2-pyrrolidinone), 40K (vinyl polymer), PVP 4000, Luvitec K 40, Povidone K 25, Agrimer K 30, Konkrepol AD 1, Polyvinyl polypyrrolidone, Pvpon K.
GNF179
GNF179 exhibits a low clearance (CL=22 ml/min/kg, ~25% of hepatic blood flow in mice), a large volume of distribution (steady-state volume of distribution, Vss=11.8 l/kg), a moderate residence time (MRT=9 hours) and suitable terminal half-life (t1/2=8.9 hours). GNF179 reduced Plasmodium berghei parasitemia levels by 99.7% with a single 100 mg/kg oral dose, and prolonged mouse survival by an average of 19 days. GNF179 was able to protect against an infectious P. berghei sporozoite challenge with a single oral dose at 15 mg/kg while NITD609 was not. Synonyms: GNF 179; GNF-179. Grade: >98%. CAS No. 1261114-01-5. Molecular formula: C22H23ClFN5O. Mole weight: 427.9.
GNF179 Metabolite
GNF179 exhibits a low clearance (CL=22 ml/min/kg, ~25% of hepatic blood flow in mice), a large volume of distribution (steady-state volume of distribution, Vss=11.8 l/kg), a moderate residence time (MRT=9 hours) and suitable terminal half-life (t1/2=8.9 hours). GNF179 reduced Plasmodium berghei parasitemia levels by 99.7% with a single 100 mg/kg oral dose, and prolonged mouse survival by an average of 19 days. GNF179 was able to protect against an infectious P. berghei sporozoite challenge with a single oral dose at 15 mg/kg while NITD609 was not. Synonyms: GNF 179 Metabolite; GNF-179 Metabolite. Grade: >98%. CAS No. 1310455-86-7. Molecular formula: C14H16FN3. Mole weight: 245.3.
LC-2
LC-2 is a potent and first-in-class von Hippel-Lindau-based PROTAC capable of degrading endogenous KRAS G12C, with DC50s between 0.25 and 0.76 ?M[1]. LC-2 covalently binds KRAS G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS G12C degradation leading to suppression of MAPK signaling in both homozygous and heterozygous KRAS G12C cell lines[2]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2502156-03-6. Pack Sizes: 1 mg; 5 mg; 10 mg; 25 mg. Product ID: HY-137516.
MRT199665
MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPK?1/AMPK?2, and SIK1/SIK2/SIK3, respectively[1]. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells[2]. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370[3]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1456858-57-3. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg. Product ID: HY-120877.
MRT-2359
MRT-2359 is a potent, orally active and selective GSPT1 depressant (IC50: >30 nM and <300 nM) that specifically induces apoptosis dependent on protein translation. MRT-2359 exhibits significant and preferred anti-proliferative activity in a variety of cancer cell lines, especially MYC-driven cell lines, such as non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) with high expression of N-Myc or L-Myc. MRT-2359 inhibits the growth of drug-resistant NSCLC and SCLC cells, making it suitable for cancer research[1][2][3][4][5]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2803881-11-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-153356.
MRT67307
MRT67307 is a dual inhibitor of the IKKε and TBK-1 with IC 50 s of 160 and 19 nM, respectively [1]. MRT67307 also inhibits ULK1 and ULK2 with IC 50 s of 45 and 38 nM, respectively. MRT67307 also blocks autophagy in cells [2]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1190378-57-4. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-13018.
MRT 67307 dihydrochloride
MRT 67307 dihydrochloride. Group: Biochemicals. Grades: Purified. Pack Sizes: 10mg, 50mg. US Biological Life Sciences.
Worldwide
MRT68921
MRT68921 is a potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively. Uses: Scientific research. Group: Signaling pathways. CAS No. 1190379-70-4. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg. Product ID: HY-100006.
MRT68921 dihydrochloride
MRT68921 dihydrochloride is a potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively[1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2080306-21-2. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-100006A.
MRT-83
MRT-83 is a potent antagonist of Smo , with an IC 50 in the nanomolar range. MRT-83 also blocks Hedgehog (Hh) signaling. Uses: Scientific research. Group: Signaling pathways. CAS No. 1263131-92-5. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-18287.
MRT-83 hydrochloride
MRT-83 (hydrochloride) is the potent antagonist of Smoothened ( Smo ) receptor. MRT-83 (hydrochloride) inhibits the Hedgehog (Hh) signaling pathway and BODIPY-cyclopamine binding to human Smo. MRT-83 (hydrochloride) has the potential for researching cancer disease [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1359944-60-7. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-18287A.
MRTX0902
MRTX0902 is an orally active and potent SOS1 inhibitor with an IC 50 of 46 nM (WO2021127429A1; Example 12-10) [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2654743-22-1. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-145926.
MRTX1133
MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations[1][2]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2621928-55-8. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg; 200 mg; 500 mg. Product ID: HY-134813.
Navlimetostat
Navlimetostat is a potent, orally active, selective PRMT5-MTA complex inhibitor, with IC50 of 3.6 and 20.5 nM for PRMT5-MTA and PRMT5. Navlimetostat binds to the PRMT5-MTA complex, with KD value of 0.14 pM. Navlimetostat shows antineoplastic activity in vitro and in vivo, and can be used for cancer study[1][2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: MRTX-1719. CAS No. 2630904-45-7. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-139611.
(S)-Navlimetostat
(S)-Navlimetostat (example 16-7) is the S-enantiomer of Navlimetostat. (S)-Navlimetostat is a PRMT5/MTA complex inhibitor, with an IC 50 of 7070 nM [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: (S)-MRTX-1719. CAS No. 2630904-44-6. Pack Sizes: 1 mg; 5 mg; 10 mg. Product ID: HY-139611B.
Tazemetostat
Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a K i value of 2.5 nM. Tazemetostat inhibits EZH2 with IC 50 s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat inhibits rat EZH2 with an IC 50 of 4 nM. Tazemetostat also inhibits EZH1 with an IC 50 of 392 nM. Tazemetostat induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: EPZ-6438; E-7438. CAS No. 1403254-99-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg; 200 mg. Product ID: HY-13803.
A cell-permeable acylguanidine compound that is shown to block Hh signaling and act as a potent, reversible and high-affinity Smo (Smoothened) antagonist. Displays 20-60 -fold greater potency than Cyclopamine and competitively inhibits bodipy-cyclopamine binding to Smo (IC50 = 4.6 and 14nM in HEK293-hSMO and HEK293-mSMO cells, respectively). Represses ShhN (N-myristoylated Shh) signaling (IC50=15nM for Gli-dependent luciferase activity in Shh-light2 cells) and SAG- induced C3H10T1/2 cell differentiation (IC50=10nM in an alkaline phosphatase activity assay). Inhibits ShhN (3nM) and SAG (10nM)-mediated proliferation of rat cerebellar granule cell precursors (IC50 ~3 and 6nM, respectively). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg. US Biological Life Sciences.
A cell-permeable BX795 analog that acts as a potent, ATP-competitive, and reversible dual kinase inhibitor of TBK1/IKK epsilon (IC50 = 19 and 160nM, respectively) with excellent selectivity over IKKalpha and IKKbeta (IC50 > 10uM). Interacts with the TBK1 kinase dimer interface and stabilizes the inactive DFG-out conformation. Also blocks the activity of MARK (microtubule- associated protein (MAP)-microtubule affinity regulating kinase) 1, 2, 3, and 4 (IC50 = 27, 52, 36, and 41nM, respectively), SIK2 (IC50 = 67nM) and Aurora B, JAK2, and MLK1,3 (> than 90% inhibition at 1uM) in a 108-kinase panel. Increases TNF-alpha-stimulated NF-kB-dependent gene transcription in wild-type macrophages and enhances CREB-dependent gene transcription by promoting dephosphorylation of CREB-regulated transcription coactivator (CRTC3). Shown to aid TLR-stimulated production of anti-Inflammatory cytokines in macrophages while suppressing the secretion of pro-inflammatory cytokines. In response to pro-inflamm Group: Biochemicals. Grades: Highly Purified. CAS No. 495-85-2. Pack Sizes: 5mg. Molecular Formula: C??H??N?O?. US Biological Life Sciences.
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