SB-4 agonist| CAS#100874-08-6 | BMP4 agonist

MedKoo Cat#: 584949 | Name: SB-4 agonist

Description:

WARNING: This product is for research use only, not for human or veterinary use.

SB-4 is a potent BMP4 agonist.

Chemical Structure

SB-4 agonist

CAS#100874-08-6

Theoretical Analysis

MedKoo Cat#: 584949

Name: SB-4 agonist

CAS#: 100874-08-6

Chemical Formula: C14H10BrNOS

Exact Mass: 318.9666

Molecular Weight: 320.20

Elemental Analysis: C, 52.51; H, 3.15; Br, 24.95; N, 4.37; O, 5.00; S, 10.01

Price and Availability

Size	Price	Availability
200mg	USD 750.00	2 Weeks
500mg	USD 1,650.00	2 Weeks
1g	USD 2,950.00	2 Weeks
2g	USD 5,250.00	2 Weeks

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Related CAS #

No Data

Synonym

SB 4; SB4; SB-4; SB-4 agonist;

IUPAC/Chemical Name

2-[[(4-Bromophenyl)methyl]thio]benzoxazole

InChi Key

JDVOIBFEFVKUPL-UHFFFAOYSA-N

InChi Code

InChI=1S/C14H10BrNOS/c15-11-7-5-10(6-8-11)9-18-14-16-12-3-1-2-4-13(12)17-14/h1-8H,9H2

SMILES Code

BrC1=CC=C(CSC2=NC3=CC=CC=C3O2)C=C1

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO and ethanol

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

SB-4 is a BMP4 agonist (EC50 = 74 nM). It activates canonical BMP signaling and increases SMAD-1/5/9 phosphorylation, with no effect on p-SMAD-2, p-SMAD-3 or p-TAK1. SB-4 bypasses noggin-induced inhibition of type I BMP receptors. When used in combination, SB-4 enhances BMP4 signaling and embryonic stem cell differentiation.

In vitro activity:

SB-4 rapidly stimulated bone morphogenetic protein (BMP) signaling in human renal cells. Activation of BMP signaling by SB-4 increased the phosphorylation of key second messengers (SMAD-1/5/9) and also increased expression of direct target genes (inhibitors of DNA binding, Id1 and Id3) in canonical BMP signaling. Reference: J Biol Chem. 2019 Mar 1;294(9):3125-3136. https://pubmed.ncbi.nlm.nih.gov/30602563/

In vivo activity:

In patients with rheumatoid arthritis, there was similarity in drug persistence at week 52 between etanercept (reference) and SB-4 in both unmatched and matched analyses. These findings suggesting comparable outcomes between etanercept and SB-4 for rheumatoid arthritis status and drug persistence. Reference: Arthritis Care Res (Hoboken). 2023 Sep;75(9):1986-1995. https://pubmed.ncbi.nlm.nih.gov/36722450/

	Solvent	mg/mL	mM
Solubility
	DMSO	32.0	100.00
	Ethanol	6.4	20.00

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 320.20 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Hayaei Tehrani RS, Sayahpour FA, Esfandiari F. A comparison between BMP4 and SB4 in inducing germ line gene expression pattern during embryonic stem cells differentiation. Differentiation. 2022 Jan-Feb;123:9-17. doi: 10.1016/j.diff.2021.11.003. Epub 2021 Nov 24. PMID: 34864442. 2. Bradford STJ, Ranghini EJ, Grimley E, Lee PH, Dressler GR. High-throughput screens for agonists of bone morphogenetic protein (BMP) signaling identify potent benzoxazole compounds. J Biol Chem. 2019 Mar 1;294(9):3125-3136. doi: 10.1074/jbc.RA118.006817. Epub 2019 Jan 2. PMID: 30602563; PMCID: PMC6398139. 3. Haugeberg G, Bakland G, Rødevand E, Hansen IJW, Diamantopoulos A, Pripp AH. Effectiveness and Persistence in SB4- and Reference Etanercept-Treated Rheumatoid Arthritis Patients in Ordinary Clinical Practice in Norway. Arthritis Care Res (Hoboken). 2023 Sep;75(9):1986-1995. doi: 10.1002/acr.25092. Epub 2023 Mar 7. PMID: 36722450. 4. Luciano N, Fusaro E, Ditto MC, Ianniello A, Bellis E, Bruni C, Viapiana O, Gremese E, Migliore A, Romoli E, Conforti L, Govoni M, Matucci-Cerinic M, Selmi C. Effectiveness of SB4 Transition from Originator Etanercept in Rheumatoid Arthritis and Axial Spondyloarthritis: A Subgroup Analysis from the BENEFIT Study. Rheumatol Immunol Res. 2022 Apr 20;3(1):31-37. doi: 10.2478/rir-2022-0005. PMID: 36467021; PMCID: PMC9524806.

In vitro protocol:

In vivo protocol:

1. Haugeberg G, Bakland G, Rødevand E, Hansen IJW, Diamantopoulos A, Pripp AH. Effectiveness and Persistence in SB4- and Reference Etanercept-Treated Rheumatoid Arthritis Patients in Ordinary Clinical Practice in Norway. Arthritis Care Res (Hoboken). 2023 Sep;75(9):1986-1995. doi: 10.1002/acr.25092. Epub 2023 Mar 7. PMID: 36722450. 2. Luciano N, Fusaro E, Ditto MC, Ianniello A, Bellis E, Bruni C, Viapiana O, Gremese E, Migliore A, Romoli E, Conforti L, Govoni M, Matucci-Cerinic M, Selmi C. Effectiveness of SB4 Transition from Originator Etanercept in Rheumatoid Arthritis and Axial Spondyloarthritis: A Subgroup Analysis from the BENEFIT Study. Rheumatol Immunol Res. 2022 Apr 20;3(1):31-37. doi: 10.2478/rir-2022-0005. PMID: 36467021; PMCID: PMC9524806.

Bradford et al (2019) High-throughput screens for agonists of bone morphogenetic protein (BMP) signaling identify potent benzoxazole compounds. J.Biol.Chem. 294 3125 PMID: 30602563

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