Repsox（ALK5 Inhibitor II）

Cas No.:	446859-33-2
Chemical Name:	1,5-Naphthyridine,2-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]-
Synonyms:	E-616452; SJN 2511; E616452; SJN2511; E 616452; SJN-2511
SMILES:	CC1=CC=CC(=N1)C2=C(C=NN2)C3=NC4=C(C=C3)N=CC=C4
Formula:	C₁₇H₁₃N₅
M.Wt:	287.32
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

RepSox is a potent and selective of the TGFβR-1/ALK5 inhibitor which inhibits ALK5 autophosphorylation with IC50 of 4 nM.

In Vitro:

RepSox also inhibits ATP binding to ALK5 with IC50 of 23 nM. RepSox shows potent activity in both binding and cellular assays and exhibits selectivity over p38 mitogen-activated protein kinase. with IC50 of >16 μM[1]. RepSox act s as an inhibitor of the Tgfβ1 kinase. Treatment with 25 μM RepSox almost completely eliminates Smad3 phosphorylation, indicating that RepSox strongly inhibits Tgfβ signaling in somatic cells. RepSox is most effective at replacing Sox2 during days 10-11 after transduction and that therefore cultures of Oct4, Klf4, and cMyc-transduced MEFs give rise to intermediates capable of responding to RepSox treatment. These intermediates appear at day 4 post-transduction and peak at days 10-11. Treatment with RepSox decreased the proportion of cells in G2/M phase of the cell cycle, indicating it does not increase the proliferation rate of these partially reprogrammed cells[2].

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC7739	SD-208	SD-208 is a potent, orally active ATP-competitive transforming growth factor-β receptor 1 (TGF-βRI) inhibitor (IC50= 49 nM)
DC6312	SB525334	SB525334 is a potent and selective inhibitor of TGFβ receptor I (ALK5) with IC50 of 14.3 nM, is 4-fold less potent to ALK4 than ALK5 and inactive to ALK2, 3, and 6.
DC5189	SB-431542	SB431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM, 100-fold more selective for ALK5 than p38 MAPK and other kinases.
DC7259	Repsox（ALK5 Inhibitor II）	RepSox(E-616452; SJN 2511) is a potent and selective inhibitor of the TGFβR-1/ALK5 with IC50 of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation, respectively.
DC7587	ML347	ML347 is a selective BMP receptor inhibitor with IC50 of 32 nM for ALK2, >300-fold selectivity over ALK3. Also inhibits ALK1 activity with IC50 of 46 nM
DC10675	LY3200882	LY3200882 is a novel, highly selective TGFβRI small molecule inhibitor.
DC6306	LY2157299(Galunisertib)	LY2157299 is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM. Phase 2.
DC7914	LDN-214117	LDN-214117 is a potent and selective ALK2 inhibitor with IC50 of 22 nM; > 100 fold selectivity for ALK5; also inhibits BMP6(IC50=100 nM).
DC7742	K02288	K02288 is a potent, and selective type I BMP receptor inhibitor with IC50 of 1.1, 1.8, 6.4 nM for ALK2, ALK1 and ALK6, showing weaker inhibition on other ALKs (3, 4, 5) and ActRIIA.
DC8028	ITD-1	ITD-1 is a novel and highly selective TGFβ pathway inhibitor. ITD-1 molecule turns stem cells into heart cells.