JL5|TGF beta Receptor (TGFBR) Inhitibor&Antagonist&Agonist|DC Chemicals

Cas No.:	2244238-50-2
Chemical Name:	4-(3-(4-(3-(quinolin-4-yl)pyrazolo[1,5-a]pyrimidin-6-yl)phenyl)propyl)morpholine
Synonyms:	BMP receptor inhibitor JL5
Formula:	C₂₈H₂₇N₅O
M.Wt:	449.558
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

JL5 is a novel potent, selective BMP receptor inhibitor with IC50 of 1, <5 and 2 nM for ALK2/ACVR1, ALK3/BMPR1A and ALK6/BMPR1B, respectively; shows much weaker acitivity against BMPR2, ALK5/TGFβR1 and TGFβR2 with IC50 of 8,510, 440 and 40 nM; shows a greater volume of distribution and suppresses the expression of Id1 and pTak1 in tumor xenografts, induces tumor cell death and tumor regression in xenograft mouse models without immune cells and humanized with adoptively transferred human immune cells.

MSDS

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MSDS_13385_DC31061_2244238-50-2

COA

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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.
DC8022	R-268712	Potent and selective inhibitor of the TGF-β type I receptor/ALK5 (IC50 = 2.5 nM). Exhibits ~ 5000-fold selectivity over p38 MAPK. Suppresses development of renal fibrosis in a unilateral ureteral obstruction model. Also reduces proteinuria, glomeruloscler
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.